bluuebunny/crossref_metadata_2025_split huggingface dataset:
N‐alkyl‐4‐chloro‐1H‐benzo[c][1,2]thiazine‐3‐carbaldehyde‐2,2‐dioxides—New functional benzothiazine derivatives
Authors: Volovenko Yulian , Volovnenko Tatyana , Popov Kirill 
Published: March 2009

Abstractmagnified imageA synthesis of N‐alkyl‐4‐chloro‐1H‐benzo[c][1,2]thiazine‐3‐carbaldehyde‐2,2‐dioxides is described. Reactivity of new β‐chloroaldehydes is investigated, a number of novel benzo[c][1,2]thiazine derivatives are synthesized and characterized using 1H, 13C‐NMR, MS and elemental analysis.
A new method for the synthesis of bicyclic pyran acetals
Authors: Ergunes Duygu , Kumbaraci Volkan , Karliga Bekir , Talinli Naciye 
Published: March 2009

Abstractmagnified imagecis‐Fused bicyclic acetals were obtained from the unusual cyclization reaction between diols and dihydropyran. Furothiopyran, substituted pyranopyrans, and pyranooxepine and pyranobenzoxepine compounds were obtained with high diastereoselectivity and cis‐diastereomers were obtained in high yields.
A highly efficient method for solvent‐free synthesis of bis(arylmethylidene)piperidinones
Authors: Saeed Abaee M. , Mojtahedi Mohammad M. , Sharifi Roholah , MehdiZahedi M. 
Published: March 2009

Abstractmagnified imageA remarkably efficient double crossed aldol condensation of piperidin‐4‐one with various aromatic aldehydes is described at room temperature in the presence of diethylamine and lithium perchlorate under solvent‐free conditions. Excellent yields of 3,5‐bis(arylmethylidene)piperidinones are achieved in a facile one‐pot general procedure. Structure of the products is determined by spectroscopic methods and elemental analysis.
Novel approach for the conversion of natural Δ3 cephalosporin derivatives into corresponding Δ2 cephalosporin derivatives
Authors: Rao Korrapati. V. V. Prasada , Dandala Ramesh , Handa Vija Y. K. , Kamat Anand. G. , Rao Inti. V. Subramanyeswara , Rani Ananta , Naidu Andra 
Published: March 2009

Abstractmagnified imageA simple one pot synthetic method for the isomerization of cephem double bond from the natural 3‐position to 2‐cephem positions is affected by silylation. Thus cephalosporin acids are treated with Ntrimethylsilylacetamide (MSA) or N,O‐bis(trimethylsilyl)acetamide (BSA) and the resulting silyl esters are treated with triethylamine at ambient temperature in the same pot to afford Δ2‐cephalosporins, which are potentially related compounds in cephalosporin antibacterial compounds.
Regioselective three‐component synthesis of novel indeno[1,2‐b]‐pyrazolo[4,3‐e]pyridines‐fused derivatives of 4‐azafluorenone alkaloid
Authors: Quiroga Jairo , Cobo Débora , Insuasty Braulio , Abonía Rodrigo , Cruz Silvia , Nogueras Manuel , Cobo Justo 
Published: March 2009

Abstractmagnified imageNew fused indeno[1,2‐b]pyridine derivatives have been prepared in a multicomponent reaction from benzaldehydes, indanedione and the appropriate aminoheteroaryl compound. The simple methodology permitted the syntheses of a series of indeno[1,2‐b]pyrazolo[4,3‐e]pyridines 4 from 5‐aminopyrazol 1 and modulated by the corresponding benzaldehyde 2.
Benzobis(pyrrolopyrimidopiridazines): Molecular structure and properties of the first π‐electronic analogues of dibenzo[a,o]picene
Authors: Serdyuk Olga V. , Gulevskaya Anna V. , Pozharskii Alexander F. , Avakyan Vadim E. 
Published: March 2009

Abstractmagnified imageMolecular structure, aromaticity and some spectral properties of benzobis(pyrrolopyrimidopiridazines) 2 that are the first π‐electronic analogues of the still unknown dibenzo[a,o]picene are discussed.
Synthesis and photochemical properties of trans‐2‐(2‐aryl‐ or heteroarylvinyl)‐4,5‐dichloropyridazin‐3(2H)‐ones
Authors: Yim Heung‐Seop , Kim Mi‐Ra , Sung Gi‐Hyeon , Chung Hyun‐A , Lee Jin‐Kook , Lee Sang‐Gyeong , Yoon Yong‐Jin 
Published: March 2009

Abstractmagnified imagetrans‐2‐(2‐Aryl‐ or heteroarylvinyl)‐4,5‐dichloropyridazin‐3(2H)‐ones 3 were synthesized from 4,5‐dichloropyridazin‐3(2H)‐one via 2 step. The photochemical behavior of 3 in THF, methylene chloride, acetonitrile and methanol is dependent on the kind of aryl or heterocyclic ring and the solvent polarity
Preparation and crystal structures of two 3‐anthracenyl isoxazolyl sulfonamides
Authors: Li Chun , Twamley Brendan , Natale Nicholas R. 
Published: March 2009

Abstractmagnified imageLateral metalation and oxidation of 3‐(9′‐anthryl)‐isoxazoles (1), using Davis' oxaziridine (6), produced the desired hydroxylation (2), along with sulfonamide adduct (3), and in the case of the use of butyl lithium as base, butyl addition products (4) and (5). Structures of isoxazole sulfonamides (3a) and (5a), were obtained as the SR/RS‐diastereomer, however, studies indicate that this is a consequence of the crystallization process. Metalation studies with isoxazole (8) demonstrate that hydroxylation (9), can be carried out cleanly, minimizing formation of (10), using camphorsulfonyloxaziridine (7) as an electrophile.
Reaction of 6‐aryl‐ or styryl‐4‐methylsulfanyl‐2‐oxo‐2H‐pyrans with active methylene compounds and fluorescence properties of the products
Authors: Mizuyama Naoko , Murakami Yuka , Nakatani Takatoshi , Kuronita Keiko , Kohra Shinya , Ueda Kazuo , Hiraoka Kyoko , Tominaga Yoshinori 
Published: March 2009

Abstractmagnified imageNew 2‐pyrone derivatives, dialkyl 3‐cyano‐6‐phenyl‐2‐oxo‐2H‐pyran‐4‐ylmalonates and alkyl 3‐cyano‐6‐phenyl‐2‐oxo‐2H‐pyran‐4‐ylacetates, which were easily prepared by the reaction of 6‐aryl‐4‐methyl‐sulfanyl‐2‐oxo‐2H‐pyran‐3‐carbonitriles with active methylene compounds in the presence of potassium carbonate, show fluorescence emission radiation. The light‐emitting region of dimethyl 3‐cyano‐6‐(4‐N,N‐dimethylamino)styryl‐2‐oxo‐2H‐pyran‐4‐ylmalonate (7h) was 620 nm in dichloromethane, making this compound a typical red fluorescent compound. Methyl 8‐hydroxy‐6‐methyl‐1‐oxo‐3‐phenyl‐1H‐pyrano‐[3,4‐c]pyridine‐5‐carboxylate deriv‐atives also showed fluorescence in the solid state. This is the first example of fluorescence in fused 2‐pyrone derivatives.
Dicyanomethylene compounds and heterocyclization of acylthiosemicarbazides
Authors: Hassan Alaa A. , Mourad Aboul‐Fetouh E. , Abou‐Zeid Ashraf H. 
Published: March 2009

Abstractmagnified image(1,3‐Dioxo‐2,3‐dihydro‐1H‐inden‐2‐ylidene)propanedinitrile (1, in ethyl acetate solution), 3‐(dicyano‐methylene)‐2‐indolone (2, in ethanol/piperidine solution) and 7,7′,8,8′‐tetracyanoquinodimethane (3, in pyridine solution) act on substituted acylthiosemicarbazides 4a‐d, forming the derivatives of oxoindeno‐pyrrolylidenehydrazide (5a‐d and 7a‐d), thiazoloindolylidenehydrazide (12a‐d), pyrroloindolylidene‐hydrazide (13a‐d) and spiro[pyrrolylidene‐4,1′(cyclohexa‐2′,5′‐dienylidene)]propanedinitrile (18a‐d). Rationales for these conversiones involving the nucleophilic addition on dicyanomethylene carbon atom are presented.
An efficient and facile microwave‐assisted synthesis of benzo[b][4,7]phenanthroline derivatives in water
Authors: Shi Feng , Zhou Dianxiang , Li Chunmei , Shao Qingqing , Cao Longji , Tu Shujiang 
Published: March 2009

Abstractmagnified imageA series of benzo[b][4,7]phenanthroline derivatives were synthesized via a three‐component reaction of aromatic aldehydes, 6‐aminoquinoline and either 1,3‐cyclohexanedione or dimedone in water under microwave irradiation without use of any catalyst. This method has the advantages of short reaction time, high yields, low cost and environmental friendliness as well as easy operation.
Synthesis of a peptide nucleic acid with a novel 1‐methyl‐6‐mercaptopurine base
Authors: Aboul‐Fadl Tarek , Rajeev Gopalan , Broom Arthur D. 
Published: March 2009

Abstractmagnified imageA novel peptide nucleic acid (PNA) monomer 16 containing a novel 1‐methyl‐6‐mercaptopurine base was synthesized by coupling the in situ generated acid chloride of (1‐methyl‐6‐mercaptopurin‐9‐yl)acetic acid (6) into an L‐lysine backbone (13) using 10% CCl4 in pyridine and Ph3P. Compound 6 was synthesized from 6‐mercapto‐1‐methylpurine and ethylbromoacetate in the presence of NaH followed by alkaline hydrolysis and subsequent neutralization with a cation exchange resin. The L‐lysine backbone (13) was obtained by the reaction of Nϵ‐CBZ‐L‐lysine allyl ester with Boc‐aminoactaldehyde in the presence of NaBH3CN under reductive amination conditions. Oligomerization of the monomer 16 to PNA analogues was achieved using BOC‐BHA‐PEG‐PS resin as a solid support and the in situ generated acid chloride of 16 by 10% CCl4 in DCM in the presence of Ph3P.
One‐pot synthesis of N2‐aminoprotected 6‐substituted and cycloalka[d] 4‐trifluoromethyl‐2‐acetylaminopyrimidines
Authors: Bonacorso Helio G. , Ferla Adriana , Cechinel Cleber A. , Zanatta Nilo , Martins Marcos A. P. 
Published: March 2009

Abstractmagnified imageThe one‐pot synthesis of a novel series of amino‐protected 6‐alkyl‐, 6‐aryl‐, 6‐heteroaryl‐ and 5,6‐fused‐cycloalkane 4‐trifluoromethyl‐2‐acetylaminopyrimidines, where alkyl = Me; aryl = Ph, 4‐CH3Ph, 4‐FPh, 4‐ClPh, 4‐BrPh, 4‐OCH3Ph, 4‐NO2Ph, 4,4′‐biphenyl, 1‐naphthyl; heteroaryl = 2‐thienyl, 2‐furyl and cycloalkyl = c‐C6H4, c‐C7H5 from the reaction of substituted 4‐methoxy‐1,1,1‐trifluoroalk‐3‐en‐2‐ones with 1‐acetylguanidine in acetonitrile or propan‐2‐ol as solvent, is reported. The acetylamino group of 2‐acetylaminopyrimidines was hydrolyzed under three different conditions to afford the corresponding free 2‐aminopyrimidines.
A short and convenient synthesis and evaluation of the antiinfective properties of indoloquinoline alkaloids: 10H‐Indolo[3,2‐b]quinoline and 7H‐indolo[2,3‐c]quinolines
Authors: Etukala Jagan R. , Kumar E. V. K. Suresh , Ablordeppey Seth Y. 
Published: March 2009

Abstractmagnified image10H‐Indolo[3,2‐b]quinoline and 7H‐indolo[2,3‐c]quinoline have been synthesized in two steps using a modified approach to our previous reported method. Starting from commercially available 3‐aminoquinoline and phenylboronic acid, the first step involved a copper acetate‐catalyzed coupling reaction and the second utilized a palladium acetate‐catalyzed intramolecular arylation reaction in the presence of trifluoroacetic acid as solvent. The anti‐infective activity of a selected number of the compounds was also evaluated.
Conventional and microwave irradiation assisted synthesis of new 1,2,4‐triazepine‐3‐thiones
Authors: Aly Ashraf A. , Hassan Alaa A , El‐Sheref Essmat M. , Mohamed Mamdouh A. , Brown Alan B. 
Published: March 2009

Abstractmagnified imageNew 1,2,4‐triazepine‐3‐thiones have been obtained during the respective reactions of N‐substituted‐hydrazino carbothioamides with dimethyl acetylenedicarboxylate and dibenzoyl acetylene under prolonged reflux in acetic acid and/or DMF. However, the reaction of the starting materials in DMF under microwave irradiation afforded the same products in higher yields within a few minutes.
An efficient synthesis of 4‐alkoxy‐5,6‐dihydro‐furo(and ‐thieno)[2,3‐d]pyrimidines using zinc chloride/triethylamine reagent system
Authors: Maruoka Hiroshi , Okabe Fumi , Yamagata Kenji 
Published: March 2009

Abstractmagnified imageThe one‐pot synthesis of 4‐alkoxy‐5,6‐dihydro‐furo(and ‐thieno)[2,3‐d]pyrimidines is described. The reactions of 2‐benzamido‐4,5‐dihydro‐3‐furan(and ‐3‐thiophene)carbonitriles 1a‐d and 2a‐c with ethanol and/or methanol in the presence of zinc chloride and triethylamine gave the corresponding 4‐alkoxy‐5,6‐dihydro‐furo(and ‐thieno)[2,3‐d]pyrimidines 3a‐d, 4a‐d, 5a‐c and 6a‐c.
Microwave‐promoted oxidation of 1,3,5‐trisubstituted 4,5‐dihydro‐1H‐pyrazoles byin‐situgeneration of NO+and NO respectively from sodium nitrite and sodium nitrate in acetic acid
Authors: Azarifar Davood , Maleki Behrooz , Sahraei Mahta 
Published: March 2009

Abstractmagnified imageMicrowave‐assisted aromatization of 1,3,5‐trisubstituted 4,5‐dihydro‐1H‐pyrazoles byin‐situgeneration of NO+and NO2+respectively from sodium nitrite and sodium nitrate in acetic acid has been carried out efficiently under mild reaction conditions in good to excellent yields.
Novel C‐acylated triazole derivatives of ravuconazole, an azole antifungal agent
Authors: Kim Oak , Zhang Yunhui , Wichtowski John , Huang Stella , Fung‐Tomc Joan , Bronson Joanne , Ueda Yasutsugu 
Published: March 2009

Abstractmagnified imageNovel C‐acylated triazoles were synthesized from ravuconazole via bicyclic triazole lactone. The synthesis and antifungal activity of these C‐acylated derivatives are described.
Synthesis of 4H‐indeno[1,2‐b]thiophenes, 8H‐indeno[2,1‐b]‐thiophenes and 8H‐indeno[2,1‐b]furans having acrylic acid unit
Authors: Jeon Ki Joon , Lee Kee‐Jung 
Published: March 2009

Abstractmagnified imageTreatment of methyl propiolate and 2‐(thiophen‐2‐yl)benzaldehyde, 2‐(thiophen‐3‐yl)benzaldehyde or 2‐(furan‐3‐yl)benzaldehyde with tetrabutylammonium iodide/zirconium (IV) chloride or treatment of methyl acrylate and the same aldehydes with 1,4‐diazabicyclo[2,2,2]octane and triethanolamine induce an aldol‐type reaction to furnish Baylis‐Hillman adducts β‐iodo‐α‐(hydroxymethyl)acrylates or α‐(hydroxy‐methyl)acrylates, respectively. These can be used for the preparation of indenothiophenes and indenofurans having acrylic acid unit by intramolecular Friedel‐Crafts reaction with sulfuric acid in tetrachloromethane.
Michael addition of dimedone with α,β‐unsaturated ketones: Synthesis of quinoline and chromene derivatives
Authors: Kendre Dhananjay B. , Toche Raghunath B. , Jachak Madhukar N. 
Published: March 2009

Abstractmagnified imageA series of quinoline and chromene derivatives has been synthesized by Michael addition of dimedone 1 with 2‐aroyl‐3‐arylacrylonitrile 2 and study of absorption and fluorescence maxima of quinolines.
An Efficient synthesis of pyrimido[4,5‐b]quinoline and indeno[2′,1′:5,6]pyrido[2,3‐d]pyrimidine derivatives via multicomponent reactions in ionic liquid
Authors: Ji Shun‐Jun , Ni Sai‐Nan , Yang Fang , Shi Jing‐Wen , Dou Guo‐Lan , Li Xiao‐Yue , Wang Xiang‐Shan , Shi Da‐Qing 
Published: March 2009

Abstractmagnified imageA series of pyrimido[4,5‐b]quinoline and indeno[2′,1′:5,6]pyrido[2,3‐d]pyrimidine derivatives were synthesized via the three‐component reaction of an aldehyde, 6‐aminopyrimidine‐2,4‐dione and 5,5‐dimethyl‐1,3‐cyclohexanedione or 1,3‐indanedione in ionic liquid 1‐n‐butyl‐3‐methylimidazolium bromide ([bmim]Br). This protocol has the advantages of easier work‐up, milder reaction conditions, high yields and an environmentally benign procedure compared with other methods.
A novel synthesis of EGFR‐tyrosine‐kinase inhibitors with 4‐(indol‐3‐yl)quinazoline structure
Authors: Lüth Anja , Löwe Werner 
Published: March 2009

Abstractmagnified imageThe epidermal growth factor (EGF) family of membrane receptors has been identified as a key element in the complex signaling network that is utilized by various classes of cell‐surface receptors. A new synthetic pathway of 4‐(indol‐3‐yl)quinazolines 15 and 16 is described using cross coupling reactions with quinazoline‐ and indole moieties. The synthesized compound 15 is a new dual and high potent EGFR‐ and HER‐2‐tyrosine kinase inhibitor with excellent cytotoxic properties at different cell lines. Furthermore this substance class shows remarkably strong fluorescence.
N‐alkylated 3,5‐bis(arylidene)‐4‐piperidones. Synthetic approaches, X‐ray structure and anticancer activity
Authors: Makarov Michael V. , Odinets Irina L. , Lyssenko Konstantin A. , Rybalkina Ekaterina Yu. , Kosilkin Ilya V. , Antipin Mikhail Yu. , Timofeeva Tatiana V. 
Published: March 2009

Abstractmagnified imageIn a search for cytotoxic fluorescent materials a series of N‐alkylated and N,N‐dialkylated 3,5‐bis(arylidene)piperidones was synthesized. Alkylation of 3,5‐bis(arylidene)‐4‐piperidone afforded quaternary salts only while condensation of N‐alkyl‐4‐piperidones with substituted benzaldehydes was a convenient route to the corresponding N‐alkylated compounds. Compounds and their pharmaceutically acceptable salts demonstrated high activity against resistant human lung carcinoma cell line A549 with IC50 values in the range of 0.3‐6.5 μM.
Synthetic and spectroscopic studies of some new 2‐[1‐aryl‐4{4‐methoxyphenyl}‐6‐thioxo‐1,6‐dihydro‐1,3,5‐triazinyl]amino/hydrazonothiazolidin‐4‐ones
Authors: Roychowdhuary P. K. , Mehrotra Sangeeta , Srivastava Sugandh , Upadhay K. K. , Mishra Rakesh K. , Kumar Ajit , Upadhyay Shalini 
Published: March 2009

Abstractmagnified imageA series of 4‐thiazolidinones having triazinethione moieties have been synthesized by the systematic chemical modification of S‐benzylmercapto‐1‐aryl‐4‐(4‐methoxyphenyl)‐1,6‐dihydro‐1,3,5‐triazine‐6‐thione.
Synthesis and in vitro antiproliferative activity of new substituted benzo[3′,2′:5,6]thiopyrano[4,3‐d]pyrimidines
Authors: Marini Anna Maria , Da Settimo Federico , Salerno Silvia , La Motta Concettina , Simorini Francesca , Taliani Sabrina , Bertini Daniele , Gia Ornella , Dalla Via Lisa 
Published: March 2009

Abstractmagnified imageThe synthesis of new planar benzo[3′,2′:5,6]thiopyrano[4,3‐d]pyrimidine derivatives, carrying different side groups in the 2 position, is described. The novel substituted pyrimidines were obtained by reaction of the key intermediate 3‐dimethylamino methylen‐7‐methoxy‐2,3‐dihydrobenzo[3′,2′:5,6]thiopyran‐4(4H)‐one, characterized by a reactive group adjacent to the CO function, with the suitable binucleophile amidines in a basic medium. All the new compounds were evaluated for the antiproliferative ability by an in vitro assay on two human tumour cell lines (HL‐60 and HeLa), and the 2‐phenyl substituted derivative showed the capacity to inhibit cell growth on HL‐60. Linear flow dichroism measurements indicated the inability to form a molecular complex with DNA.
Full Characterization and some reactions of 1‐(2‐adamantyl)‐3‐(1‐adamantyl)aziridin‐2‐one
Authors: Lengyel István , Taldone Tony , Lyons Theresa , Cesare Victor 
Published: March 2009

Abstractmagnified imageWe found that 1‐(2‐adamantyl)‐3‐tert‐butylaziridin‐2‐one (5a) is unstable. It slowly decomposes at room temperature, although detectable by IR spectroscopy (1840 cm−1 band in CCl4). On the other hand, a closely related analogue, 1‐(2‐adamantyl)‐3‐(1‐adamantyl)aziridin‐2‐one (5b), is very stable, in concurrence with an earlier report [1]. We fully characterized aziridinone 5b, identified its thermal decomposition products (7 and 8) and reacted it with two aprotic ionic (tBuO− and HO−) and one protic non‐ionic nucleophile (benzylamine). All three products (9b, 10, and 11) result from exclusive cleavage of the lactam (1‐2) bond.
Synthesis of 5‐mono‐ and 5,7‐diamino‐pyrido[2,3‐d]‐pyrimidinediones with potential biological activity by regioselective amination
Authors: Van Tinh Dang , Stadlbauer Wolfgang 
Published: March 2009

Abstractmagnified image5‐Alkyl‐/arylamino‐ and 5,7‐dialkyl/arylamino‐pyrido[2,3‐d]pyrimidine‐2,4‐diones (4,5, 7‐9) were prepared from the corresponding 5,7‐dichloro‐pyrido[2,3‐d]pyrimidine‐2,4‐diones 2 with aliphatic and aromatic amines 3 and 6 in a regioselective reaction. The 7‐monoazides 10, obtained by azidation of 5‐amino‐7‐chloro derivatives 4, were converted to iminophosphoranes by reaction with triphenyl‐phosphane via Staudinger reaction. Hydrolysis with aqueous acetic acid produced in one step 7‐unsubstituted‐amino‐pyrido[2,3‐d]pyrimidine‐2,4‐diones 12. In a similar amination reaction, 5‐chloropyrido[2,3‐d]pyrimidine‐2,4,7‐triones 13 were aminated and formylated to 5‐alkyl/arylamino‐6‐formyl derivatives 14‐16 in a combined one‐step‐reaction with bulky arylamines or alkylamines in the presence of dimethylformamide.
A highly efficient microwave‐assisted synthesis of chromeno‐[3,4‐b][4,7]phenanthroline derivatives through multicomponent reactions in water
Authors: Zhuang Qiya , Zhou Dianxiang , Tu Shujiang , Li Chunmei , Cao Longji , Shao Qingqing 
Published: March 2009

Abstractmagnified imageA short and simple synthesis of chromeno[3,4‐b][4,7]phenanthroline derivatives was accomplished by three‐component reactions involving an aromatic aldehyde, 6‐aminoquinoline and 4‐hydroxycoumarin in water, under microwave irradiation without use of any catalyst. This protocol has the advantages of short reaction time, high yields, low cost and being environmental‐friendly as well as easy operation.
Synthesis of substituted amino‐cycloalkyl[b]thieno‐[3,2‐e]pyridines
Authors: Seck Pierre , Thomae David , Kirsch Gilbert 
Published: March 2009

Abstractmagnified imageAn efficient two respectively three steps procedure for the synthesis of cycloalkyl[b]thieno[3,2‐e]‐pyridine amines was developed and in general good to very good yields were obtained.
Preparation of analogues of efaroxan and KU14R as potential imidazoline receptor subtype 3 ligands
Authors: Farn Richard D. , Ramsden Christopher A. , Morgan Noel G. 
Published: March 2009

Abstractmagnified imageThe preparation and characterization of new analogues of the imidazoline insulin secretagogue efaroxan 1 are described. These include 1,2,4‐triazole, 1,3,4‐oxadiazole, pyrimidine, 1,4,5,6‐tetrahydropyrimidine and 1,2‐dihydro‐1,2,4,5‐tetrazine analogues. Bromination of 2,3‐dihydro‐2‐ethylbenzo[b]furan‐2‐carbonitrile 19 gives the 3,3‐dibromo analogue 28, which is readily hydrolysed to the corresponding ketone 29. Reduction of this ketone gives the alcohol 31 as a mixture of diastereoisomers that is converted to the fluoride 32 using diethylaminosulfur trifluoride.
A convenient and practical synthesis of olmesartan medoxomil methyl ether
Authors: Pati Hari Narayan , Lahiri Saswata , Sabbam Ramesh Kumar , Vangala Vijaya Bhaskar , Ramalingam Boobalan , Hiriyanna Salmara Ganeshbhat , Bose Prosenjit 
Published: March 2009

Abstractmagnified imageSynthesis of Olmesartan medoxomil methyl ether (2), a potential impurity of Olmesartan medoxomil (1), an angiotensin II receptor blockers is reported for the first time.
A facile synthesis and heteroannulation of thiazolopyrimidine and related heterocyclic systems
Authors: Aly A. A. 
Published: March 2009

Abstractmagnified imageReaction of pyrimidinylacetic acid 2 with different electrophilic and nucleophilic reagents gave annulated pyrimidine derivatives 3‐11, respectively. Compound 3 was transformed to pyrimidinylacetyl azide 12, which upon heterocyclization with active methylene compounds, acidic and basic reagents furnished functionally substituted heteroaromatic compounds 13‐21, respectively. The antimicrobial activity of some synthesized compounds was investigated. The structures of the synthesized derivatives were elucidated by elemental and spectral analyses.
Studies with S‐alkylpyrimidine: New route for the synthesis derivatives of isoxazol, pyrazolo[1,5‐a]pyrimidine, pyridazine, pyridine, thieno[2,3‐b]pyridine and thiophene of potential anti‐HIV
Authors: Al‐Omran Fatima A. , El‐Khair Adel A. 
Published: March 2009

Abstractmagnified imageDerivatives of thiophene, thieno[2,3‐b]pyridine, pyridine, isoxazol, pyrazolo[1,5‐a]pyridine, pyridazine linked with s‐pyrimidine derivative have been synthesized and tested for antimicrobial and antifungal activities. The structure of the newly synthesized compounds have been established on the basis of their analytical and spectral data.
Simple microwave‐assisted ligand‐free suzuki cross‐coupling: Functionalization of halo‐pyrimidine moieties
Authors: Colombo Matteo , Giglio Marco , Peretto Ilaria 
Published: March 2009

Abstractmagnified imageAn advantageous ligand‐free protocol for Suzuki couplings is described. The synthetic procedure entails microwave irradiation for the reduction of the reaction times and the use of silica cartridges for the purification. Dihalo‐pyrimidine structures, interesting scaffolds in medicinal chemistry, were chosen as test compounds.