bluuebunny/crossref_metadata_2025_split huggingface dataset:
Reactivity of 3‐amino‐3H‐quinazolin‐4‐one derivatives towards some electrophilic and nucleophilic reagents and using of the products in the building of some interesting heterocycles as anticancer agent
Authors: Abdel‐Rahman Taha.M. 
Published: March 2009

Abstractmagnified imageThe chemical reactivity of N‐[1‐(3‐amino‐6,8‐dibromo‐4‐oxo‐3,4‐dihydro‐quinazolin‐2‐yl)‐2‐(2‐chlorophenyl)‐vinyl]benzamide (3) towards electrophilic and nucleophilic reagents have been reported. Structures of the products 3‐24 have been confirmed by elemental analysis and spectral data (IR, 1H‐NMR, 13C and MS). The bioassay indicates that some of the prepared compounds have a good selective anticancer activity.
Facile preparation and the crystal structure of N, N′‐dialkyl‐2,6‐pyridinedimethanaminium halide
Authors: Kobayashi Tohru , Yaita Tsuyoshi , Sugo Yumi , Suda Hiroki , Suzuki Shinji , Fujii Yuki , Nakano Yoshiharu 
Published: March 2009

Abstractmagnified imageA facile preparation and the crystal structures of N, N′‐dialkyl‐2,6‐ pyridinedimethanaminium halides were described. Direct substitution reactions were convenient to prepare specifically secondary diamines using 2,6‐bis(chloromethyl)‐ pyridine and 10 equivalents molar of primary alkylamines. Hydrogen halide salts were obtained in good yields and the crystal structures of three N, N′‐dialkyl‐2,6‐pyridinedimethanaminium salts were determined by the X‐ray diffraction method. A cancroid structure around the pyridine ring was observed commonly in the three salts. Acidity constants of the three salts were determined. Since the pKa values of the salts were slightly smaller than those of several common triamines previously reported, the acidities did not correlate with the cancroid structure directly. This is probably due to electrostatic interaction of the two protonated amino groups, furthermore the central pyridine nitrogen was not protonated in all the ligands.
Chloroformamidinium salts: Efficient reagents for preparation of 2‐aminobenzoimidazole, 2‐aminobenzoxazole, and 2‐aminobenzothiazole derivatives
Authors: El‐Faham Ayman , Chebbo Mohamed , Abdul‐Ghani Mohamed , Younes Ghassan 
Published: March 2009

Abstractmagnified imageA Reaction involving chloroformamidinium salts (TCFH 1a, BTCFH 1b, DmCFH 1c, DmPCFH 1d, BPCFH 1e) and 2‐aminophenol 9a, benzene‐1,2‐diamine 9b, and 2‐aminothiophenol 9c afforded 2‐aminobenzoxazole 13, 2‐aminobenzoimidazole 14, and 2‐aminobenzothiazole 15 derivatives, respectively as major products, due to the in situ heterocyclization with dimethylamine acting as the better leaving group. Attempts for preparation of 13‐15 from the reaction of N,N‐dimethyl carbomyl chloride 16 with 2‐aminophenol 9a, benzene‐1,2‐diamine 9b, and 2‐aminothiophenol 9c were unsuccessful, and gave the unexpected products benzoxazol‐2‐ol 18a, benzoimidazol‐2‐one 18b, and S‐(2‐amino‐phenyl) N,N‐dimethylthiocarbamate 19 respectively. On the other hand reaction of chloroformamidinium salts 1a‐e with 3‐benzyl‐2‐hydrazinoquinoxaline 3 and 1‐hydrazinophthalazine hydrochloride 4 in the presence of triethylamine as a base, afforded the [1,2,4]triazolo derivatives 6 and 7 respectively in good yield and purity. These triazole derivatives were formed due to the strong tendency towards heterocyclization and substitution of dimethylamine group as a better leaving group.
Cyclocondensation reactions of heterocyclic carbonyl compounds XI . Synthesis and study of cyclocondensation reactions of some 3‐substituted‐5‐(2‐aminobenzyl)‐1H‐[1,2,4]triazine‐6‐ones
Authors: Guckýa Tomáš , Slouka Jan , Fryšová Iveta , Maloň Michal 
Published: March 2009

Abstractmagnified imageA series of 2‐substituted‐4‐(2‐nitrobenzylidene)‐4,5‐dihydrooxazol‐5‐ones (2a‐2i) was prepared by the Erlenmeyer's synthesis of 2‐nitrobenzaldehyde with acylglycines (1a‐1i) and the series of corresponding aminoderivatives (3b‐3d and 3g‐3i) was synthetised by catalytic hydrogenation of (2b‐2d and 3g‐3i). Hydrazinolysis of azlactones (2) and (3) gave hydrazides (4) and (5). The hydrazides (5) were also obtained by catalytic hydrogenation of corresponding nitroderivatives (4). The cyclization reaction of hydrazides (4) or (5) proceeded to 3,5‐disubstituted‐1,6‐dihydro‐[1,2,4]triazine‐6‐ones (6) or (7). Aminoderivatives (7) were also obtained by reduction of nitro group of compounds (6). The aminoderivatives (7) were then cyclized to 3‐substituted‐1,5‐dihydro‐[1,2,4]triazino[6,5‐b]quinolines (9), resp. its tautomers (10).
Furan ring opening ‐ indole ring closure: Synthesis of furo[2′,3′:3,4]‐cyclohepta[1,2‐b]indolium chlorides
Authors: Butin Alexander V. , Smirnov Sergey K. , Stroganova Tatyana A. 
Published: March 2009

Abstractmagnified imageA new synthetic approach to furo[2′,3′:3,4]cyclohepta[1,2‐b]indolium chlorides is elaborated starting from 2‐acetylaminoaryldifurylmethanes or 2‐aminoaryldifurylmethanes under treatment with methanolic HCl solution. The reaction proceeds in three steps: recyclization, intramolecular cyclization, and disproportionation. In this case the furan ring takes part in building up both pyrrole and seven‐membered rings. The same salts can be obtained directly from 2‐acetylaminobenzaldehydes and 2‐methylfuran under similar conditions without isolation of corresponding 2‐acetylaminoaryldifurylmethanes.
Ring expansion of isopropenyldihydrofuran derivatives
Authors: Yamaguchi Seiji , Tsuchida Nao , Umeda Kayoko , Yokoyama Hajime , Miyazawa Masahiro , Hirai Yoshiro 
Published: March 2009

Abstractmagnified imageLactonization of 2‐(hydroxymethyl)‐5‐isopropenyl‐4,5‐dihydrofuran‐3‐carboxylic acids 1a,b,c with dicyclohexylcarbodiimide gave the corresponding furano‐lactones, 5‐isopropenyl‐5,6‐dihydro‐1(3H)‐furo[3,4‐b]furanone 2a,b,c, which were readily converted to the corresponding oxepino‐lactones, 6‐methyl‐5,8‐dihydro‐1(3H)‐furo[3,4‐b]oxepinone 3a,b,c by respective thermal ring expansions.
Synthesis, properties and X‐ray structure of 5‐azido‐2‐methoxy‐1,3‐xylyl‐18‐crown‐5
Authors: Yonekawa Sayuri , Goodpaster Aaron M. , Abel Benjamin A. , Paulin Rodney G. , Sexton Charles W. , Poole James S. , Storhoff Bruce N. , Fanwick Phillip E. 
Published: March 2009

Abstractmagnified image5‐Azido‐2‐methoxy‐1,3‐xylyl‐18‐crown‐5 has been prepared by reacting p‐toluenesulfonyl azide with the carbanion generated from the reaction of 5‐bromo‐2‐methoxy‐1,3‐xylyl‐18‐crown‐5 with n‐butyl lithium. The asymmetric N3 stretch of this product has been observed as a single band at 2110 cm−1 in dichloromethane solution. Addition of solid NaSCN, KSCN and CsSCN shifts this band to 2115, 2113 and 2112 cm−1, respectively. Computational studies of this azide at the B3LYP‐6‐31G* level in the presence and absence of Na+ predicted these bands to be at 2173 cm−1 and 2184 cm−1. For the salt‐containing solutions, additional bands were observed at 2066 cm−1, 2056 cm−1 and 2055 cm−1, respectively, which are in the range expected for CN stretches. The X‐ray structure of this azide has been determined. The terminal and internal NN bond lengths were found to be 1.127(2) and 1.245(2) Δ, respectively, which is the usual pattern for aromatic azides. The crown ether is looped over the face of the aromatic ring resulting in an angle of 38.94° between the plane defined by the aromatic ring and that defined by the five ring oxygen atoms. In addition, the CH3 group is rotated out of the plane of the phenyl ring with C1‐C18‐O181‐C182 and C17‐C18‐O181‐C182 dihedral angles of 93.81(14)° and ‐90.54(14)°, respectively.
A study on the ability of 2,5‐dihydro‐ and 2,3,4,5‐tetrahydro‐1h‐phosphole oxides, as well as 7‐phosphanorbornene 7‐oxide derivatives to undergo uv light‐mediated fragmentation‐related phosphinylation of methanol
Authors: Keglevich Gyöurgy , Kovács János , Szelke Helga , Köurtvéalyesi Tamás 
Published: March 2009

Abstractmagnified imageReactivity of the title P‐heterocycles (1‐14) in the photoinduced fragmentation‐related phosphinylation of methanol was found to be influenced by the extent of ring strain and the UV absorption at 254 nm. The 7‐phosphanorbornene oxides (7‐14) are universal precursors due to their ring strain, no matter if they are UV‐active or not at 254 nm. The easily available 2,5‐dihydro‐1H‐phosphole oxides can be applied only in case of 1‐phenyl substitution that enhances the absorption at 254 nm. The ring strain of representative P‐heterocycles (5‐8) was evaluated by HF/6‐31G* and B3LYP/6‐31+G* calculations. UV spectra of compounds 5‐8 were interpreted by ZINDO/S and MNDO‐d calculations. The new precursors (11‐14) made possible the extension of the phosphinylations.
Novel synthesis of 2H‐3,1‐benzoxazine derivatives
Authors: Li Jia‐Rong , Ma Shu‐Ling , Sun Yong‐Jiang , Wei Xiao‐Jie , Zhou Zhi‐Ming 
Published: March 2009

Abstractmagnified imageOn heating of the 2‐amino‐5‐nitrobenzonitrile 1 with cyclohexanone 2a in the presence of catalyst, the novel compound 6‐nitrospiro[3,1‐benzoxazine‐2,1′‐cyclohexan]‐4(1H)‐imine 5a was formed. Also, reaction of 1 with cyclopentanone 2b or cycloheptanone 2c afforded 5b or 5c respectively. All new compounds were identified by 1H NMR, 13C NMR, IR, MS spectra and elemental analysis. The crystal structure of product 5a was determined by crystal X‐ray diffraction. And the mechanism for these reactions is proposed.
1,3‐Dihydro‐2H‐imidazo[4,5‐c]pyridin‐2‐one
Authors: Holt Jarle , Bakke Jan M. , Fiksdahl Anne 
Published: March 2009

Abstractmagnified imageA facile acid catalysed cyclisation method for the preparation of the cyclic urea 2H‐imidazo[4,5‐c]pyridin‐2‐one (2) in > 95 % yield is reported. The biologically active compound 2 can be obtained by heating (3‐amino‐4‐pyridinyl)‐carbamic acid methyl, ethyl or tert‐butyl esters (1a‐c) in sulfuric acid (0.1 %) or in aqueous HBF4 (3.5 equivalents) for 10 min. ‐ 3 hrs at 90 °C. The corresponding microwave‐promoted (MW) reactions afforded the pure product 2 within few minutes. The 6‐butylamino‐substituted analogue (2a) was correspondingly obtained by MW irradiation in 99 % yield by cyclisation of 2‐(butylamino)‐5‐amino‐4‐pyridylcarbamic acid isopropyl ester (1d). Quantitative precipitation of product 2 was obtained by pH adjustment. The process represents a solvent‐free, “green” method for the preparation of 2.
One pot synthesis of diarylpyrido[3,2‐c]coumarins
Authors: Pandya Shashi U. , Pandya Urvish R. , Hirani Bhanu R. , Brahmbhatt Dinker I. 
Published: March 2009

Abstractmagnified imageVarious diarylpyrido[3,2‐c]coumarins 3a‐l have been synthesized in one step by reacting 4‐hydroxy coumarins 1a‐d with α,β‐unsaturated ketones 2a‐c in the presence of ammonium acetate and acetic acid under Kroehnke's reaction conditions.
The dipolar route to naphtho[2,1‐c]isoxazoles from the baylis‐hillman adducts of 2‐alkynylbenzaldehydes
Authors: Ji Sang‐Hoon , Hong Wan Pyo , Ko Seung Ho , Lee Kee‐Jung 
Published: March 2009

Abstractmagnified imageA new synthesis of 4‐carbomethoxynaphtho[2,1‐c]isoxazoles 4a‐d from methyl 3‐(alkynylphenyl)‐2‐nitromethyl‐2‐propenoates 2a‐d by the intramolecular nitrile oxide cycloaddition is described. The latter are readily obtained from 2‐alkynylbenzaldehydes through the Baylis‐Hillman adduct acetates 1a‐d followed by nucleophilic substitution of nitrite anion.
Transformation of a spirobarbituric acid via aminobarbituric acid‐hydantoin rearrangement
Authors: Ambrożak Agnieszka , Güutschow Michael 
Published: March 2009

Abstractmagnified imageA successful application of the aminobarbituric acid‐hydantoin rearrangement to produce a bicyclic carbamoylhydantoin from an intermediate spirobarbituric acid is reported. 7a‐Phenylcarbamoyl‐tetrahydro‐1H‐pyrrolo[1,2‐c]imidazole‐1,3(2H)‐dione (8) was obtained in a one‐pot multistep reaction of 1‐acetyl‐2,2‐bis(ethoxycarbonyl)pyrrolidine (5) and phenylurea in the presence of sodium ethoxide. Under less severe conditions, 5 and phenylurea were reacted to afford 1‐acetyl‐7‐phenyl‐triaza[4,5]decane‐6,8,10‐trione (6). The structural elucidation of the bicyclic hydantoin 8 and the spirobarbituric acid 6 was based on relevant nmr signals in accordance with those of reference compounds, i.e. monocyclic hydantoins 4a,b and acetamidobarbituric acids 2a‐c. The latter compounds were newly prepared from diethyl acetamidomalonates 1 and phenylurea.
An efficient one‐pot synthesis of 6‐aryl‐5‐cyano‐2‐thiopyrimidinone derivatives and their piperidinium ionic forms, x‐ray crystal structures
Authors: Balalaie Saeed , Bararjanian Morteza , Rominger Frank 
Published: March 2009

Abstractmagnified imageThree‐component condensation of benzaldehyde derivatives, alkyl cyanoacetates and thiourea in the presence of piperidine in reflux condition provides a direct route to piperidinium 6‐aryl‐5‐cyano 2‐thiopyrimidonate salts in good yields. These reactions were also carried out under microwave irradiation. The yields of products under the microwave condition were better as compared to the reflux media. The acidification of these ionic forms resulted in the formation of 6‐aryl‐5‐cyano‐2‐thiopyrimidone derivatives. The X‐ray structures of the ionic forms (4, 5, and 7) show that there are anionic thiopyrimidinone skeletons hydrogen bridged with piperidinium cations.
A facile synthesis of pyrazolo[3,4‐D]pyridazines Via the 1,3‐dipolar cycloaddition of 3‐arylsydnones. Synthesis and computational studies of 1‐aryl‐4,5‐dihydro‐1H‐pyrazolo[3,4‐D]pyridazine‐3,6‐diones and their 3,6‐dichloro derivatives.
Authors: Sanyal R. , Badami Bharati V. 
Published: March 2009

Abstractmagnified imageThe synthetic utility of 1,3‐dipolar cycloaddition of DMAD to sydnones has been exploited in the preparation of new 1‐aryl‐4,5‐dihydro‐1H‐pyrazolo[3,4‐d]pyridazine‐3,6‐diones 7a‐j and their aromatic 3,6‐dichloro analogues 8a‐j. The lactam‐lactim tautomerism of compound 7a has been studied by the semi emperical (PM3) and ab initio methods.
Ring transformation of 1,5‐diazabicyclo[3.1.0]hexanes under the action of arylketenes
Authors: Shevtsov Alexander V. , Kuznetsov Vladimir V. , Kislukhin Alexander A. , Petukhova Vera Yu. , Strelenko Yu. A. , Makhova Nina N. , Lyssenko Konstantin A. 
Published: March 2009

Abstractmagnified imageThe reactions of 1,5‐diazabicyclo[3.1.0]hexanes 8 with arylketenes 1 have been studied in different conditions. The 1‐(arylacethyl)pyrazolidines 11 were obtained at −30 °C in ether and at 20 °C in benzene instead of the expected bicyclic systems 1,5‐diazabicyclo[3.2.1]octan‐6‐one 9 and 3‐aryl‐1,5‐diazabicyclo[3.3.0]octane‐2‐one 10. The synthesis of two representatives of bicycles 10 (10a,b) proceeded in the reaction of unsubstituted 1,5‐diazabicycle[3.1.0]hexane 8a, accordingly, with diphenylketene 1a in benzene at 20 °C and with 4‐chlorophenylketene 1b in toluene at 60‐110 °C. Mechanisms of the studied transformations were offered.
Synthesis and chemical transformation of fused tetrazoles derived from 2‐bromomethyl‐ and 2‐iodomethyl‐3,5,6,7‐tetrahydro‐4(2H)‐benzofuranones
Authors: Mphahlele Malose J. , Moekwa Thwanthwadi B. 
Published: March 2009

Abstractmagnified imageThe 2‐bromomethyl‐3,5,6,7‐tetrahydrobenzofuranones 1a‐d were subjected to triazidochlorosilanesodium azide‐mediated Schmidt rearrangement to afford the corresponding tetrazolofuroazepine derivatives 2a‐d via methylene shift. Under similar reaction conditions, the 2‐iodomethyl‐3,5,6,7‐tetrahydrobenzofuranones 1e‐h afford mixtures of the corresponding tetrazolofuroazepines 2e‐h and the 4‐azido‐2‐iodomethyl‐2,3‐dihydrobenzofuran derivatives 3a‐c. A mechanism is proposed to account for the divergence in the reactivity of these 2‐halogenomethyltetrahydrobenzofuranones (X = Br versus I). In turn, the 2‐halogenomethyltetrazolofuroazepines 2a,b,d‐h and the 4‐azido‐2‐iodomethyl‐2,3‐dihydrobenzofurans 3a,b underwent nucleophilic substitution with triethyl phosphite and dehydrohalogenation using DBU in refluxing toluene to give the corresponding tetrazolofuroazepines 4a‐d and 5a‐c and benzofurans 6a,b.
Efficient synthesis of 3‐arylaminopyrroline‐2‐ones by the tandem reaction of anilines and β,γ‐unsaturated α‐ketoesters
Authors: Wu Yan‐Chao , Liu Li , Wang Dong , Chen Yong‐Jun 
Published: March 2009

Abstractmagnified imageA concise and efficient synthetic approach to 3‐arylaminopyrroline‐2‐ones from anilines and β,γ‐unsaturated α‐ketoesters in boiling dichloromethane has been developed. This protocol possesses many advantages such as short reaction time, high isolated yields, and expanding substrate scopes. According to the isolated intermediates and controlled reactions, the reaction was tentatively proposed to involve the Michael addition/condensation and subsequent intramolecular cyclization. The structures of the title compounds were unambiguously confirmed by various spectral data such as X‐ray crystallographic analysis.
New TRANS/CIS tetrahydroisoquinolines. 3. [1,3]‐oxazolo‐[3,2‐B]‐tetrahydroisoquinolinones having an angular aryl substituent
Authors: Christov P. P. , Kozekov I. D. , Palamareva M. D. 
Published: March 2009

Abstractmagnified imageThe parent compound 5‐oxo‐10a‐phenyl‐2,3,10,10a‐tetrahydro‐5H‐[1,3]‐oxazolo‐[3,2‐b]‐isoquinoline‐10‐carboxylic acid (5) was prepared in large scale and a good yield by reaction between homophthalic anhydride (3) and 4,5‐dihydro‐2‐phenyl‐1,3‐oxazole (4). Thus, the closure of the isoquinoline ring and fusion of the 1,3‐oxazol ring occur in one step. Trans configuration was assumed for the product. The parent acid 5 was converted in four steps to the target aminomethyl derivatives 9a‐1. The latter contain four features that make them interesting from pharmaceutical point of view.
Synthesis and biological activities of cis and trans 5‐amino‐3‐[(6‐chloro‐3‐pyridyl)methyl]amino‐1‐(5,5‐dimethyl‐2‐oxo‐4‐substitutedphenyl‐1,3,2‐dioxaphosphinan‐2‐yl)‐4‐cyano(ethoxycarbonyl)‐1H‐pyrazoles
Authors: Luo Zai‐Gang , Shi De‐Qing 
Published: March 2009

Abstractmagnified imageA series of novel title compounds have been designed and synthesized by a multi‐step reaction, the stereochemistry of the reaction was investigated, the structures of all compounds prepared have been confirmed by 1H NMR, IR, EI‐MS spectroscopy and elemental analysis. The crystal structures of cis 6b and trans 6b were determined by single crystal X‐ray diffraction. The results of preliminary bioassay indicate that some compounds possess a certain extent inhibition effect against aphides at the concentration of 250 ppm.
Convenient synthesis of some 2‐substituted 4(3H)‐quinazolinone derivatives
Authors: Philipova I. , Dobrikov G. , Krumova K. , Kaneti J. 
Published: March 2009

Abstractmagnified imageA series of 2‐substituted‐4(3H)‐quinazolinones 13‐20 has been synthesized in good yields using the reaction of double lithiated 2‐methylquinazolinone‐4 with a variety of aromatic aldehydes. They have been easily transformed in high yields into the corresponding 2‐substituted conjugated derivatives 21‐28 bearing terminal aryl groups by F3CCOOH mediated dehydration.
Stereocontrolled synthesis of tricyclic fused oxazolidinone as antibacterial agent
Authors: Cui Yingjie , Dang Yaxian , Yang Yushe , Ji Ruyun 
Published: March 2009

Abstractmagnified imageTricyclic fused oxazolidinone 3a and 3b have been synthesized as antibacterial agents in 12 and 11 steps respectively. The key intermediates 10a and 10b have been developed via opening of epoxide 9a and 9b and cyclization by the resulting oxygen anion attack.
Chemistry of quinuclidines as nitrogen bicyclic bridged‐ring structures
Authors: Hamama Wafaa S. , El‐Magid Osama. M. Abd , Zoorob Hanafi H. 
Published: March 2009

AbstractThis review summarises the structure, basicity, asymmetric organocatalysis, synthesis and reactions of quinuclidines. Quinuclidines are bicyclic saturated pyridin‐containing compounds with rigid structures and a ring‐juncture nitrogen atom. This review covers the period from 1984–2005.
Highly diastereoselactive synthesis of chimeras of proline and glutamate
Authors: Kudryavtsev Konstantin V. , Tsentalovich Mikhail Yu. , Yegorov Anton S. , Kolychev Eugene L. 
Published: March 2009

Abstractmagnified imageAzomethine ylides have been generated from aromatic aldimines of α‐amino acid methyl esters under treatment with LiBr/Et3N and trapped with tert‐butyl acrylate yielding racemic orthogonally protected cis‐5‐arylpyrrolidine‐2,4‐dicarboxylates regio‐ and stereo‐selectively in high yields. Subsequent N‐methylation and deprotection of 4‐carboxylic group of cycloaddition products led to novel prolineglutamate cis‐chimeras with substituents at 2 and 5 positions of pyrrolidine scaffold.
A highly regioselective synthesis of 1‐n‐methyl‐spiro‐[2,3′“]‐oxindole‐spiro‐[3,2”]indane‐1“, 3”‐dione‐4‐arylpyrrolidines through 1,3‐dipolar cycloaddition protocol
Authors: Babu A. R. Suresh , Raghunathan R. , Gayatri G. , Sastry G. Narahari 
Published: March 2009

Abstractmagnified image2‐Arylidene‐1,3‐indanediones undergo a regioselective 1,3‐dipolar cycloaddition reaction with the azomethine ylide derived from isatin and sarcosine by decarboxylative route affording a series of 1‐N‐methyl — spiro[2.3′“]oxindole‐spiro[3.2”]indane‐1“,3”‐diones‐4‐aryl pyrrolidines. The structures were established by spectroscopic techniques as well as single crystal X‐ray analysis. Density functional theory at B3L YP/6‐31G* and the semi empirical AM1 calculations were employed to rationalize the observed results. The experimental regioselectivity of 1,3‐dipolar cycloadditions could be corroborated nicely with the computed Fukui frontier orbital energies and reaction energies.
Synthesis of new flat polyheterocyclic systems potential DNA intercalating agents diazines part 47
Authors: Audoux Jérôme , Achelle Sylvain , Turck Alain , Marsais Francis , Plé Nelly 
Published: March 2009

Abstractmagnified imageUsing a regioselective metallation in connection with Stille cross‐coupling reaction, we report here an original synthetic route to obtain in few steps various flat tetra‐ or pentaheterocyclic compounds which could be potential intercalating DNA agents.
Alpha vinylation of haloquinoline‐5,8‐diones with methyl acrylate and methyl vinyl ketone under baylis‐hillman reaction conditions
Authors: Song Hyoung Seok , Song Young Seok , Lee Kee‐Jung 
Published: March 2009

Abstractmagnified imageA synthesis of mono‐ and di‐vinylquinolinediones based on substitution of the halogens in 6,7‐dihaloquinoline‐5,8‐diones by DABCO‐assisted enolate ion is described. Divinylquinolines undergo 6π‐electrocyclization by thermally to give the benzo[g]quinoline derivatives.
Regioselective one pot synthesis of 2‐alkyl/aryl‐4h‐benzo[1,4] thiazine‐3‐one via microwave irradiation
Authors: Kamila Sukanta , Koh Benjamin , Khan Omair , Zhang Hongming , Biehl Edward R. 
Published: March 2009

Abstractmagnified imageA series of 2‐alkyl/aryl‐4H‐benzo[1,4]thiazine‐3‐ones have been synthesized by microwave irradiation of ethyl‐2‐bromo‐2‐alkyl/aryl acetate and 2‐amino thiophenol in the presence of 1,8‐diazabicyclo‐[5.4.0] undec‐7‐ene and N‐methylpiperidine. All compounds were characterized by 1H NMR, 13C NMR and elemental analyses, and by X‐ray crystallography in the case of 2‐methyl‐4H‐benzo[1,4]thiazin‐3‐one.
Some imines and azo compounds containing furoxan ring synthesized from methylisoeugenol
Authors: Dinh Nguyen Huu , Ly Ngo Thi , Van Hoan Pham 
Published: March 2009

Abstractmagnified imageSome imines and azo compounds containing furoxan and benzene rings have been prepared starting from methylisoeugenol. The structure of reported compounds has been confirmed by elemental analysis, ms, uv, ir, and nmr spectroscopy. It is shown that, on treatment with Na2S2O4, the nitro group on the benzene ring was reduced to an amino group, but the N←O group of furoxan ring was not. The 1H‐ and 13C nmr signals are assigned based on their spin‐spin splitting patterns, in some cases, NOESY and HMBC spectra are used. The NOESY spectra indicate that the reported imines have E‐configuration. Among 8 tested compounds, there are 5 compounds that exhibit anti‐microbial activity toward Gr+ S. aureus at concentration 12.5μg/mL.