A simple, convenient, and efficient one‐pot synthesis of fully substituted pyrimidines was developed by cyclocondensation of α‐oxo ketene dithioacetals with amidine in the presence of potassium carbonate in good yield. Structures of all the newly synthesized compounds were elucidated by elemental analysis and spectral analysis. All the newly synthesized compounds are tested toward different microorganisms.

A convenient synthesis of substituted 1,2,4-triazolo[1,5-a]pyrimidine was carried out by the reaction of various ketene dithioacetals with 5-amino 1,2,4-triazole in methanol in presence of sodium methoxide. The newly synthesized compound were characterized by 1H NMR, 13 C NMR, IR, MS, elemental analysis and screened for their antimicrobial activity against various strains of bacteria and fungi.

A development of Groebke‐Blackburn‐Bienaymé (GBB) reaction was shown by the application of Etidronic acid as a green catalyst. A number of 1H‐imidazo[1,2‐b]pyrazoles derivatives were prepared via multicomponent GBB reaction in one pot sequential steps by the condensation of 5‐amino‐1H‐pyrazole, aldehyde and isonitrile. Here, we have demonstrated the development of GBB protocol by the utility of Etidronic acid in milder reaction medium to modify and simplify the existing synthetic strategies that removes hazardous acids, toxic solvents and drastic conditions with sustainable product yields and purity.

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ABSTRACT.A simple and efficient approach for the synthesis of thiophenyl thiazole based triazolo [4,3-a]quinoxaline derivatives is described. In this methodology, 3-hydrazinyl-N-(4-(thiophen-2-yl)thiazol-2-yl)quinoxalin-2-amine derivatives treated with various aromatic aldehyde to form Schiff base which on treatment with iodobenzene diacetate in dichloromethane at room temperature to furnish title compounds. The synthesized compounds were characterized by 1 H NMR, 13C NMR, FT-IR, elemental analysis, and mass spectral data. INTRODUCTION1,2,4-triazoles are very interesting targets for medicinal and pharmaceutical applications. The recent literatures are enriched with progressive findings about the synthesis and pharmacological action of fused heterocyclic systems. The structural diversity and biological importance of nitrogen containing heterocyclic systems have made them attractive synthetic targets over many years and they are found in various natural products [1]. Quinoxalines are an important class of nitrogen containing heterocycles with a variety of biological activities. In particular quinoxaline scaffolds were found as a core unit in a number of biologically active compounds. These include anticancer [2,3], antibacterial [4], antiviral [5], anti-inflammatory [6], anti HIV [7,8] and antihelmintic activities [9]. Quinoxaline derivatives are also used in the development of novel organic dyes and organic semiconductors. Triazolo [4,3-a]quinoxaline [10] have been reported to possess antiviral, and antimicrobial activities. Many other triazolo quinoxaline derivatives have been reported [11][12][13] to possess other types of biological properties. Thus, triazolo quinoxaline derivatives continue to attract much attention as these molecules are of potential biological interest.For synthesis purpose, triazolo quinoxalines can be achieved in several ways. Reaction of 1-(2-chloroquinoxalin-3-yl)hydrazine and triethyl orthoformate gave triazolo quinoxaline [14]. Reactions of benzyl bromide or benzyl cinnamate with N-(benzotriazol-1-ylmethyl)arylimidoyl chlorides in the presence of t-BuOK occur with opening of the benzotriazole ring affording 1,2,4-triazolo[1,5-a]quinoxalines [15]. Reaction of N'-(1,2-dihydro-2-oxoquinoxalin-3-yl)benzohydrazide and HMPA formed triazolo quinoxaline [16]. By heating 2-hydrazino 3-phenylquinoxaline with phenyl-1,3-butanedione produced triazolo quinoxaline [17]. N-(2-chloro-4a,8a-dihydroquinoline3yl-methyl)-N-3-chloro-quinoxalin-2yl) hydrazones cyclised by iodobenzene diacetate under microwave irradiation technique to furnish the respective quinolinyl-1, 2, 4-s-triazolo [4,3-a]quinoxalines [18]. Here we report an efficient and clean synthesis of thiophene thiazole depended novel triazolo quinoxaline derivatives by cyclisation reaction. The constitutions of all the products were confirmed using 1 H NMR, 13C NMR, FTIR, and elemental analysis. EXPERIMENTALRequired all reagents were obtained commercially. Solvents were purified and dried before being used. All melting points were taken in open ...