bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis of the enantiomers of the dual function 2‐nitroimidazole radiation sensitizer RB 6145
Authors: Sercel Anthony D. , Beylin Vladimir G. , Marlatt Mark E. , Leja Boguslawa , Showalter H. D. Hollis , Michel André 
Published: March 2009

Abstractmagnified imageShort, efficient pathways are described for the synthesis of racemic 2‐nitroimidazole radiation sensitizer RB‐6145 (2a) and each of its corresponding (R)‐ and (S)‐enantiomers (2b and 2c, respectively). The synthesis of each enantiomer commences with the appropriate chiral epichlorohydrin and utilizes a novel application of 3‐trimethylsilyl‐2‐oxazolidinone (3b) as a mild, safe surrogate for highly toxic aziridine. The synthesis of the (R)‐enantiomer (2b) has been successfully scaled up to provide multi‐kilo quantities of material for early stage preclinical evaluation.
Microwave‐assisted “green” synthesis of 2‐alkyl/arylbenzothiazoles in one pot: A facile approach to anti‐tumor drugs
Authors: Kamila Sukanta , Koh Benjamin , Biehl Edward R. 
Published: March 2009

Abstractmagnified imageA series of new 2‐alkyl/arylbenzothiazoles has been synthesized on the basis of the potent and selective in vitro anti‐tumor properties of 2‐(3,4‐diethoxyphenyl)‐5‐fluorobenzothiazole. The synthesis of benzothiazole analogs was achieved via microwave irradiation of a 1:1 mixture of o‐aminothiophenol and alkyl/aryl acylacetonitriles at temperature of 200°C for 10 min. The yields are very good to excellent. All the products were characterized by 1H nmr, 13C nmr and elemental analysis.
Synthesis of 2‐phenylquinolin‐4‐amines substituted with diverse amino and aminoalkyl groups
Authors: Say Martial , Paliakov Ekaterina , Henary Maged , Strekowski Lucjan 
Published: March 2009

Abstractmagnified imageFacile synthetic approaches to 2‐phenylquinolin‐4‐amines containing an aminoalkyl group at N4 of the quinolin‐4‐amine and amino or aminoalkyl groups at the phenyl moiety are presented.
Synthesis of 2,4‐diaminothieno‐ and pyrrolo[2,3‐d]pyrimidine‐6‐carboxylic acid derivatives
Authors: Tumkevicius S. , Dailide M. , Kaminskas A. 
Published: March 2009

Abstractmagnified imageA series of new 2,4‐diaminothieno[2,3‐d]‐ and 2,4‐diaminopyrrolo[2,3‐d]pyrimidine derivatives were synthesised. Reaction of 2‐amino‐4,6‐dichloropyrimidine‐5‐carbaldehyde (1) with ethyl mercaptoacetate, methyl N‐methylglycinate or ethyl glycinate afforded ethyl (2‐amino‐4‐chloro‐5‐formylpyrimidin‐6‐yl)thioacetate (2a), methyl N‐(2‐amino‐4‐chloro‐5‐formylpyrimidin‐6‐yl)‐N‐methylglycinate (2b) and ethyl N‐(2‐amino‐4‐chloro‐5‐formylpyrimidin‐6‐yl)glycinate (2c), respectively. Compounds 2a,b by treatment with bases cyclised to the corresponding 2‐amino‐4‐chlorothieno‐ and pyrrolo[2,3‐d]pyrimidine‐6‐carboxylates (3a,b). Heating 2,4‐diamino‐6‐chloropyrimidine‐5‐carbaldehyde (5) with ethyl mercaptoacetate or methyl N‐methylglycinate gave 2,4‐diaminothieno[2,3‐d]‐ and 2,4‐diaminopyrrolo[2,3‐d]‐pyrimidine‐6‐carboxylates (6a,b), whereas compound 5 with ethyl glycinate under the same reaction conditions afforded ethyl N‐(2,4‐diamino‐5‐formylpyrimidin‐6‐yl)glycinate (7). Treatment of 2,4‐diaminothieno[2,3‐d]pyrimidine‐6‐carboxylic acid (8a) with 4‐methoxy‐, 3,4,5‐trimethoxyanilines or ethyl N‐(4‐aminobenzoyl)‐L‐glutamate in the presence of dicyclohexylcarbodiimide and 1‐hydroxybenzotriazole furnished the corresponding N‐arylamides 9‐11.
One pot synthesis of novel dispiro[oxindole‐thiazolidinedione/thioxo‐thiazolidinone/dihydro pyrazolone]‐pyrrolidines via 1,3‐dipolar cycloaddition reaction of azomethine ylides
Authors: Ponnala Shashikanth , Sahu Devi Prasad , Kumar Rishi , Maulik Prakas R. 
Published: March 2009

Abstractmagnified imageA series of novel dispiro[oxindole‐thiazolidinedione]pyrrolidine, dispiro[oxindole‐thioxothiazolidinone]‐pyrrolidine, dispiro[oxindole‐dihydro‐pyrazolone]pyrrolidine were synthesized by both regio‐ and stereo‐selective 1,3‐dipolar cycloaddition reaction of azomethine ylide generated from amino acid and amino acid ester with π‐deficient alkenes in a single pot protocol in good yield. X‐ ray crystallographic studies established orthogonal disposition between spiro‐oxindole and spiro‐thiazolidinedione rings in 4a and 5a.
Reactions of α‐diazoketones with indolinone imines: Synthesis of new 1,3,3‐triaryl‐1′‐methylspiro[azetidine‐2,3′‐indoline]‐2′,4‐diones
Authors: Singh Girija S. , Mmolotsi Boycie J. 
Published: March 2009

Abstractmagnified imageThe paper describes the synthesis of new 1,3,3‐triary‐1′‐methylspiro[azetidine‐2,3′‐indoline]‐2′,4‐diones from reaction of the 2‐diazo‐1,2‐diarylethanones with 3‐arylimino‐1‐methyl‐2‐indolinones. The compounds have been characterized by satisfactory analytical and spectral (IR, 1H NMR and 13C NMR) data. The diarylketenes, generated in situ from thermal decomposition of the 2‐diazo‐1,2‐diarylethanones, react with azomethine linkage in preference to carbonyl group leading to the formation of products.
Synthesis of some new 4‐substituted‐3, 5‐bis(2‐pyridyl)‐1h‐pyrazole
Authors: Zhang Wei , Liu Jianhui , Jin Kun , Sun Licheng 
Published: March 2009

Abstractmagnified imageSeveral 4‐substituted‐3, 5‐bis(2‐pyridyl)‐1H‐pyrazoles, where the substituent is chloro, bromo, iodo, nitro, diazo, were synthesized under mild reaction conditions in high yields. The structures of the products were characterized by 1H NMR, 13C NMR, ESI‐MS, IR and elemental analyses.
Electrochemical oxidation of catechols in the presence of ethyl‐2‐chloroacetoacetate. Synthesis and mechanistic study
Authors: Shamsipur Mojtaba , Davarani Saied Saeed Hosseiny , Nematollahi Davood 
Published: March 2009

Abstractmagnified imageElectrochemical oxidation of catechol and some of 3‐substituted catechols (1a‐c) has been studied in the presence of ethyl‐2‐chloroacetoacetate (3) in water/acetonitrile (90:10) solution using cyclic voltammetry and controlled‐potential coulometry. The results indicate that the quinones derived from catechols (1a‐c) participate in Michael addition reactions with ethyl‐2‐chloroacetoacetate(3), with consumption of only two electrons per molecule of 1, to form the corresponding benzofurans (10a‐c). The electrochemical synthesis of benzofurans (10a‐c) has been successfully performed at a carbon rod electrode and in an undivided cell with good yields and purity. A new two‐electron mechanism for the electrode process is proposed.
Synthesis of new TTF‐anthracene dyads as potential fluorescence probe for 1O2
Authors: Liu Wei , Lu Jing‐Hua , Xu Ming , Zuo Jing‐Lin , You Xiao‐Zeng 
Published: March 2009

Abstractmagnified imageThree new fluorescence probes for 1O2 with different electron‐rich tetrathiafulvalene and anthracene units have been synthesized and characterized. Among them, compound 3c, 2,3‐bis[2‐(9‐anthryloxy) ethylthio]‐6,7‐(propylenedithio)‐1,4,5,8‐tetrathiafulvalene, is very sensitive and may act as the fluorescence probe for 1O2.
An efficient approach towards three component coupling of one pot reaction for synthesis of functionalized benzopyrans
Authors: Kumar B. Sunil , Srinivasulu N. , Udupi R. H. , Rajitha B. , Reddy Y. Thirupathi , Reddy P. Narsimha , Kumar P. S. 
Published: March 2009

Abstractmagnified imageThree component coupling of one pot reaction which servers as the most convenient route to the synthesis of benzopyran derivatives using the TiCl4 catalyst (10 mol %) under solvent free conditions is described. The procedure offers a systematic method with a number of advantages including operational simplicity, neat reactions, reduced reaction time, high yields of products and applicability to large scale reactions.
New synthesis, x‐ray structural determination, conformational analysis and anomeric effect study of 3,7‐di (3‐nitrophenyl)‐1,5‐dioxa‐3,7‐diazacyclooctane
Authors: Kakanejadifard A. , Mahmodi L. , Yari A. , Mohajeri A. 
Published: March 2009

Abstractmagnified image3,7‐Di(3‐nitrophenyl)‐1,5‐dioxa‐3,7‐diazacyclooctane was prepared from 3‐nitroaniline and formaldehyde in acetonitrile. Conformational behavior of ring inversion of the molecule was studied so it prefers a crown conformation. The evaluated ΔG* was approximately 58.0 ± 1.0 kJ/mole. The X‐ray structure determination of the compound shows a crown conformation, in line with two‐anomeric effect in N‐C‐O moiety.
The [3 + 2] cycloaddition route to 5‐carbomethoxy‐4h‐1,2,3‐triazolo[1,5‐a][1]benzazepines from baylis‐hillman acetates of 2‐azidobenzaldehydes
Authors: Song Young Seok , Lee Kee‐Jung 
Published: March 2009

Abstractmagnified imageA new, simple synthesis of 5‐carbomethoxy‐4H‐1,2,3‐triazolo[1,5‐a][1]benzazepines from the reaction of several Baylis‐Hillman acetates of 2‐azidobenzaldehydes with alkynide Grignard reagents such as phenylethynyl‐, 1‐propynyl‐ and ethynylmagnesium bromides followed by cycloaddition reaction has been described.
A general synthesis of 8‐hydroxy‐6‐substituted‐1,7‐naphthyridines
Authors: Jiang Xinglong , Chen Guang‐Pei , Prasad Kapa , Repič Oljan , Blacklock Thomas J. 
Published: March 2009

Abstractmagnified imageA general method for the synthesis of 8‐hydroxy‐6‐substituted‐1,7‐naphthyridines is described using acylation of the dianion derived from tert‐butylamide 1, followed by cyclization of the resulting intermediate ketones 2 with ammonium acetate.
Azopyrazolobenzylidene derivatives of 4‐amino‐1,2,4‐triazol‐3‐ones. Synthesis of 4‐{[4‐(3,5‐dimethyl‐1H‐pyrazol‐4‐yl)diazenyl]‐benzylidene}amino‐2‐aryl‐5‐methyl‐3H‐[1,2,4]‐triazol‐3‐ones
Authors: Sunagar Vinay A. , Latthe Prashant R. , Badami Bharati V. 
Published: March 2009

Abstractmagnified imageThe Schiff bases 3a‐h obtained from 4‐amino‐1,2,4‐triazol‐3‐ones 1a‐h when subjected to Japp‐Klingemann reaction yielded the corresponding 3‐{2‐[(2‐aryl‐5‐methyl‐3H‐[1,2,4]‐triazol‐3‐one‐4‐yl)]‐iminophenyl}‐pentane‐2,4‐diones 4a‐h. These diones on cyclisation with N2H4 yielded the title compounds 5a‐h. The energetics of the Keto‐enol tautomers of the diones was calculated by semiemperical calculations using AM1 and PM3 methods. All these compounds were screened for their antimicrobial activity against few microbes and most of them exhibited fungal inhibition more than the reference drugs used.
New routes to steroidal heterocyclic derivatives: Synthesis of biologically active pyrazolyl‐ and isoxazolylpregnene derivatives
Authors: Abdelhamid Abdou O. , Abdelhalim Mervat M. , Elmegeed Gamal A. 
Published: March 2009

Abstractmagnified imagePyrazolyl‐ and isoxazolylpregnene derivatives were synthesized from the appropriate hydrazonoyl chlorides and hydroximoyl chlorides with enaminoprogesterone derivative. The newly synthesized compounds were elucidated by elemental analysis, spectral data and chemical transformation. Some products were tested towards some bacteria and some Fungal‐plant pathogens
Metathetic approach towards macrocyclic bis‐ethers and in sequence use of barbier reaction and RCM for spirocyclic ethers
Authors: Brahma Sulagna , Maity Susama , Ray Jayanta K. 
Published: March 2009

Abstractmagnified imageAn efficient method for the synthesis of novel macrocyclic bis‐ethers from alizarin and also some new spiro ethers from various substituted ketones by the use of Barbier and ring‐closing metathesis (RCM) reactions has been developed.
A novel synthesis of some new benzoyl‐substituted heterocycles from 2‐benzoyl‐3‐phenylpent‐2‐ene‐1,5‐dinitrile
Authors: Abdelrazek Fathy M. , Ghozlan Said A. , Michael Farid A. 
Published: March 2009

Abstractmagnified image2‐Benzoyl‐3‐phenylpent‐2‐ene‐1,5‐dinitrile 1 undergoes bromination with N‐bromosuccinimide (NBS) to afford the bromo derivative 2a. This bromo derivative undergoes reactions with sodium hydrogen sulfide, ethyl thioglycollate, hydroxylamine hydrochloride, hydrazines, cyanoacetamide, cyanacetohydrazide and urea derivatives to afford the thiophene 4, 4H‐thiopyran 6, 4H‐1,2‐oxazine 8, 4H‐pyridazines 10a,b, the pyridine 15, pyrrolo[1,2‐b]pyridazine 17 and the N‐substituted‐pyrrole derivatives 19a‐c respectively.
In situ preparation of rhodium/n‐heterocyclic carbene complexes and use for addition of arylboronic acids to aldehydes
Authors: Kilinçarslan Rafet , Çetinkaya Engin , Çetinkaya Bekir , Yiǧit Murat , Özdemir İsmail 
Published: March 2009

Abstractmagnified imageThe in situ prepared three component system [RhCl(COD)]2/imidazolidinium salts (2, 4) and KOBut catalyses the addition of phenylboronic acid to sterically hindered aldehydes affording the corresponding arylated secondary alcohols in good yields. Four novel 1,3‐dialkylimidazolidinium (2‐4) salts as NHC precursors were synthesized from N,N′‐dialkylethylenediamine.
Syntheses and biological activities of novel triazole compounds
Authors: Zhang Shu‐Sheng , Wan Jun , Li Chun‐Li , Li Xue‐Mei , Qu Bin 
Published: March 2009

Abstractmagnified imageFifteen novel compounds bearing the triazole moiety were synthesized and structurally characterized. The title compounds showed some antimycotic and plant growth regulating activities, especially in the case of 4d and 4c. The latter compound affected also the liver cancer 7402 cell viability.
A facile preparation of selenohydantoins using isoselenocyanate
Authors: Koketsu Mamoru , Takahashi Ayako , Ishihara Hideharu 
Published: March 2009

Abstractmagnified imageReactions of isoselenocyanate with methyl aminoacetate hydrochlorides in the presence of triethylamine afforded selenohydantoins, 2‐selenoxoimidazolidin‐4‐ones, in high yields.
Phenacylsulfonylacetic esters — source for thiadiazoles, triazoles and oxadiazoles
Authors: Padmavathi Venkatapuram , Thriveni Pinnu , Reddy Boreddy Chandra Obula , Mahesh Konda 
Published: March 2009

Abstractmagnified imageA new class of thiadiazoles, triazoles and oxadiazoles were prepared from phenacylsulfonylacetic ester by protecting the carbonyl group by oximation. Deoximation was affected by using β‐cyclodextrin in the presence of an oxidizing agent.
Studies with enamines and azaenamines: A novel efficient route to 6‐amino‐1,4‐dihydropyridazines and their condensed derivatives
Authors: Ghozlan Said A. S. , Abdelhamid Ismail A. , Hassaneen Hamdi M. , Elnagdi Mohamed H. 
Published: March 2009

Abstractmagnified image1‐Arylhydrazonopyruvaldehydes 1 react with α,β‐unsaturated nitriles 2 to yield 6‐amino‐1,4‐dihydropyridazines 4 that are converted into pyridazinones 5 via refluxing in an acetic acid/hydrochloric acid mixture and into the ethylidenemalononitrile derivatives 6 on reflux with malononitrile in ethanolic/piperidine solution.
Synthesis and fluorescence of 2h‐pyrone derivatives for organic light‐emitting diodes (OLED)
Authors: Mizuyama Naoko , Murakami Yuka , Kohra Shinya , Ueda Kazuo , Hiraoka Kyoko , Tominaga Yoshinori , Nagaoka Junko , Takahashi Kojiro , Shigemitsu Yasuhiro 
Published: March 2009

Abstractmagnified image2H‐Pyrone derivatives were synthesized through the reaction of aryl acetyl compounds with ketene dithioacetals in the presence of sodium hydroxide, and they showed very strong fluorescence in the solid state. The light‐emitting region of these 2H‐pyrones is 447‐630 nm in the solid states.
Synthesis of an 4‐oxo‐1,4‐dihydropyridinomethylidene substituted 2‐indolinone
Authors: Lumetzberger Astrid , Löwe Werner , Weber Manuela , Luger Peter 
Published: March 2009

Abstractmagnified imageThe (Z)‐3‐substituted 2‐indolinone 6 was prepared using the aldehydes 4 and 8 unknown up to now and 2‐indolinone.
Regioselective synthesis of some novel pyrazoles, isoxazoles, pyrazolo[3,4‐d]pyridazines and isoxazolo[3,4‐d]pyridazines pendant to benzimidazole
Authors: Shaaban Mohamed R. , Farag Ahmad M. , Saleh Tamer S. , Osman Fayez H. 
Published: March 2009

Abstractmagnified image2‐Acetyl‐1‐methyl‐1H‐benzimidazole reacts with dimethylformamide‐dimethyl‐acetal (DMF‐DMA) to afford the corresponding E‐1‐(1‐methyl‐1H‐benzimidazol‐2‐yl)‐3‐N,N‐dimethylaminoprop‐2‐enone. The latter compound reacts regioselectively with some nitrilimines and nitrile oxides to afford the corresponding pyrazole and isoxazole derivatives, respectively. These reaction products react with hydrazine hydrate to give the novel pyrazolo[3,4‐d]pyridazine and isoxazolo[3,4‐d]pyridazine derivatives, respectively.
New derivatives of dibenzo[b,e][1,4]diazepin‐1‐ones by an efficient synthesis and spectroscopy
Authors: Cortés Eduardo Cortés , Cornejo Ana L. Valencia , de Cortés Olivia García‐Mellado 
Published: March 2009

Abstractmagnified imageAn efficient synthesis of four steps to obtain twelve new derivatives of 3,3‐dimethyl‐2,3,4,5,10,11‐hexahydro‐8‐[(o‐; and p‐methoxy)phenoxy]‐11‐[(o‐; and p‐R)phenyl]‐1H‐dibenzo[b,e][1,4]diazepin‐1‐ones IV, 1‐12 with possible biological and pharmacological activity as anticonvulsant and schizophrenia treatment in the central nervous system (CNS). The final products were obtained by condensation and cyclization between 3‐{4‐[(o‐; and p‐methoxy)phenoxy]‐1,2‐phenylenediamine}‐5,5‐dimethyl‐2‐cyclohexenone with (o‐; and p‐R)benzaldehyde. The structure of all products was corroborated by spectroscopy of ir, 1H‐nmr, 13C‐nmr, with bidimensional experiments and MS in Low and high resolution with Collision‐Induced Dissociation experiments (CID).
Synthesis and spectral determination of new derivatives of 1‐[(p‐substituted)phenyl]‐3a‐[(o‐ and p‐substituted)phenyl]‐5‐chloro‐9‐methylthio‐10,3a‐dihydro‐[1,2,4]‐oxadiazolo[2,3‐b][1,4]benzodiazepines
Authors: Cortés Eduardo , Ramírez Erik Peréz , de Cortés Olivia García‐Mellado 
Published: March 2009

Abstractmagnified imageA new synthesis to obtain eight novel derivatives of 1‐[(p‐substituted)phenyl]‐3a‐[(o‐ and p‐substituted)‐phenyl]‐5‐chloro‐9‐methylthio‐10,3a‐dihydro‐[1,2,4]‐oxadiazolo[2,3‐b][1,4]benzodiazepines with possible biological and pharmacological activity as anxiolytics, hypnotics, anticonvulsants in the central nervous system. The final products were obtained by condensation between 2‐methylthio‐5‐[(o‐; p‐substituted)‐phenyl]‐3H‐7‐chloro‐[1,4]benzodiazepine with benzonitrile oxide generated in situ from benzohydroxamoyl chloride in triethylamine. The structure of all products was corroborated by ir, 1H‐nmr, 13C‐nmr, with experiments bidimensional and ms in low and high resolution.
Synthesis of substituted 3‐pyrrolidinecarbonitriles
Authors: Maruoka Hiroshi , Okabe Fumi , Yamagata Kenji 
Published: March 2009

Abstractmagnified imageCyclopropanes substituted at the same ring carbon by two electron‐withdrawing groups such as alkoxycarbonyl or cyano group react with the primary arylamines via a ring‐opening reaction and ensuing intramolecular cyclization to form substituted pyrrolidines.
An efficient and high yielding protocol for the synthesis of substituted dihydropyrimidin‐2(1h)‐ones and spiro‐fused heterocycles by involving tandem reactions
Authors: Bose D Subhas , Idrees MohD. 
Published: March 2009

Abstractmagnified imageA simple and efficient method has been developed for the synthesis of 3,4‐dihydropyrimidin‐2(1H)‐ones by a one‐pot three component cyclocondensation reaction of alkyl acetoacetates, aldehyde, and urea in the presence of a catalytic amount of the reusable catalyst zinc per chlorate hexahydrate, Zn(ClO4)2.6H2O (10 mol %) the scope of this protocol is utilized for the synthesis of mitotic Kinesin EG5 inhibitor monastrol and new class of fused heterobicyclic compounds in high yields.
Preparation of 4,5‐dihydro‐1,3‐selenazoles by reaction of aromatic primary selenoamides with acetylenedicarboxylate
Authors: Koketsu Mamoru , Ando Hiromune , Sasaki Tomomi , Ishihara Hideharu 
Published: March 2009

Abstractmagnified imageReactions of primary selenoamides with dimethyl acetylenedicarboxylate afforded 2‐aryl‐5‐methoxy‐carbonylmethylene‐4,5‐dihydro‐1,3‐selenazol‐4‐ones in moderate to high yields. Reactions of the primary selenoamides with acetylenedicarboxylic acid gave 2‐aryl‐5‐carboxymethylene‐4‐ethoxy‐4,5‐dihydro‐1,3‐selenazol‐4‐ols in moderate yields.
Convenient synthesis of c2‐symmetric diazepinium salts derived from 1,1′‐binaphthyl‐2,2′‐diamine
Authors: Herrmann Wolfgang A. , Baskakov Denys , Ruhland Klaus 
Published: March 2009

Abstractmagnified imageNew C2‐symmetric atropisomeric diazepinium salts were prepared utilizing Vilsmeier‐Haack activation of corresponding formamide precursors by phosgene solution in toluene. The structures of these substances were verified by X‐ray diffraction.
Synthesis and anti‐HIV activity of n‐(3‐amino‐3,4‐dihydro‐4‐oxopyrimidin‐2‐yl)‐4‐chloro‐2‐mercapto‐5‐methylbenzenesulfonamide derivatives
Authors: Brzozowski Zdzislaw , Sączewski Franciszek 
Published: March 2009

Abstractmagnified imageA series of N‐(3‐amino‐3,4‐dihydro‐4‐oxopyrimidin‐2‐yl)‐4‐chloro‐2‐mercapto‐5‐methylbenzenesulfonamide derivatives 10‐17 have been synthesized as potential anti‐HIV agents. The in vitro anti‐HIV‐1 activity of these compounds has been tested at the national Cancer Institute (Bethesda, MD), and the structure‐activity relationships are discussed. The selected N‐[3‐amino‐3,4‐dihydro‐6‐(tert‐butyl)‐4‐oxothieno[2,3‐e]pyrimidin‐2‐yl]‐4‐chloro‐2‐metcapto‐5‐methylbenzenesulfonamide (14) showed good anti‐HIV‐1 activity with 50% effective concentration (EC50) value of 15 μM and weak cytotoxic effect (IC50 = 106 μM).
Convenient way to 5‐substituted 4‐amino‐2,3‐dihydro‐4H‐1,2,4‐triazole‐3‐thiones
Authors: Smičius Romualdas , Burbuliene Milda Malvina , Jakubkienė Virginija , Udrwėnaitė Emilija , Vainilavičius Povilas 
Published: March 2009

Abstractmagnified imageVarious 4‐amino‐2,3‐dihydro‐4H‐triazoles with aromatic, aliphatic and heterocyclic substituents at the C(5) position were synthesized from corresponding esters and thiocarbohydrazide. This method allows the synthesis these heterocycles in a short time and at reduced expenses.
Fluorescent behavior of 2‐(3,4,5,6‐tetrafluoro‐2‐hydroxyphenyl)imidazo‐[1,2‐a]pyridine in the presence of metal perchlorate
Authors: Tanaka Kiyoshi , Kurushima Tohru , Iwata Satoru , Shimada Syunsuke 
Published: March 2009

Abstractmagnified image2‐(3,4,5,6‐Tetrafluoro‐2‐hydroxyphenyl)imidazo[1,2‐a]pyridine (1) emits long wavelength light around 540 nm both in polar and in nonpolar solvents. Zn2+ perchlorate in acetonitrile causes the intermediate wavelength emission around 430 nm, which is ascribed to the species where the imidazole nitrogen atom and the phenolate oxygen atom bridge Zn2+. In the presence of Hg2+ and Al3+ perchlorates, short wavelength emission around 370 nm is strongly increased and this fluorescent enhancement is attributable not to the coordination of Hg2+ and Al3+ to 1 but to the formation of the salt of perchloric acid of 1.
Novel compounds for the synthesis of cefdinir
Authors: Rao K. V. V. Prasada , Dandala Ramesh , Sivakumaran Meenakshisunderam , Rani Ananta , Naidu A. 
Published: March 2009

Abstractmagnified imagePreparation of two new compounds 2‐mercapto‐5‐methyl‐1,3,4‐thiadiazolyl‐(Z)‐2‐(2‐amino‐4‐thiazolyl)‐2‐trityloxyiminoacetate (14) and 2‐mercapto‐5‐methyl‐1, 3,4‐thiadiazolyl‐ (Z)‐2‐(2‐amino‐4‐thiazolyl)‐2‐acetyloxyiminoacetate (12) and their use in the preparation of 7β‐[(Z)‐2‐(2‐amino‐4‐thiazolyl)‐2‐hydroxyiminoacetamido]‐3‐vinylcephem‐4‐carboxylic acid, also known by the generic name Cefdinir (1) has been accomplished in a single step by coupling with 7‐amino‐3‐vinylcephem‐4‐carboxylic acid (7) with purity of greater than 99% by HPLC.