bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis of 3,4‐dihydro‐1(2H)‐isoquinolinonesxs
Authors: Showalter H. D. Hollis , Sercel Anthony D. , Stier Michael A. , Turner William R. 
Published: March 2009

AbstractApproaches toward the preparative‐scale synthesis of target 3,4‐dihydro‐1(2H)‐isoquinolinones 1–3 are presented. Compounds 1 and 2 were prepared via a Schmidt rearrangement on easily obtained indanone precursors, but in low overall yield. A better method to make this class of compounds is exemplified by the large‐scale synthesis of 2 via a Curtius rearrangement sequence. Thus, high‐temperature thermal cyclization of an in situ formed styryl isocyanate from precursor 8 in the presence of tributylamine gave the corresponding 1(2H)‐isoquinolinone (9). Catalytic hydrogenation of 9 provided the desired 3,4‐dihydro‐5‐methyl‐1(2H)‐isoquinolinone (2) in 65 % overall yield. Similar reduction of a commercially available 5‐hydroxy‐1(2H)‐isoquinolinone precursor 10 followed by an O‐alkylation/amination sequence gave target 3 in good overall yield. The route proceeding via the Curtius rearrangement is recommended for large scale synthesis of other 3,4‐dihydro‐1(2H)‐isoquinolinones. Only when deactivating substituents or sensitive functionality within the benzenoid ring render the high temperature ring closure of the intermediate isocyanate inefficient might a Schmidt rearrangement protocol be the method of choice.
Synthesis of new thienotriazolopyrimidine and thienopyrimidotetrazine derivatives from bifunctional intermediates
Authors: Modica Maria , Santagati Maria , Santagati Andrea 
Published: March 2009

AbstractNew compounds containing the thienotriazolopyrimidine and thienopyrimidotetrazine skeleton are prepared from the bifunctional intermediates 2,3‐diamino‐5,6‐dimethylthieno[2,3‐d]pyrimidin‐4(3H)‐one derivatives 13–17. The 2,3‐dihydro‐3‐substituted‐5,6‐dimethylthieno[2,3‐d]pyrimidin‐4(1H)‐one derivatives 8–12 are also prepared.
Synthesis of new pyrazolo[1,5‐a]pyrimidines and pyrazolo[3,4‐b]pyridines
Authors: Al‐Mousawi Saleh M. , Mohammad Mohammad A. , Elnagdi Mohamad H. 
Published: March 2009

AbstractWhile 3(5)‐aminopyrazole reacts with enaminonitrile to yield pyrazolo[1,5‐a]pyrimidines, 3‐amino‐5‐pyrazolone reacts with the same reagents to yields pyrazolo[3,4‐b]pyridines.
A facile synthesis of biogenetic precursor, puerarone, isolated from Pueraria sp
Authors: Khan Riaz A. , Kapil Randhir S. 
Published: March 2009

AbstractPuerarone was synthesized using chalcone oxidation with thallium (III) trinitrate and chromenation of the resulting isoflavone using 3‐hydroxyisovaleraldehyde dimethylacetal. The key demethylation step was achieved with boron tribromide.
Synthesis of novel pyrazolopyrrolopyrazines, potential analogs of sildenafil
Authors: Kopp Marina , Lancelot Jean‐Charles , Dallemagne Patrick , Rault Sylvain 
Published: March 2009

AbstractSynthesis of novel pyrazolopyrrolopyrazines is herein described with the aim to reach new specific PDE‐5 inhibitors of potential clinical interest in male erectile dysfunction.
Efficient one pot preparation of variously substituted thieno [2,3‐b] thiophene
Authors: Cornel Alain , Kirsch Gilbert 
Published: March 2009

AbstractAn efficient one pot access to variously substituted thieno[2,3‐b]thiophene is described. The title compounds were obtained from 1,3‐dicarbonyl or equivalent compounds, carbon disulfide and halomethyl derivatives in good to high yields and fully characterized.
A revision of the alcoholysis and alkanethiolysis of 3‐amino‐6‐chloropyridazine
Authors: Maes Bert U. W. , Lemière Guy L. F. , Dommisse Roger , Haemers Achiel 
Published: March 2009

AbstractThe synthesis of 3‐amino‐6‐alkoxy‐ and 3‐amino‐6‐alkylthiopyridazines via nucleophilic aromatic substitution on 3‐amino‐6‐chloropyridazine is described. In contrast to literature reports, no pressure tube is required to perform these reactions.
Synthesis of methyl‐2,4‐bis(cyclohexane)dispiro‐1,2,3,4,4a,5,6,7‐octahydro‐(lH,3H)quinazoline‐8‐carbodithioate derived from cyclohexanone in one step
Authors: Contreras Ricardo R. , Fontal Bernardo , Reyes Marisela , Suárez Trino , Bellandi Fernándo , Bahsas All 
Published: March 2009

AbstractThe new compound Methyl‐2,4‐bis(cyclohexane)dispiro‐1,2,3,4,4a,5,6,7‐octahydro‐(1H,3H)‐quinazo‐line‐8‐carbodithioate has been synthesized from cyclohexanone and carbon disulfide. It has been characterized by uv‐visible, FTTR, mass spectra and a complete structure proposed based on 1H and 13C NMR spectroscopy.
New compounds in ring‐opening reaction of 5‐substituted epoxyisoindolines
Authors: Mance Ana Dunja , Borovička Branko , Jakopčić KreŠImir , Pavlović Gordana , Leban Ivan 
Published: March 2009

AbstractMethoxy or nitro group present in the furan ring of tertiary alkenylfurfurylamine changes the expected results of both, the intramolecular [4+2]cycloaddition and the acid catalyzed ring‐opening reaction of the derived oxatricycloadduct. With a 5‐methoxy group, in addition to the expected 5‐methoxyisoindoline 3, the corresponding hydroxy derivative 5 was obtained. On the other hand a 5‐nitro group changes the outcome of the reaction even more profoundly. Instead of the expected 5‐nitroisoindoline 12, 5‐nitro‐substituted epoxy‐isoindoline 6 submitted to ring‐opening reaction with the mixture of hydrobromic and acetic acid, yielded the mixture of bromo‐substituted epoxy compounds 7,8, 9 and/or bromo‐substituted isoindolines 10 and 11.
On triazoles XLIV [1]. synthesis of new ring systems containing imidazo[2′,1′:3,4] [1,2,4] triazolo [1,5‐a]pyrimidine and imidazo[1′,2′:2,3][1,2,4]triazolo[1,5‐a]pyrimidine skeleton
Authors: Berecz Gábor , Reiter József , Argay Gyula , Kálmán Alajos 
Published: March 2009

AbstractDedicated to Dr. János Császár on the occasion of his 70th birthdayRing transformation of 2‐cyanoimido‐3‐methyl‐1,3‐oxazolidine (10) yielded 5‐amino‐3‐[N‐(2‐hydrox‐yethyl)‐N‐methyl]amino‐1H‐1,2,4‐triazole (6) that was ring closed with different β‐keto esters to 2‐[N‐(2‐hydroxyethyl)‐N‐methyl]amino‐1,2,4‐triazolo[1,5‐a]pyrimidinones (4). Cyclisation of derivatives 4 led to imidazo[2′,1′:3,4][1,2,4]triazolo[1,5‐a]pyrimidines (2) and imidazo[1′,2′:2,3][1,2,4]triazolo[1,5‐a]pyrim‐idines (3) representing 10 novel ring systems. Besides spectroscopical evidence of structure of derivatives 2 and 3 X‐ray diffraction analysis of derivative 2b was also performed.
On triazoles XLV [1]. synthesis of 5,7‐diamino‐1,2,4‐triazolo[1,5‐a] [1,3,5]triazines
Authors: Berecz Gábor , Pongó László , Kövesdi István , Reiter József 
Published: March 2009

AbstractDedicated to Professor András Messmer on the occasion of his 80th birthdayThe reaction of differently substituted 5‐amino‐1,2,4‐triazoles (5) with isothiourea derivatives (3) to yield isomeric 5,7‐diamino‐1,2,4‐triazolo[1,5‐a][1,3,5]triazines (6 and 7), previously described as not proceeding in melt, was performed in different solvents as well as in the melt at 150‐160°. It was proved that the above reaction had rather general validity. The structure of isomers 6 and 7 were proved spectroscopically. The structure of 6/5 (Q = ethylamino) was corroborated with single crystal X‐ray diffraction determination, as well.
Diarylthiopyrimidines and pyridines: Synthesis and biological activity
Authors: Delia Thomas J. , Kanaar John B. , Knefelkamp Elizabeth 
Published: March 2009

AbstractPrior work with diarylethers of pyrimidine, pyridine, and benzene showed encouraging antitumor results. As an extension of that work the synthesis of diarylthio derivatives of pyrimidine and pyridine has been accomplished. The synthetic scheme employed the nucleophilic displacement of chlorines from trichloropyrimidine, 1, dichloropyrimidines 4 and 6, and 2,6‐dichloropyridine 8 using the anion of thiophe‐nols 2. Antitumor evaluation by the National Cancer Institute showed no useful activity.
Unexpected ring closure reaction of α,β‐unsaturated ketones with aminoguanidine. entry into 1,3,5‐trisubstituted pyrazoles
Authors: Světlík Jan , Šallai Ladislav 
Published: March 2009

AbstractCyclizations of α,β‐unsaturated ketones with aminoguanidine under neutral conditions were examined. In contrast to literature reports of 1,2,4‐triazines as reaction products, formation of 5‐aryl‐4,5‐dihy‐dro‐3‐methyl‐1H‐pyrazole‐1‐carboximidamides and carboxamides was observed. An explanation based on the Hard‐Soft Acid‐Base principle is presented and the probable causes of divergent reaction pathways are discussed.
Synthesis and spectral properties of 7‐chloro‐5‐[(o‐ and p‐R1)phenyl]‐1‐R2‐3H‐[1,4]benzodiazepin‐2‐ones
Authors: Cortés Eduardo Cortés , Martínez Isidro Ebromares , Mellado Olivia García 
Published: March 2009

AbstractA series of twelve new 7‐chloro‐5‐[(o‐ and p‐R1)phenyl]‐1‐R2‐3H‐[1,4] benzo‐diazepin‐2‐ones, which have possible pharmacological properties were synthesized. The synthesis of all the final compounds was carried out by four steps. The structure of all final products was corroborated by ir, 1H nmr, 13C nmr and ms, and have been obtained in 35‐94% yield.
Synthesis of tetronic acid derivatives from novel active esters of α‐hydroxyacids
Authors: Mitsos Christos , Zografos Alexandras , Igglessi‐Markopoulou Olga 
Published: March 2009

AbstractActive esters, produced by condensation of O‐acetyl protected α‐hydroxyacids with N‐hydroxysuccin‐imide, react with anions of active methylene compounds to afford β,β‐tricarbonyl derivatives which upon deprotection undergo cyclization to 3‐alkoxycarbonyl and 3‐acyl tetronic acids. Incorporation of (S)‐2‐ace‐toxyphenylacetic acid in this reaction sequence enables the synthesis of optically active 5‐phenyltetronic acid derivatives.
Determination of aromaticity indices of thiophene and furan by nuclear magnetic resonance spectroscopic analysis of their phenyl esters
Authors: Lee Chang Kiu , Yu Ji Sook , Lee Hye‐Jin 
Published: March 2009

AbstractA series of m‐ and p‐substituted phenyl benzoates, 2‐thienoates, and 2‐furoates were prepared and their 1H and 13C nmr spectroscopic characteristics were examined. In general, good correlations were observed between the chemical shift values of protons and carbons of the acyl aromatic rings and the Hammett σ. Plots of the chemical shift values of the carbonyl carbons of the benzoates against those of the 2‐thienoates and 2‐furoates gave an excellent correlation and the values of the slopes are 0.85 and 0.75, respectively, in dimethyl sulfoxide‐d6 and 0.90 and 0.78, respectively, in chloroform‐d. The values could be considered as a set of aromaticity indices.
Synthesis of 2‐(1‐methyl‐1,2,5,6‐tetrahydropyridin‐3‐yl)benzimidazoles
Authors: Jung Myung Hee , Park Jung Mee , Lee Ihl‐Young Choi , Ahn Mija 
Published: March 2009

AbstractA useful approach for the synthesis of pharmacologically active tetrahydropyridinylbenzimidazoles is described. 2‐Pyridin‐3‐ylbenzimidazoles 3a‐d have been synthesized by condensation of 3‐pyridinecarbox‐aldehyde 1 with substituted 1,2‐phenylenediamines 2a‐d following oxidative cyclization with iodobenzene diacetate. Methylation of 3a‐d with iodomethane and potassium hydroxide, subsequent formation of methylpyridinium salts 4a‐d and 7a‐d and reduction thereafter afforded tetrahydropyridinylbenzimidazoles 5a‐d and 8a‐d.
The synthesis of 4‐amino‐3‐(2‐pyridyl)pyrazolo[5,1‐c][1,2,4]triazine and some of its derivatives
Authors: Cankař Petr , Slouka Jan 
Published: March 2009

AbstractA mixture of both geometrical isomers of hydrazones 3a‐3e was obtained by the coupling reactions of pyrazole‐3‐diazonium salts 2a‐2d and benzenediazonium chloride 2e with 2‐pyridylacetonitrile 1. Hydrazones 3a‐3d were cyclized to the corresponding 4‐amino‐3‐(2‐pyridyl)pyrazolo[5,1‐c][1,2,4]triazines 4a‐4d.
Synthesis and properties of bowl‐shaped homotriazacalix[3 and 6] arenes and the acyclic analogues
Authors: Ito Kazuaki , Sato Tomokazu , Ohba Yoshihiro 
Published: March 2009

AbstractBowl‐shaped chiral homotriazacalixarenes were prepared by the cyclization reactions of chiral triamines with three equimolar amounts of bis(chloromethyl) phenols or bis(chloromethyl) phenol‐formaldehyde dimers in moderate yields. The corresponding acyclic phenol‐formaldehyde oligomers were also synthesized. The structural analysis of the macrocycles by nmr and circular dichroism spectra imply the existence of chiral transmission from the point chirality of the cysteine bridge to the cyclophane moiety. Their cyclic and acyclic compounds have a π‐base cavity large enough to include the ammonium ion.
N‐phenyl‐substituted pyrrolidines, piperidines and azabicyclics by a tandem reduction‐double reductive amination reaction
Authors: Bunce Richard A. , Herron Derrick M. , Lewis Jason R. , Kotturi Sharadsrikar V. 
Published: March 2009

AbstractN‐Phenyl‐substituted pyrrolidines and piperidines have been synthesized by catalytic reduction of nitrobenzene in the presence of 4‐ and 5‐oxoaldehydes, respectively. The process involves reduction of the aromatic nitro group to give the N‐phenylhydroxylamine or aniline followed by reductive amination with the two carbonyl functional groups. Monocyclic systems are generally formed in high yield and are easily purified. The method has also been extended to the synthesis of fused N‐phenylazabicyclics from 2‐(3‐oxo‐propyl)cycloalkanones. A high degree of diastereoselectivity for the trans‐fused product is observed in substrates having an ester group α to the cycloalkanone carbonyl. Bicyclic precursors lacking this ester group give mixtures of cis and trans products. Finally, contrary to previous reports, we have demonstrated that aniline can be substituted for nitrobenzene in these reactions.
Solid‐phase synthesis of a novel series of 2,3,4,5‐tetrahydro‐1,4‐benzodiazepin‐2,5‐dione libraries
Authors: Migihashi Chiaki , Sato Fuminori 
Published: March 2009

AbstractAn efficient solid‐phase synthetic method for 2,3,4,5‐Tetrahydro‐1,4‐benzodiazepin‐2,5‐diones, having amine derivatives on the benzene ring, was developed. This method has been successfully applied to the synthesis of several spatially separated drug‐like and information‐rich small‐molecule libraries composed of 400 compounds using ACT‐496 automatic synthesizer and the IRORI radio frequency‐encoded split‐mix synthesis technology.
Synthesis of some novel annelated 1,2,3‐selena/thiadiazoles and 2h‐diazaphospholes
Authors: Padmavathi Venkatapuram , Reddy Dandu Bhaskar , Reddy Tippireddy Venkat Ramana , Reddy Kamireddy Audisesha 
Published: March 2009

AbstractA number of annelated heterocyclic indene derivatives having 1,2,3‐selena/thiadiazole and 2H‐1,2,3‐diazaphosphole rings have been synthesized by exploiting the α‐ketomethylene functionality in some novel 1‐methyl‐piperidin‐4‐ones and 1‐oxo‐tetrahydrothiopyran‐4‐ones and were characterized by their physical and spectral data.
N‐Azolylmethyl ketones as building blocks in heterocyclic synthesis: Synthesis of new polyfunctionally substituted azolylarylazophenols, azolylpyridones and azolylthiophenes
Authors: Al‐Saleh Balkis , El‐Apasery Morsy Ahmed , Abdelkhalik Mervat Mohammed , Elnagdi Mohammed Hilmy 
Published: March 2009

AbstractThe title compounds 1a‐b and 2 reacted with 2‐arylhydrazonopropanals 3a‐c to yield polyfunctionally substituted azolylarylazophenols 5 and 8. The reaction of 1b and 2 with phenylisothiocyanate in the presence of α‐haloketones afforded the azolylthiophenes 12a,b and 13a,b. The reaction of 20 with α‐haloketone afforded 5‐benzotriazol‐1‐yl‐6‐methyl‐2‐(2‐oxopropylsulfanyl)nicotinonitrile 21 that was utilized as building blocks for the synthesis of condensed pyridines. Compound 21 was condensed with dimethylformamide dimethylacetal to yield thieno[2,3‐b]pyridin‐3‐yl‐N, N‐dimethylformamidine derivative 22. This was further cyclized with sodium hydride to 1H‐fhieno[2,3‐b; 4,5‐b']dipyridin‐4‐one derivative 23.
Synthesis of 1‐azabicyclic systems by double cyclization
Authors: Oka Mitsuru , Baba Kunihisa , Hamajima Hitoshi , Unno Ryoichi , Matsumoto Yukiharu , Nakamura Kensuke , Dong Lulu 
Published: March 2009

Abstract5‐Cyano‐1‐azabicyclo[3.3.0]octane (1) was prepared in one step from 1,7‐dichloro‐4‐heptanone (4) under mild conditions. The application of this method for the preparation of 5‐cyano‐4,6‐dimethyl‐1‐azabicy‐clo[3.3.0]octane (11) gave two diastereomers in equilibrium. The NMR measurements of 11 and its reduced compound 15 showed that the major isomer is the cis‐exo form, and the minor isomer is the trans form. Molecular orbital calculations indicated that the cis‐exo form is more stable than the trans form, in agreement with the experimental results. Furthermore, 6‐cyano‐1‐azabicyclo[4.3.0]nonane (17) and 1‐azabicy‐clo[4.4.0]decane (19), both including a six‐membered ring, were prepared from appropriate haloketones by using this double cyclization method.
Azinoiminophosphorane mediated 4H,8H‐1,2,4‐triazolo[1,5‐C]‐[1,3]oxazepin‐4‐ones and 5,6‐dihydro‐7H, 12H‐naphtho[2,1‐f]‐[1,2,4]triazolo[1,5‐c][1,3]oxazepin‐7‐ones synthesis
Authors: Kim Kyoung Tae , Lee Chang Hoon , Lee Kee‐Jung 
Published: March 2009

AbstractThe aza‐Wittig reactions of benzaldehyde‐, acetophenone‐ and benzophenone 1‐[(triphenylphosphor‐anylidene)amino]ethylidenehydrazones (1) with 2,3‐furandiones 6 provide a new route to 4H,8H‐1,2,4‐triazolo[1,5‐c][1,3]oxazepin‐4‐ones 14 or 5,6‐dihydro‐7H,12H‐naphtho[2,1‐f|[1,2,4]triazolo[1,5‐c]‐[1,3]oxazepin‐7‐ones 17 via the thermal reaction of the expected azinoimine vinylogous lactones.
New reactions of carbon suboxide with alkynes
Authors: Casu Laura , Bonsignore Leonardo , Cottiglia Filippo , Loy Giuseppe , Maccioni Elias 
Published: March 2009

AbstractSynthesis of 3,4,7,8‐tetraalkyl‐2‐oxa‐bicyclo[4.2.0]octa‐1(6),3,7‐trien‐5‐ones(4a‐d),4,5,7,8‐tetraalkyl‐2‐oxa‐bicyclo[4.2.0]octa‐1(6),4,7‐trien‐3‐ones (6a‐d) and 3,4,7,8‐tetraalkyl‐2H,5H‐cyclobuta[b]pyrano‐[2,3‐d]pyran‐2,5‐diones (7a‐d) from the reaction of alkynes (la‐d) with carbon suboxide (2) in various molar ratios is described.
Synthesis and biological evaluation of structural variants of carbazoquinocin C
Authors: Aygün Alparslan , Pindur Ulf 
Published: March 2009

AbstractSome new structural variants of the alkaloid carbazoquinocin C were synthesized in a few steps with good to excellent yields. The key step comprises a cyclisation reaction of appropriate 2‐vinylindoles with oxalyl chloride. The carbazole‐3,4‐quinones are able to trap oxygen‐centred radicals. In some biological/biochemical assays some of these compounds exhibit extraordinary results including inhibition of cyclooxygenase‐1 and 5‐lipoxygenase in the μM‐range. Moreover some of the carbazoquinocin C‐variants inhibit significant oxidative damage of cellular DNA in nM‐range.
Preparation of 5,5′‐pyrilidene and 5,5′‐quinolidene bis‐barbituric acid derivatives
Authors: Jursic Branko S. , Neumann Donna M. 
Published: March 2009

AbstractNMR reaction following experiments were used to find optimal conditions for the barbituric acid double addition to aromatic and heteroaromatic carboxaldehydes. It was established that aromatic aldehydes with electron‐donating substituents such as hydroxy, methoxy, and dimethylamino produce only the single addition barbituric acid adduct (barbituric acid benzylidenes). If these electron‐donating substituents are transformed into electron‐withdrawing substituents by virtue of protonation (NMe2 to NHMe2+) then the double barbituric acid adduct becomes the sole product of the reaction. This is also true regardless of the reaction media if strong electron‐withdrawing substituents (such as a nitro group) are present. Considering that the reactive species for nitrogen containing aromatic heterocycles are actually the conjugated acids (electron deficient molecule) only the double barbituric acid adducts are isolated. All synthetic procedures presented are applicable to multi‐gram scale preparations of double barbituric acid adducts.
A study of substituent effect on 1H and 13C nmr spectra of N‐ and C‐substituted carbazoles
Authors: Bonesi Sergio M. , Ponce Maria A. , Erra‐Balsells Rosa 
Published: March 2009

Abstract1H and 13C nmr spectra of several N‐ and C‐substituted carbazoles (Series 1, 2, 3 and 4) were measured. Correlations between chemical shifts and substituent constants show that these parameters describe properly the substituent effect on the nmr phenomena. Atomic charge densities for carbazoles of Series 1, 2, 3 and 4 were calculated by using the semi empirical PM3 method. These values also show a linear correlation with the 13C chemical shifts. The synthesis of several carbazole derivatives 1a – 1g, 2a – 2g, 3a – 3j and 4a – 4g have been carried out according to literature procedures. The carbazoles 3i, 3j and 4c have been synthesized and fully characterized for the first time.
Enaminones as building blocks in heterocyclic synthesis: New syntheses of nicotinic acid and thienopyridine derivatives
Authors: Abdelkhalik Mervat Mohammed , Eltoukhy Afaf Mohammed , Agamy Samia Michel , Elnagdi Mohammed Hilmy 
Published: March 2009

AbstractReacting 1,3‐diphenyl‐propan‐2‐one with equimolecular amount of dimethylformamide dimethylacetal afforded the enaminone 4. This when reacted with another equimolecular amount of dimethylformamide dimethylacetal afforded the dienaminone 5. Compound 4 condenses with cyanothioacetamide and with cyanoacetamide to yield 2‐thioxo‐ and 2‐oxo‐pyridine‐3‐carbonitrile derivatives 6a,b respectively. Compound 6a reacted with α‐chloroacetone 8 to yield the thieno[2,3‐b]pyridine derivative 10 that cyclized further into 4,7,8‐trisubstituted pyrido[2′,3′:2,3] thieno[4,5‐d]pyrimidine 12. Compound 4 also afforded 2,5,6‐trisubstituted nicotinic acid ethyl ester 13 by reaction with ethyl acetoacetate in acetic acid in the presence of ammonium acetate. The dienaminone 5 reacted with acetic acid, ammonium acetate/acetic acid, phenylhydrazine and 5‐amino‐3‐methylpyrazole yielding 3,5‐diphenyl‐pyran‐4‐one 15a, 3,5‐diphenyl‐1H‐pyridin‐4‐one 15b and 1,3,5‐trisubstituted pyridin‐4‐ones 16a‐b.
Synthesis and characterization of new biologically active 2‐(1,3‐disubstituted pyrazolyl)chromones and corresponding pyrimidine, thiopyrimidine, pyrazolyl derivatives
Authors: Joshia N. S. , Karale B. K. , Gill C. H. , Bhirud S. B. 
Published: March 2009

AbstractA series of 2‐(1‐methyl‐3‐n‐propylpyrazol‐5‐yl)‐chromones with interestingPhosphodiesteraseIV inhibitition activities were synthesized. Different derivatives of the titled compounds like aminopyrimidine, thiopyrimidine, pyrazolyl were synthesized and theirPhosphodiesteraseIV inhibitition activities were checked.
A facile one‐pot synthesis of novel substituted 1,2,3,4‐tetrahydropyrimidine, part 2: Synthesis of 1‐(aralkyl/aryl)‐3‐(alkyl/aralkyl/aryl)‐5‐aroyl‐1,2,3,4‐tetrahydropyrimidines
Authors: Chanda Kaushik , Dutta Milan Ch. , Karim Enamul , Vishwakarma Jai N. 
Published: March 2009

Abstract1‐(Aralkyl/aryl)‐3‐(alkyyaralkyl)‐5‐aroyl‐1,2,3,4‐tetrahydropyrimidines (2a‐c) have been synthesized by dethiomethylation of 5‐aroyl‐6‐methylthio‐1,2,3,4‐tetrahydropyrimidines (1a‐c). An alternative one‐pot synthetic strategy has been developed for the title compounds 2a‐t by the reaction of enaminones 3 with pri mary amine and formaldehyde in refluxing methanol in good yields.
Novel synthesis of thieno[2,3‐b]pyridine and substituted 2‐thienylthiourea derivatives as antibiotic agents
Authors: Al‐Omran Fatima , El‐Khair Adel A. 
Published: March 2009

AbstractDerivatives of thieno[2,3‐b]pyridine, 2‐thienylthiourea, 2‐thienylurea, 2‐thienylacetamide incorporating the 2‐phthalimidomethyl moiety have been synthesized. The synthesized compounds were then investigated for antibacterial activity against Escherichia coli, Bacillus subtilis and Staphylococcus aureus. The compounds were also investigated for antifungal activity against Aspergillus niger and Fusarium oxysporium. The structures of the newly synthesized compounds have been established on the basis of their analytical and spectral data.