bluuebunny/crossref_metadata_2025 huggingface dataset:
Synthesis of hydroxy, epoxy, nitrato and methoxy derivatives of tetralins and naphthalenes
Authors: Erenler Ramazan , Demirtas Ibrahim , Buyukkidan Bulent , Cakmak Osman
Published: December 2009

Stereoselective syntheses are described for cis,trans,cis-2,3,5-tribromo-1,4-dihydroxytetralin, trans,trans,cis-2,3,5-tribromo-1,4-dihydroxytetralin, trans,trans,trans-1,4-dihydroxy-2,3-dibromotetralin, trans,trans,trans-1-hydroxy-2,3,4-tribromotetralin, cis,cis,cis-1,2-epoxy-3,5-dibromo-4-hydroxytetralin, anti-1,2:3,4-diepoxytetralin, 1-hydroxy-4-bromonaphthalene, trans,trans,trans-1,4-dinitrato-2,3-dibromotetralin, 1-nitrato-2,3,4-tribromotetralin, 2,3-dibromonaphthalene and 1-methoxy-4-nitrato-2,3-dibromonaphthalene. These isomeric arene oxides and disubstituted naphthalenes provide excellent precursors for a number of 1,4- and 2,3-disubstituted naphthalene derivatives that are difficult to prepare using other routes. The structures of the naphthalene and tetralin derivatives were assigned by NMR and other techniques.
A facile stereoselective synthesis of 1,4-dienyl sulfides via Stille coupling reactions of (E)-α-stannylvinyl sulfides with allylic bromides
Authors: Wang Dong , Hao Wenyan , Cai Mingzhong
Published: December 2009

( E)-α-Stannylvinyl sulfides 1 underwent Stille coupling reactions with allylic bromides 2 in DMF at room temperature in the presence of Pd(PPh3)4 and CuI co-catalyst to afford stereoselectively 1,4-dienyl sulfides 3 in good yields.
Synthesis and X-ray crystallographic analysis of some 1,6-dihydro-1,2,4,5-tetrazines
Authors: Hu Wei-Xiao , Xu Feng
Published: December 2009

Eight 1,6-dihydro-1,2,4,5-tetrazines (2a–2h) were synthesised by reaction of sodium borohydride with 3,6-substituted-1,2,4,5-tetrazines. The structure of 2c was confirmed by single-crystal X-ray diffraction. The central six-membered ring of 2c has an obvious unsymmetrical boat conformation. It could be considered that the molecule has a homoaromaticity.
A convenient route to 2-substituted benzothiazole-6-carboxylic acids using nitrobenzene as oxidant
Authors: Charris Jaime , Camacho José , Ferrer Rosa , Lobo Gricela , Barazarte Arthur , Gamboa Neira , Rodrigues Juan , López Simón
Published: December 2009

Various substituted benzothiazole-6-carboxylic acids (4a–i) have been prepared by the condensation of 4-amino-3-mercaptobenzoic acid and aldehydes in nitrobenzene as oxidant. Compound 4i was found to be a good candidate as an inhibitor of β-hematin formation in vitro.
A mild synthesis of α,α′-[iminobismethylene]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol]
Authors: Bai Yihui , Chen Xinzhi
Published: December 2009

A new synthesis of α,α′-[iminobismethylene]bis[6-fluoro-3,4-dihydro-2 H-1-benzopyran-2-methanol (1) is described, with most reactions being carried out at room temperature and normal pressure, that will further contribute to the development of new scalable synthesis of the related drug substance of Nebivolol (overall yield: 33%).
Intermolecular interactions of sulfur trioxide and sulfuric acid dimers studied by the DFT method
Authors: Zhou Su-Qin , Ju Xue-Hai , Fan Xiao-Wei
Published: December 2009

Density functional theory with 6-311++G** basis sets has been applied to the investigation of intermolecular interactions of sulfur trioxide and sulfuric acid dimers. Counterpoise procedure was used for the basis set superposition error (BSSE) correction. The corrected binding energy for (HSO4) 2 is −71.37 kJ/mol at the B3LYP/6-311++G** level, and −37.79 and −39.04 kJ/mol for two H2SO4/SO3 binary complexes (denoted as dimers B and C) respectively. Dimers B and C can be spontaneously produced when gaseous sulfur trioxide mixes with sulfuric acid, which is in agreement with the experimental fact that sulfur trioxide is prone to dissolve in sulfuric acid. The O…S interacting is stronger than the O…H interacting in the heterodimer of H2SO4/SO3. Electron density at bond critical points and natural bond orbital analysis were performed to probe the origin of the intermolecular interactions.
The transformation of 2,6-di-tert-butyl-4-(alkylamino)methylphenols to N,N-bis(3,5-di-tert-butyl-4-hydroxylbenzyl)-N-alkylamines
Authors: Zeng Tao , Chen Ligong , Li Jiangsheng , Zhang Yuecheng , Deng Yi
Published: December 2009

Several derivatives of N,N-bis(3,5-di-tert-butyl-4-hydroxybenzyl)- N-alkylamines were isolated in the reduction of the imines obtained from 3,5-di-tert-butyl-4-hydroxylbenzaldehyde and primary amines. Experimental results showed that they were transformed from the corresponding 2,6-di-tert-butyl-4-alkylaminomethylphenols.
Diazotisation of aromatic amines and solvolysis of diazonium salts in ethylene glycol ethers
Authors: Ram Ram N. , Singh Virinder
Published: December 2009

Aniline and unhindered alkyl-substituted anilines undergo solvolysis in dioxane and DME saturated with dry hydrogen chloride on diazotisation with isoamyl nitrite to give 2-(2-chloroethoxy)ethyl aryl ethers and 2-methoxyethyl aryl ethers respectively in 36-47% yields. 2,6-Dialkyl-substituted anilines give the corresponding chloro compounds as the major product along with the aryl ethers in lower yields. Diazotisation of aniline in ethylene glycol and monomethyl ethers of ethylene glycol and diethylene glycol gave the corresponding alcoholysis products in low yields. The solvolysis of aniline did not occur on diazotisation in diethyl ether or THF.
First total synthesis of Saurufuran B via regioselective alkylation
Authors: Yang Yihua , Li Yulin
Published: December 2009

Saurufuran B (1), a furanditerpene isolated from the root of Saururus chinensis, was prepared in a highly efficient manner by regioselective alkylation from ( E, E)-farnesol (8) and the readily available citraconic anhydride (5).
Synthesis of New Class of Phosphorus and Oxygen Macroheterocycles
Authors: Kasthuraiah Maddali , Reddy Kachi Reddy Kishore Kumar , Balakrishna Avula , Reddy Cirandur Suresh , Reddy Chichili Devendranath
Published: December 2009

New class of macrocyclic aryloxy phosphoranes (10a–d, 11a–d, 12a–d) were prepared by reactants the bifunctional synthons (7–9) with bis(2/3-chloroalkyl)phenyl triester of phosphoric acid (5a–d) in the presence of aq.NaOH in n-BuOH in moderate yields. Their chemical structures were established by analytical and spectral (IR, 1H, 13C and 31P and Mass) data.
Synthesis and Crystal Structure of Ethyl 7-Chloro-3-Amino-9-(4-Bromophenyl)Thieno-[3,2-b]Benzothiazine 4,4-Dioxide 2-Carboxylate
Authors: Charris Jaime , Barazarte Arthur , Ferrer Rosa , Camacho José , Gamboa Neira , Rodrigues Juan , Atencio Reinaldo , González Teresa
Published: December 2009

The X-ray crystal structure of 7-chloro-3-amino-9-(4-bromophenyl)thieno-[3,2-b]benzothiazine 4,4-dioxide 2-carboxylate 1 is determined. The thiophene ring and the exocyclic ester group adopt a co-planar conformation, which is stabilised by an intramolecular hydrogen bond. The moderate antimalarial activity shown by this compound appears to be related to the formation of such an intramolecular N–H···O =C hydrogen bond.
A New Sesquiterpene from the Seeds of Physalis Alkekengi L. var. Franchi
Authors: Zhan Zha-Jun , Li Cheng-Ping , Shan Wei-Guang
Published: December 2009

A new sesquiterpene, named as 13-hydroxy-3,11-(7αH, 10βH)-acordien-3-one (1), and a known norsesquiterpene 3β-hydroxy-5α, 6α-epoxy-7-megastigmen-9-one (2) were isolated from the seeds of Physalis alkekengi L. var. franchi. The structure of 1 was established by spectroscopic methods. Compound 1 was found to show modest antibacterial activity.
Synthesis and Tautomeric Structure of the Azo-Coupling Products of 2-Methyl-7-Phenylpyrimido[1,2-b][1,2,4]triazepine-4,9(3H,5H)-dione
Authors: Shawali Ahmad S. , Sherif Sherif M. , Farghaly Thoraya A. , Shehata M.R. , Darwish Manal A.A.
Published: December 2009

A simple synthetic strategy is described for synthesis of 3-arylazo-2-methyl-7-phenylpyrimido[1,2- b][1,2,4]triazepine-4,9-diones 4a–j. The acid dissociation constants were determined for the series prepared and were correlated by a Hammett-type equation using enhanced substituent constants. The results of such correlation together with the spectral data, including 15N isotopic labelling, indicated that the studied compounds exist predominantly in the hydrazone tautomeric form.
Phenolic Structure and Colour in Mannich Reaction Products
Authors: Tyman John H.P. , Patel Mahesh
Published: December 2009

Mannich reactions have been carried out with a variety of model alkylphenols and dimethylamine, methylamine, and diethylenetriamine to trace the origin of persistent coloured products occurring in related reactions with pentadeca(e)nylphenol and 4- tert-alkylphenols. It was found to be attributable to the presence of resorcinolic impurities.
The Synthesis of Benzhydroximoyl Chloride and Nitrile Oxides under Solvent Free Conditions
Authors: Bigdeli Mohammad A. , Mahdavinia Gholam Hossein , Jafari Saeed
Published: December 2009

Benzhydroximoyl chlorides were prepared as nitrile oxide precursors with acidic (HCl) silica gel/Oxone in solvent less media in excellent yields with the selective chlorination of aldoximes vs. aromatic substitution. Nitrile oxides were generated by Huisgen's method in solvent free conditions and were trapped via reactions with styrene yielding isoxazolines. The one pot preparation of isoxazolines from substituted benzaldehyde oximes was successfully investigated.
Trichlorocyanuric Acid: An Efficient Reagent for One-Pot Synthesis of Ptychodiscus Brevis (PB-1) Toxin and its Derivatives
Authors: Gupta Arvind K. , Acharya Jyotiranjan , Dubey Devendra K. , Kaushik Mahabir P.
Published: December 2009

Trichlorocyanuric acid is an efficient regent for simple and one-pot synthesis of dialkyl, N-cycloctylphosphoraamidates (PB-1) and its various derivatives in excellent yields. The procedure is operationally simple and involves the reaction of various dialkylphosphites with trichloroisocyanuric acid in acetonitrile and subsequent treatment with amines in presence KF-celite to give PB-1 and derivatives.
Simple Efficient Synthesis of Pyranoquinoline Alkaloids: Flindersine, Khaplofoline, Haplamine and their Analogues
Authors: Thangavel Dhanabal , Ravindran Sangeetha , Moonsamy Gengan Robert , Palathurai Mohan Subramaniam
Published: December 2009

An efficient two step synthesis of pyranoquinoline alkaloids is described. Direct treatment of isoprene with 4-hydroxyquinolin-2(1H)-one in the presence of polyphosphoric acid furnished dihydroflindersine in good yield, and which on dehydrogenation led to a new synthesis of flindersine. Khaplofoline, a linear pyranoquinoline alkaloid, was obtained as a minor product. The syntheses of derivatives are also documented.
Regio- and Stereoselectivity in 1,3-dipolar Cycloaddition Reaction of 2-diazopropane with Benzylidene-N-arylsuccinimide and Benzylidene-N-arylmethylsuccinimide Derivatives: Synthesis of Gem-dimethylcyclopropane
Authors: Hamadi Naoufel Ben , Msaddek Moncef
Published: December 2009

1,3-dipolar cycloaddition of 2-diazopropane with (E)-benzylidene-N-arylsuccinimide and (E)-benzylidene-N-arylmethylsuccinimide derivatives is taking place regiospecifically to give a new spiro-pyrazolines. The reaction of 2-diazopropane with (E)-benzylidene-N-arylmethylsuccinimide derivatives is diastereospecific. Irradiation of the pyrazoline led to clean extruction of nitrogen to give the new spiro-cyclopropanes.
[4+2] Diels–Alder Cycloaddition Reaction of 2-benylidineamino-4-phenyl-1,3-thiazoles with Sulfene and their Antifungal Activities
Authors: Borthakur Susanta Kr. , Boruah Paran , Goswami Birendra N.
Published: December 2009

2-Benzylidineamino-4-phenyl-1,3-thiazole undergoes [4+2] Diels–Alder cycloaddition reaction with sulfene resulting in good yield of a mixture of isomeric 2,6-diphenyl-2H,4H-[1,3]thiazolo[3,2-c][1,3,5]thiadiazine 3,3-dioxides and 3, 7-diphenyl[1,3]thiazolo[3,2-b] [1,2,4]thiadiazine 5,5-dioxides derivatives are reported.
Correlation Analysis in the Benzylation of Sulfur Nucleophiles
Authors: Kalyani P. , Manikyamba P.
Published: December 2009

In the nucleophilic substitution reaction of benzyl bromides with three sulfur nucleophiles a linear relationship between the nucleophile discrimination parameter (s) and the Hammett substituent constant (σ) is observed.
A Facile Solvent-free One-pot Three-component Mannich Reaction of Aldehydes, Amines and Terminal Alkynes Catalysed by CuCl2
Authors: Sharifi Ali , Mirzaei Mojtaba , Naimi-Jamal M. Reza
Published: December 2009

A solventless Mannich condensation of aldehydes, amines, and terminal alkynes catalysed by 10 mol% of CuCl2 was investigated. The components were simply mixed and heated together under vacuum, without any need of solidsupport or solvent. This results in the formation of Mannich products in high yields.
3-Aryl-1-benzoylthioureas with α-bromoketones in Water form 2-N-benzoyl-3-arylthiazol-2(3H)-imines, not 3-aryl-1-benzoylimidazoline-2-thiones
Authors: Singh C.B. , Murru Siva , Kavala Veerababurao , Patel Bhisma K.
Published: December 2009

The products obtained by the reaction of 1-benzoyl-3-phenylthioureas with α-bromoketones in water in the presence of triethylamine are not imidazoline-2-thiones as reported (J. Chem. Res. 2005, 689–690); rather they are thiazol-2-imine derivatives.
Synthesis of 2-exo-acryloyloxy-N-(1-adamantyl)Bornane-10-sulfonamide Diastereomers as Chiral Scaffolds
Authors: Duggan Andrew R. , Kaye Perry T.
Published: December 2009

Routes to the synthesis of 2-exo- and 2-endo-acryloyloxy-N-(1-adamantyl)bornane-10-sulfonamide have been developed, and preliminary applications of the former as a chiral Baylis–Hillman substrate have been explored.
Medium-size Cyclophanes, 751 Synthesis of anti-[2.3]metacyclophan-1-ene and Conversion to syn-1,2-epoxy[2.3]metacyclophane
Authors: Saisyo Tatsunori , Shiino Mikiko , Hironaka Tohru , Yamato Takehiko
Published: December 2009

McMurry cyclisation of 1,3-bis(5-formyl-2-methoxyphenyl)propane afforded anti-6,13-dimethoxy[2.3]metacyclophan-1-ene, which was converted to the corresponding syn-1,2-epoxyl[2.3]metacyclophane by treatment of m-chloroperbenzoic acid.
Synthesis of 3α-chlorinated Methyl Lithocholate Derivatives
Authors: Nahar Lutfun , Sarker Satyajit D. , Turner Alan B.
Published: December 2009

Methyl lithocholate (1), a bile acid derivative which contains a rigid steroid part as well as a flexible side chain, has been used as the starting material for the convenient synthesis of 3α-chlorinated methyl lithocholate, 3α-chloro-5β-cholan-24-oic acid methyl ester (2), and three other chlorinated derivatives, 3α-chloro-5β-cholan-24-ol (3), 3α-chloro-5β-cholan-24-yl tosylate (4) and ethyl (3α-chloro-5β-cholan)-24-yl oxalate (5). The identity of all these synthesised steroidal molecules (2–5) has been determined by spectroscopic analyses.
Synthesis and Inclusion Properties of 1,3-alternate-bis[(ethoxycarbonyl) Methoxy]thiacalix[4]arene-mono(crown-4) Ether
Authors: Pérez-Casas Carol , Rahman Shofiur , Begum Nazneen , Xi Zeng , Yamato Takehiko
Published: December 2009

A novel ditopic receptor possessing two complexation sites such as crown ether and (ethoxycarbonyl) methoxy groups bearing 1,3-alternate conformation based on thiacalix[4]arene was prepared. The binding behaviours with alkali metals have been examined by 1H NMR titration experiment. The exclusive formation of the heterogeneous dinuclear complexes of 1,3-alternate-3 with Li+ and K+ was observed.
A Formal Total Synthesis of (±) –cacalol
Authors: Banerjee Ajoy K. , Melean Carlos E. , Mora Henry D. , Cabrera Elvia V. , Laya Manuel S.
Published: December 2009

A formal total synthesis of Cacalol is described. Synthesis of methyl tetralin 8 has been achieved from the 5–methoxy-1-tetralone 2. The conversion of 8 into tetralol 11 has been accomplished in three steps (bromination, formylation and oxidation).
The Synthesis of Novel Pyrrolizidines under Classical, Ionic Liquid and Solvent-free Microwave-assisted Conditions
Authors: Jadidi Khosrow , Moghaddam Mojtaba Mirhosseini , Aghapoor Kioumars , Gharemanzadeh Ramin
Published: December 2009

Novel pyrrolizidines (1) were synthesised from 1, 3-dipolar cycloaddition of azomethine ylides and dipolarophiles (4). The one-pot three-component reactions were highly diastereoselective and regioselective and were carried out in classical, room temperature ionic liquid and solvent-free microwave-assisted conditions. All methods gave the products in high yields, and their structures were determined by 1H and 13C NMR spectral data and X-ray diffraction.
A Facile One-pot Solid-phase Synthesis of Oxazolidin-2-ones Using Polymer-supported 2-hydroxyalkyl Selenide Reagent
Authors: Hu Qiao-Sheng , Sheng Shou-Ri , Lin Shu-Ying , Wei Mei-Hong , Xin Qin , Liu Xiao-Ling
Published: December 2009

A simple, efficient and environmentally friendly procedure for one-pot solid-phase synthesis of 2-oxazolidinones in moderate to good yields by reaction of polystyrene-supported 2-hydroxyalkyl selenide with benzoyl isocyanate and subsequent oxidation/cyclisation-hydrolysis using a selenium traceless linker strategy is described.
Conversion of Piperidine-4-ones into [1,4]-diazepan-5-ones under Microwave Irradiation Using a Silica Gel Supported NaHSO4 Catalyst
Authors: Gopalakrishnan M. , Kumar P. Suresh , Thanusu J. , Prabhu C. , Kanagarajan V.
Published: December 2009

A rapid conversion of some 2,6-diarylpiperidin-4-ones into 2,7-diaryl-[1,4]-diazepan-5-ones in high yields has been developed involving treatment with hydroxylamine hydrochloride under microwave irradiation in the presence of a silica gel supported NaHSO4 catalyst.
A Novel Synthetic Method for β-keto Esters
Authors: Qian Hao , Ge Chunrong , Huang Xian
Published: December 2009

A novel synthetic method for the preparation of β-keto esters has been developed. α-Phenylseleno acetate was treated with LDA to produce a selenium-stabilised carbanion, which reacted with aldehydes, followed by selenoxide syn-elimination, to give β-keto esters.
Regioselective Synthesis of 4′-amino-1′H-spiro[cyclohexane-1,2′-(pyrimido [1,2-a]benzimidazole)]-3′-carbonitrile in Aqueous Medium
Authors: Dandia Anshu , Sarawgi Pritima , Bingham Ann L. , Drake John E. , Hursthouse Michael B. , Light Mark E. , Ratnani Raju
Published: December 2009

A simple, mild and environment-friendly procedure for synthesis of 4′-amino-1′H-spiro[cyclohexane-1,2′-(pyrimido[1,2-a]benzimidazole)]-3′-carbonitrile is developed using microwave irradiation in water. The product is obtained in short time, in excellent yield, and in a good state of purity. The reaction pathway and the influence of reaction conditions on regiochemistry are also investigated. The regioselectivity in this process is confirmed chemically and by single-crystal X-ray molecular structure determination.
Synthesis and in Vitro Activity towards Mycobacterium Tuberculosis of L-serinyl Ester and Amino Derivatives of Pyrazinoic Acid
Authors: Pinheiro Alessandra C. , Kaiser Carlos R. , Lourenço Maria C.S. , de Souza Marcus V.N. , Wardell Solange M.S.V. , Wardell James L.
Published: December 2009

Reactions between either L-serine methyl ester hydrochloride (1), or the cbz derivative, methyl (S)-(+)-2-(benzyloxycarbonylamino)-3-hydroxypropanoate (2), and pyrazinoyl chloride (3), have been studied. Methyl (S)-(+)-2-benzyloxycarbonylamino-3-[(pyrazinecarbonyl)oxy]propionate (4), methyl (S)-(+)-3-hydroxy-2-[(pyrazine-2-carbonyl) amino]propionoate (7), methyl 2-[(pyrazinecarbonyl)amino]acrylate (8) were obtained. Additional products, methyl (S)-(+)-2-benzyloxycarbonylamino-3-formyloxypropionoate (5) and methyl (R)-(+)-2-benzyloxycarbonylamino-3-chloropropionoate (6), were isolated from reaction of 2 with 3, in the presence of DMF remaining from the preparation of 3, from pyrazinecarboxylic acid. The coupling of pyrazinecarboxylic acid with 1, in the presence of DCC was prevented by the formation of the unreactive adduct between DCC and pyrazinoic acid. The compounds were tested against M. tuberculosis: compounds (8) and (6) exhibited a MIC (μg/ml) value of 50 and 100, respectively, compared to the MIC value of 100 for the first line TB drug, pyrazinamide. The confirmation of the structure of (8) was obtained via X-ray crystallography.
Stereoselective Hydrohalogenation of Alkynoic Acids and Their Esters in Ionic Liquids
Authors: Salazar José , Fernández Francys , Restrepo Jelem , López Simón E.
Published: December 2009

A novel procedure is described for the hydrohalogenation of alkynoic acids and their esters using N-alkylpyridinium ionic liquids. Hydrohalogenating agents were prepared by mixing N-alkylpyridinium halides with an equimolar amount of trifluoroacetic acid. The corresponding halogenated alkenes were obtained in good yields with high diastereoselectivity.
A One-pot Stereoselective Synthesis of 2-selenenyl-substituted 1,3-dienes by Hydrostannylation-Stille Tandem Reaction of Bu3SnH with Acetylenic Selenides and Alkenyl Iodides
Authors: Hao Wenyan , Yu Iamei , Cai Mingzhong
Published: December 2009

2-Selenenyl-substituted 1,3-dienes can be stereoselectively synthesised in one pot under mild conditions in good yields by the palladium-catalysed hydrostannylation of acetylenic selenides, followed by Stille coupling with alkenyl iodides.
Synthesis, Characterisation and Crystal Structure of a Co-crystal of Two Components: 1,2-bis(6-methylpyridin-2-yl)ethane-1,2-dione and 1-(pyridin-2-yl)-2-(6-methylpyridin-2-yl)ethane-1,2-dione
Authors: Percino M. Judith , Chapela Víctor M. , Urzúa Omar , Toribio Héctor , Rodríguez-Barbarín Cecilia
Published: December 2009

A condensation reaction of an equimolar ratio of 2-pyridinecarboxaldehyde and (6-methylpyridin-2-yl)methanol without a catalyst in a solvent-free reaction at 140°C was expected to yield 2-hydroxy-[1,2-bis(6-methylpyridin-2-yl)]ethan-1-one. FT-IR spectroscopy of the yellow-brown solid reaction product indicated the presence of a –CO–COH– group. The solid compound was treated with cyclohexane and green crystals were produced. The crystals were characterised by FT-IR, 1H NMR, EI mass spectrometry and single-crystal X-ray diffraction. The molecular and crystal structure determined by single-crystal X-ray diffraction resolved one crystal showing two molecular components [C13H10N2O2 and C14H12N2O2] at a ratio of 60.4:39.6 [C13.40H10.79N2O2]. Both compounds co-crystallise in the triclinic space group P-1, with a = 7.859(5), b = 8.021(14), c = 9.060(5) Å, α = 101.36(2)°, β = 90.06(3)°, γ = 90.92(3)°, V = 559.8(5) Å3, Z = 2. The compounds were 1,2-bis(6-methylpyridin-2-yl)ethane-1,2-dione and 1-(pyridin-2-yl)-2-(6-methylpyridin-2-yl)ethane-1,2-dione. These results are important because they confirm that condensation in a solvent- and catalyst-free reaction yielded precursors that were converted into α-diketone compounds by the action of solvent and oxygen.
A Facile Stereoselective Synthesis of (Z)-2-arylsulfonyl-substituted 1,3-enynes from (E)-α-stannylvinyl Sulfones and Alkynyl Bromides
Authors: Hu Ronghua , Chen Guiqin , Cai Mingzhong
Published: December 2009

Palladium-catalysed hydrostannylation of acetylenic sulfones 1 in benzene at room temperature gives stereoselectively (E)-α-stannylvinyl sulfones 2 in good to high yields. (E)-α-Stannylvinyl sulfones 2 are difunctional group reagents which undergo cross-coupling reactions with alkynyl bromides 3 in the presence of Pd(PPh3)4 and CuI co-catalyst to afford stereoselectively (Z)-2-arylsulfonyl-substituted 1,3-enynes 4 in good yields.
Reaction of Sarcosine with Chromone-3-carbaldehyde and 6,6′-(polymethylenedioxy)di(chromone-3-carbaldehyde)
Authors: Ghosh Tarun , Bandyopadhyay Chandrakanta
Published: December 2009

On treatment with N-methylglycine in DMF, the chromone-3-carbaldehydes 1a–c produce 3-[3-(2-hydroxybenzoyl)-1-methyl-2,5-dihydropyrrol-2-yl]-4H-chromen-4-ones 10a–c and the deformylated products 9a–c, whereas the bis-chromone derivatives 12a–c give the bis[3-(2-hydroxybenzoyl)-1-methylpyrrole] structures 13a–c.
An Efficient Protocol for the Acylation of T-butanol in the Presence of Samarium Diiodide
Authors: Jia Xueshun , Li Li Zhu, Qing , Li Jian , Li Dafeng , Li Shaoyu
Published: December 2009

Samarium diiodide (SmI2) promotes the rapid acylation of t-butanol with a variety of acid chlorides under neutral conditions to afford cleanly the corresponding t-butyl esters in excellent yields.
Facile Synthesis of 4-phenyl-6-[(Z)phenylimino]-3,6-dihydro-1,3,5-thiadiazine-2,2-dicarbonitriles
Authors: Aly Ashraf A. , El-Shaieb Kamal M.
Published: December 2009

N-Imidoylthioureas 2a–e reacted with 1,1,2,2-tetracyanoethylene (1) to form the thiadiazines 3a–e. In the case of 1e, tricyanovinylation of a phenyl substituent accompanied formation of the thiadiazine ring.
EPR Studies on Carboxylic Esters. Part 17.1 EPR Spectra and Spin Densities in the Radical Anions of Thio and Dithiocoumarins
Authors: Voss Jürgen , Edler Ronald
Published: December 2009

The radical anions of 4-methyl-1-thiocoumarins and 4-methyl-1-thio-2-thionocoumarins are generated by internal electroreduction and studied by EPR spectrosopy. The spin density distribution is evaluated from the proton hfs coupling constants and by MO calculations. The radical anions of the corresponding coumarins and 2-thionocoumarins are not persistent enough for EPR spectroscopic measurements.
Synthesis and Morpholinolysis of N,N-diethyl Carbamate Derivatives of 4- HOAt, 7-HOAt and HOBt
Authors: Khattab Sherine N. , Hassan Seham Y. , Hamed Ezzat A. , El-Faham Ayman
Published: December 2009

N,N-Diethyl carbamates of 1-hydroxy-7-azabenzotriazole (7-HOAt), 1-hydroxy-4-azabenzotriazole (4-HOAt), 1-hydroxybenzotriazole (HOBt), and 1-hydroxypyrrolidine-2,5-dione have been synthesised. The reactivities of these active esters have been determined by studying the kinetics and mechanism of their morpholinolysis in acetonitrile at different temperatures.
Syntheses, Crystal Structure and Antibacterial Activities of Mononuclear and Tetranuclear Di-n-butyltin(IV) Complexes Constructed from 2-(4-formyl-2-methoxyphenoxy)Acetic Acid
Authors: Zhu Dongsheng , Mei Zemin , Xu Lin
Published: December 2009

Two new organotin(IV) carboxylates of composition n-Bu2Sn(O2CCH2OC6H3OCH3 CHO)2 (1) and {[n-Bu2Sn(O2CCH2 OC6H3OCH3CHO)2]2O}2 (2) were obtained by the reaction of n-Bu2SnO and 2-(4-formyl-2-methoxyphenoxy)acetic acid (LH). The compounds 1 and 2 have been characterised by elemental analysis and IR, 1H NMR and X-ray crystallographic diffraction studies. The tin atom in 1 is found to adopt the skew-trapezoidal bipyramidal geometry in the polymeric chains. The compound 2 adopts a dimeric ladder structure and contains a tetranuclear tin framework with six distannoxane rings. The antibacterial activities decrease in the order 2 > 1 > (n-Bu)2SnO > LH.
Synthesis and Structure Determination of 8- and 9-iodocamphorquinone Bis(ethylene ketal)
Authors: Magqi Nceba , Lobb Kevin A. , Kaye Perry T. , Caira Mino R.
Published: December 2009

The structures of 8- and 9-iodocamphorquinone bis(ethylene ketal) have been confirmed by spectroscopic and single crystal X-ray analysis. The unexpected formation of the latter isomer is attributed to intramolecular rearrangement of the camphor skeleton, the mechanistic details of which have been explored using coset analysis.
Synthesis of Amino Substituted Pyrazoles
Authors: Singh Okram Mukherjee , Ahmed Mohammad Farooque , Singh Sarangthem Joychandra , Lee Sang-Gyeong
Published: December 2009

An efficient and convenient synthesis of substituted pyrazoles with aryl and heteroarylamino substituents attached to the C-3 and C-5 positions by the action of hydrazine hydrate on either ketene N,S-acetals or mixed N,N-aminals hydrate is reported.
Synthesis of Novel Benzimidazo[1,2-c][1,2,4]triazolo[4,3-a]quinazoline derivatives
Authors: Davoodnia Abolghasem , Heravi M. Momen , Golshani Ehsan , Bakavoli Mehdi , Dehabadi Leila
Published: December 2009

Cyclocondensation of 2-(1 H-benzimidazol-2-yl)anilines 1a,b with carbon disulfide in the presence of potassium t-butoxide in boiling DMF afforded the corresponding benzimidazo[1,2- c]quinazoline-6(5 H)-thiones 2a,b. Treatment of these compounds with hydrazine hydrate at reflux in ethanol gave the hydrazine derivatives 3a,b which were subsequently cyclised to the title compounds 4a–f on heating with orthoesters in ethanol.
The Synthesis and Biological Activities of 6-aryl-3-(D-glucoheptonichexitol-1-yl)-7H-1,2,4-triazolo[3,4-b][1,3,4]Thiadiazines
Authors: Ye Xiaoxia , Chen Zhenfei , Zhang Anjiang , Zhang Lixue
Published: December 2009

A series of novel 6-aryl-3-(D-glucoheptonic-hexitol-1-yl)-7H-1,2,4-triazolo[3,4-b][1,3,4] thiadiazines (2a–2j) have been synthesised in high yield by means of the reaction of 4-amino-5-mercapto-3-(D-glucoheptonic-hexitol-1-yl)-1,2,4-triazole (1) with substituted ω-brom- oacetophenones. The structures of the compounds were determined by elemental analysis, IR, 1H NMR, 13C NMR and MS. Most possessed high plant growth-regulating activities.
Isoflavones from Psorothamnus arborescens via high-throughput Natural Product Chemistry Methods
Authors: Hu Jin-Feng , Garo Eliane , Hough Grayson W. , Goering Matt G. , Yoo Hye-Dong , O'Neil-Johnson Mark , Eldridge Gary R.
Published: December 2009

One new isoflavone, arborestin (2), together with the known fremontin (1), were obtained from Psorothamnus arborescens via high-throughput natural product chemistry methods. The isoflavones were isolated and the structure elucidation was performed using a capillary scale NMR probe and HR-/LR-ESIMS data.
Sulfur-nitrogen Heterocycles from the Condensation of Pyrazolones and 2-iminothiazolidin-4-ones with Phenyl Isothiocyanate
Authors: Bagdatli Emine , Akkus Senem , Yolacan Cigdem , Öcal Nüket
Published: December 2009

The condensation of 2-pyrazolin-5-ones with phenyl isothiocyanate, followed by reaction of the resulting thiolate ions with chloroacetyl chloride, phenacyl bromide, oxalyl chloride, 1,4-dibromo-2,3-butanedione and ethyl chloroformate, resulted in cyclisation to S,N-heterocycles in all cases. 2-Iminothiazolidin-4-ones, with phenyl isothiocyanate and then chloroacetyl chloride or phenacyl bromide, similarly formed 2,4′-bi(thiazolidine)-derived products.
Efficient Synthesis of Naphthalene-Fused Dilactam Crown Ethers
Authors: Eshghi Hossein , Mirzaei Mehdi , Esmaily-Shahry Hadi
Published: December 2009

The novel macrocyclic dilactams that structurally fuse to naphthalene chromophore were synthesised. These compounds were obtained in the macrocyclisation step by fast addition methods and the results were compared with solvent-free conditions.
Synthesis of N4-β-D-glycoside cytosines and sugar N4-acetylcytosin-1-ylmethylhydrazones as antiviral agents
Authors: Ali Omar M. , Amer Hamada H. , Abdel-Rahman Adel A.-H.
Published: December 2009

Reaction of monosaccharide aldoses with cytosine (1) gave stereoselectively β- N-glycosides 2a–d, which were treated with acetic anhydride in pyridine to afford the corresponding acetylated derivatives 3a–d. N4-Acetylcytosine (4) was synthesised and treated with ethyl chloroacetate to give 1-(ethoxycarbonylmethyl)- N4-acetylcytosine (5). Hydrolysis of the latter ester with hydrazine hydrate afforded the hydrazide derivative 6. Condensation of the hydrazide with monosaccharide aldoses gave the corresponding sugar hydrazones 7a–f. Acetylation of the hydrazones afforded the per- O-acetyl derivatives 8a–f. The prepared compounds were tested for antiviral activity against hepatitis B virus (HBV) which showed moderate activities.
Active Metallic Indium-Mediated Ring-Opening of Epoxides with Diphenyl Diselenides: A Novel One-Pot Synthesis of β-hydroxy Selenides in Aqueous Media
Authors: Chen Xian , Wu Huayue , Su Weike , Xu Rong , Liu Miaochang , Ding Jinchang
Published: December 2009

An efficient and simple one-pot procedure for the synthesis of β-hydroxy selenides in aqueous media through highly regioselective ring-opening of epoxides with diphenyl diselenide in the presence of active metallic indium is described.
Synthesis of C, N-diaryl Nitrones from the Reduction of Nitroarene with Aromatic Aldehydes Promoted by Metallic Samarium
Authors: Jia Xueshun , Li Dafeng , Huang Qing , Zhu Li , Li Jian
Published: December 2009

A mild and facile reduction of nitroarene with aromatic aldehydes promoted by metallic samarium to C, N-diaryl nitrones in moderate yields has been developed.
Preparation, X-ray Structure and Propylaminolysis of 7,7-dichloro-5,7-dihydro-thieno[3,4-b]pyridin-5-one
Authors: van Es Theodorus , Staskun Benjamin , Fernandes Manuel A.
Published: December 2009

Refluxing 2-methylpyridine-3-carboxylic acid with thionyl chloride for 6–7 h gave (∼50%) title compound dichlorothienolactone 2 as was confirmed by a X-ray structure analysis. The propylaminolysis of 2 provides a new and convenient access to highly functionalised pyrrolo[3,4- b]pyridine derivatives.
Synthesis and Characterisation of a New Pyridinium Salt/Crown Ether Complex and its Self-Assembly
Authors: Li Jiang-Sheng , Chen Li-Gong , Zhang Ying-Ying , Xu Yan-Jie , Deng Yi , Zeng Tao , Huang Peng-Mian
Published: December 2009

The monoprotonated bipyridinium cation can complex with dibenzo-24-crown-8 by means of ion-dipole and charge-transfer interactions. They both thread to form a [2]pseudorotaxane-like complex for further intercomplex association to produce pseudopolyrotaxane arrays through N+–H···N hydrogen bonding in the solid state.
Synthesis of Propargylic Alcohols by base promoted Alkynylation of Ketones with Ethynylbenzene using Ionic Liquid [(bmim) PF6]
Authors: Jagtap Sachin R. , Bhanage Bhalchandra M.
Published: December 2009

A mild and efficient addition of ethynylbenzene with ketones using KOH in ionic liquid 1-butyl-3-methylimidazolium hexaflurophosphate [(bmim) PF6] gives propargylic alcohols in high yields.
Characterisation of a Mixed N-heterocycle, 2-(N-methylimidazole-2′-yl-thiomethyl)benzimidazole, and its complexes with nickel(II) and copper(II)
Authors: Satyanarayana Srikantaiah , Nagasundara Kuderu R
Published: December 2009

2-(N-methylimidazole-2′-yl-thiomethyl)benzimidazole (L) has been synthesised and the complexes [ML2 (ClO4)2]·2H2O (M = Ni or Cu) and [MLX2] nH2O (M = Cu, X = Cl or Br, n = 0; M = Ni, X = Cl, n = 3; M = Ni, X = Br, n = 0) prepared and characterised. Proposed geometries for the complexes are: octahedral geometry for perchlorate complexes; tetrahedral geometry for chloro-and bromo-complexes; dimeric square pyramidal for the chloro-complex of copper(II).
Syntheses and Crystal Structures of Cobalt(II) and Nickel(II) Complexes with Thiocyanate and Pyridyl Carboxylic Acid
Authors: Yang Guang , Zhang Qian , Zhang Xiang-Pei , Zhu Yu , Ng Seik Weng
Published: December 2009

The syntheses and crystal structures of [Co(m-NCS)2(nicH)2]·(nicH), [Ni(NCS)2(H2O)2(isonicH)2]·(isonicH)·2H2O are reported, where nicH is nicotinic acid; isonicH is isonicotinic acid. In the crystals of the two complexes, (iso)nicotinic acids are not deprotonated and thus the carboxy groups act as both donors and acceptors of H-bonds to form networks.
Synthesis of Symmetrically 1,4-disubstituted piperazine-2,5-diones: A New Class of Antileishmanial Agents
Authors: Hazra Abhijit , Paira Priyankar , Palit Partha , Banerjee Sukdeb , Mondal Nirup B. , Sahu Niranjan P.
Published: December 2009

A series of 1,4-diphenyl-2,5-dioxopiperazine derivatives were synthesised in one pot sequence. The compounds demonstrated appreciable cytotoxic activity against Leishmania donovani on both forms of the parasite, and the results suggested that some derivatives (4, 11 and 12) could be exploited as antileishmanial agents.
Synthesis and reactivity of N-[3-amino-4-(benzoxazol-2-yl)pyrazol-5-yl]phenylamine
Authors: Abdelhamid Abdou O. , Baghos Victorin B. , Halim Mervat M.A.
Published: December 2009

Pyrazolo[5,1- a]pyrimidines and pyrazolo[5,1-c][1,2,4]triazines containing benzooxazole moiety are synthesised from N-[3-amino-4-(benzoxazol-2-yl)pyrazol-5-yl]phenylamine or its diazonium chloride with the appropriate active methylene compounds. The newly synthesised compounds were elucidated by elemental analysis, spectral data and alternative synthetic route whenever possible.
Zinc Mediated Selective Acylation of Ferrocene under Solvent-Free Conditions
Authors: Purecha Vishal H. , Nandurkar Nitin S. , Bhanage Bhalchandra M. , Nagarkar Jayashree M.
Published: December 2009

A simple, convenient and environmentally-friendly method for selective acylation of ferrocene to monoacylferrocene in the presence of Zn metal under solvent-free conditions is described. The protocol requires mild operating conditions, affording higher yields of desired products both with acyl chloride/carboxylic acid within a short reaction time (15–30 min).
Liquid-phase Synthesis of Ethyl (Z)-2-(thiocyanatomethyl)alk-2-enoates from PEG-bound α-phenylselenopropionate
Authors: Hu Qiao-Sheng , Yu La-Mei , Sun Wu-Kang , Sheng Shou-Ri , Liu Xiao-Ling
Published: December 2009

Aldolisation of novel PEG-bound α-phenylselenopropionate with aldehydes, followed by oxidation-elimination with 30% hydrogen peroxide and then treatment with potassium thiocyanate formed PEG-bound 2-(thiocyanatomethyl)alk-2-enoates. Subsequent cleavage from the PEG efficiently afforded ethyl ( Z)-2-(thiocyanatomethyl)alk-2-enoates in good yields and high purities.
Unusual Reactivity of 2,3-diphenylcyclopropenone towards N-imidoylthioureas; Facile Synthesis of 3-aryl-2,5,6-triphenylpyrimidin-4(3H)-one (PART III)
Authors: Aly Ashraf A. , NourEl-Din Ahmed M. , Gomaa Moshen A.-M. , Brown Alan B. , Fahmi Magda S.
Published: December 2009

2,3-Diphenylcyclopropenone (1) reacts with N-imidoylthioureas 2a–e to form the pyrimidin-4(3 H)-ones 5a–e. The reaction mechanism can be described as due to stepwise addition accompanied by elimination of phenyl isothiocyanate.
Synthesis, Characterisation and Hydrolytic Reactions of the First Pentaisopropoxostannate Derivatives of Magnesium, Zinc and Cadmium
Authors: Shahanl Jayshree , Singh Anirudh
Published: December 2009

Pentaisopropoxostannate derivatives of the types [{M[Sn(OPri)5](μ–Cl)}2] and [M{Sn(OPri)5}2] have been prepared by the reactions of MCl2 (M = Mg, Zn, and Cd) with NaSn(OPri)5 in 1:1 and 1:2 molar ratios, respectively, in benzene. All these derivatives have been characterised by elemental and isopropoxo group analyses, spectroscopic (IR, 1H and 13C NMR) studies, and molecular weight determinations. Two typical hydrolytic reactions of [Zn{Sn(OPri)5}2] have also been investigated.
The Effective Preparation of Secondary Amines Bearing a Vinylsilane Functionality via the reaction of Primary Amines with α-chlorine-substituted Allylsilanes Catalysed by CuCl
Authors: Kozuka Makoto , Mitani Michiharu
Published: December 2009

The reaction of α-chlorine-substituted allylsilanes with primary amines was promoted by CuCl to result in the selective formation of secondary amines bearing the vinylsilane functionality by a probable SN2′-allylation keeping the silyl group intact.
Regioselective Synthesis of Novel 4,4′-and 5,5′-bi-(1,2,4-triazole) Derivatives
Authors: Farag Ahmad M. , Dawood Kamal M. , Khedr Nabila A.
Published: December 2009

A regioselective synthesis is reported of a series of polysubstituted 1,2,4-triazoles and 4,4′- and 5,5′-bi-(1,2,4-triazoles) via 1,3-dipolar cycloaddition reactions of nitrilimines with some aza- and diaza-butadiene derivatives.
Cleavage of C=N derivatives and Oxidation of Thiols in Water under Neutral Conditions with 1,4-dichloro-1,4-diazoniabicyclo[2,2,2]octane bischloride
Authors: Tajbakhsh Mahmood , Habibzadeh Setareh
Published: December 2009

1,4-Diazabicyclo[2,2,2]octane (DABCO) is easily chlorinated and gives a complex which efficiently converts aliphatic and aromatic oximes, phenylhydrazones and semicarbazones to their corresponding carbonyl compounds in water at 50°C in high yield. This reagent can also be used for conversion of thiols to their compounding disulfide under the same reaction conditions. DABCO is quantitatively recovered which can be rechlorinated and reused several times.
One-pot Regioselective Synthesis of 2,9-Disubstituted Imidazo[1,2-a] Benzimidazoles from 2-Aminobenzimidazole and α-Tosyloxy Ketones
Authors: Kumar Ashok , Kumar Sunil , Kumar Devinder , Gupta Rakesh K.
Published: December 2009

One-pot regioselective synthesis in high yields of 2,9-disubstituted imidazo[1,2-a]benzimidazoles from 2-aminobenzimidazole and α-tosyloxy ketones is described.
Polyphosphoric Acid Trimethylsilylester: A Useful Reagent for Organic Synthesis
Authors: López Simón E. , Restrepo Jelem , Salazar José
Published: December 2009

This review describes the composition, preparation and applications in organic synthesis of polyphosphoric acid trimethylsilylester (PPSE). It covers the literature since it first appeared in the eighties until the first trimester of 2007. A discussion of the synthetic utility of PPSE, compared to other related reagents such as polyphosphoric acid (PPA) and polyphosphoric acid ethyl ester (PPE) as well as various Lewis acids, is also included.
The First Immobilisation of Glycoluril-Based Molecular Clips on Silica Gel and Alumina
Authors: Rahimizadeh Mohammad , Seresht Esmaeel Rezaei , Bakavoli Mehdi , Golari Neda
Published: December 2009

The first example of immobilisation of some glycoluril-based molecular clips, which are good receptors for dihydroxybenzenes, on silica gel and alumina is described. 4,4′-Bis(methoxyphenyl)glycoluril was used as the base scaffold for the synthesis of molecular clips. After demethylation of the methoxy groups, the clip compounds were attached to silica gel and alumina using the linker (3-chloropropyl)trimethoxysilane. The resulting clip-functionalised silica gel and alumina could be applied as a stationary phase in an affinity chromatography technique for the separation and purification of dihydroxybenzenes and the more important biologically active catecholamines.
Synthesis of 3-[(acetylamino)(aryl)methyl]-4-Hydroxycoumarins
Authors: Anary-Abbasinejad Mohammad , Anaraki-Ardakani Hossein , Saidipoor Azimeh , Shojaee Mahmood
Published: December 2009

One-pot, three-component reaction between aryl aldehydes, 4-hydroxycoumarin, and acetonitrile in the presence of chlorosulfonic acid affords 3-[(acetylamino)(aryl)methyl]-4-hydroxycoumarins in excellent yields.
Synthesis and Inclusion Properties of thiacalix[4]arene tetraamides in cone- and 1,3-alternate conformation
Authors: Rahman Shofiur , Begum Nazneen , Pérez-Casas Carol , Yoshizawa Akina , Yamato Takehiko
Published: December 2009

Novel thiacalix[4]arene tetraamides in cone- and 1,3- alternate conformation were prepared, in which the cone-tetraamide shows stronger intramolecular hydrogen bonding than 1,3- alternate-tetraamide. The two-phase solvent extraction data indicated that tetraamides show no extractability for alkali metal cations, but small extractability for dichromate anion (Cr2O72-).
Synthesis and Photolysis of Hexahydropyrrolo[3,4-c]pyrazole derivatives
Authors: Hamadi Naoufel Ben , Louhichi Nesrine , Msaddek Moncef
Published: December 2009

The 1,3-dipolar cycloaddition of 2-diazopropane 1 with N-arylcitraconimides and N-arylmaleimides 2, at −78°C, has led to monoadducts 3. The same addition of 2-diazopropane with maleimide 4, has led to a new and unexpected Δ3-1,3,4-oxadiazoline 5. Irradiation of the pyrazolines 3 led to clean extruction of nitrogen to give the cyclopropanes 6.
A Novel Macrocyclic Dimeric Dicarboxylato Distannoxane Assembled from a Flexible Dicarboxylic Acid
Authors: Zhu Dongsheng , Kang Wanli , Dong Dewen , Liu Qun , Xu Lin
Published: December 2009

The novel macrocyclic complex [(Bu2Sn)2OL]2•CH3CN (2) has been prepared from the flexible dicarboxylic acid, LH2, (1). Single crystal X-ray diffraction shows that complex 2 has a centrosymmetric structure, with a central rhomboid cyclic Bu4Sn2O2 unit, linked at the oxygen atoms to two exocyclic tin atoms. The dicarboxylate ligands bridge exocylic and endocyclic tin atoms, completing two rings each of 22 atoms, and two of the four carbonyl oxygen atoms coordinate to the exocyclic tin atoms, to raise their coordination state to five and complete two more six-membered, rings.
Synthesis of 2-alkylisoflavones under phase-transfer Catalysis Conditions
Authors: DeMing Dai , LingLing Weng
Published: December 2009

2-alkyl isoflavones were synthesised with the aliphatic acid chloride and 2-hydroxydeoxybenzoins under phase-transfer catalysis in acetone–K2CO3 medium involves the modified Baker–VenKataraman transformation
Water–acetone Media Enforced Chemoselective Synthesis of 2-substituted Pyrrole Stable Phosphorus Ylides from Reaction between Pyrrole and Acetylenic Esters in the Presence of Triphenylphosphine
Authors: Maghsoodlou Malek Taher , Hazeri Nourollah , Habibi-Khorassani Sayyed Mostafa , Moeeni Zohreh , Marandi Ghasem , Lashkari Mojtaba , Ghasemzadeh Marjan , Bijanzadeh Hamid Reza
Published: December 2009

Pyrrole undergoes a smooth reaction with dialkyl acetylenedicarboxylates in the presence of triphenylphosphine in a mixture of water–acetone (50:50) as a solvent pathway to produce phosphorus ylides of 2-substituted pyrrole in good yield.
Reactions with Hydrazonoyl Halides 601: Synthesis of Thieno[2′,3′:4,5] Pyrimidino[1,2-b][1,2,4,5]tetrazines, [1]benzothieno[2′,3′:4,5]pyrimidino [1,2-b][1,2,4,5]tetrazines, Pyrazolo[3′,4′:4,5]pyrimidino[1,2-b] [1,2,4,5]tetrazines and Pyrazolo[3,4-d]pyridazines
Authors: Abdelhamid Abdou O. , Ismail Zeineb H. , Abdel-Aziem Anhar
Published: December 2009

Thieno[2′,3′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, [1]benzothieno-[2′,3′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, pyrazolo [3′,4′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, triazolo[4,3- a]pyrimidin-5(1 H)-one, 1-{[2-(1-benzofuran-2-yl)-5-phenyl-4,5-dihydro-1 H-pyrazol-1-yl]-4-substituted-1,3-thiazol-5-yl}-2-phenyldiazene, 3-acyl-4-(1-benzofuran-2-ylcarbonyl) pyrazole and pyrazolo[3,4- d]pyridazine derivatives could be obtained via reactions of hydrazonoyl halides with the appropriate pyrimidine-2-thione, 3-amino-5,6-dimethyl-2-sulfanylthieno[2,3- d]pyrimidin-4(3 H)-one, 5-amino-6-mercapto-1-phenyl-1,5-dihydropyrazolo[3,4- d]pyrimidin-4-one and 1-(benzofuran-2-yl)-3-(dimethylamino)prop-2-en-1-one. Structures of the products have been determined by elemental analyses, spectral data studies and alternative synthesis whenever possible.
Synthesis of Novel Macroheterocycles containing Phosphorus and Nitrogen
Authors: Babu Boppudi Hari , Srinivasulu Kambam , Prasad Gandavaram Syam , Raju Chamarthi Naga
Published: December 2009

Syntheses of novel 3-[1-(4-chlorophenyl)ethyl]-1(indol-1-yl-methylphenyl-phosphinoyl/thiophosphinoyl/selenophosphinoyl methyl)-1 H-indole derivatives were accomplished in two steps. The synthetic route involves the cyclisation of equimolar quantities of 3-[4-chlorophenyl(1 H-3-indolyl)methyl]-1 H-indole (1) with bis(iodomethyl)phenylphosphine, bis(2-bromoethyl)phenylphosphine and tris-2-chloroethylphosphite (2a–c) in the presence of NaH under nitrogen atmosphere in dry THF to get P(III) intermediates (3a–c). These were further converted into the corresponding oxides, sulfides and selenides (4a–i) by reacting them with hydrogen peroxide, sulfur and selenium respectively.
Three-component reaction of Cyclohexyl Isocyanide, Barbituric Acid and Aryl Aldehydes; Synthesis of N-cyclohexyl-N-[aryl-(2,4,6-trioxohexahydropyrimidin-5-yl)methyl]formamides
Authors: Anary-Abbasinejad Mohammad , Kamali-Gharamaleki Maryam , Hassanabadi Alireza
Published: December 2009

Three-component reaction of cyclohexyl isocyanide, barbituric acid and different aldehydes, in a mixture of water: acetonitrile (1:1) as solvent, produces the corresponding N-cyclohexyl- N-[aryl-(2,4,6-trioxohexahydropyrimidin-5-yl)methyl]formamides in excellent yields.
Three-component reaction between Triphenylphosphine, Acetylenic Esters and 4-hydroxycoumarin, 4-(phenylamino)coumarin, 4-hydroxyquinolin-2(1H)-one or 4-hydroxy-1-methylquinolin-2(1H)-one
Authors: Anary-Abbasinejad Mohammad , Anaraki-Ardakani Hossein , Ezadi Ali , Hassanabadi Alireza
Published: December 2009

Three-component reaction between dialkyl acetylenedicarboxylates and triphenylphosphine in the presence of 4-hydroxycoumarin, 4-(phenylamino)coumarin, 4-hydroxyquinolin-2(1 H)-one or 4-hydroxy-1-methylquinolin-2(1 H)-one is described.