3-mercapto-1,2,4 benzotriazine (1) was methylated by methyl iodide in the presence of base to afford 1,2-dihydro-3-methyhercapto-1, 2,4 benzotriazine (2). the latter was reacted with hydrazine hydrate to give the corresponding 3-hydrazine derivative (3). compound (3) on condensation with phenacyl bromide gave 3- phenacyl hydrazino l,2,4-benzotriazine (4). ppa cyclization of the ketone (4) yield...

An efficient procedure for 2-aroylbenzofuran preparation from 2-bromophenols, phenacyl bromides and paraformaldehyde is described. The cheap and stable paraformaldehyde served as the carbon source via an in situ formylation reaction.

SYNTHESIS AND EVALUATION OF NOVEL PHENACYL BASED CARBOXAMIDE DERIVATIVES OF PIPERIDINE AS ANTIHYPERTENSIVE AGENTS Shamim Akhtar, Z S Saify, M Arif, Nousheen Mushtaq, Ahsana Dar, Ashfaq Ahmed Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Karachi, Karachi-75270, Pakistan, *Department of Pharmacology, HEJ Research Institute of Chemical Sciences, University of Karachi, ...

1,3-Enynes were easily prepared from coupling between vinyl halides and alkynes or domino coupling of vinyl halides in the presence of copper iodide. It is noteworthy that the double-bond geometry of the vinyl halides was retained during the reaction. This ligand-free protocol is potentially useful and practical.

A palladium-catalyzed difluoromethylthiolation of heteroaryl halides and triflates under mild conditions was described. A vast range of heteroaryl halides such as pyridyl, quinolinyl, benzothiazolyl, thiophenyl, carbazolyl and pyazolyl halides could be difluoromethylthiolated efficiently, thus providing medicinal chemists with new tools for their search of new lead compounds for drug discovery....

The synthesis of 3-methyl-1,4-diphenyl-7-thioxo-4,6,8,9-tetrahydropyrazolo[5,4-b] pyrimidino[5,4-e]pyridine-5-one (6) was achieved by two different one-pot multi-component synthesis (one-pot three-component and one-pot four component synthesis). Mono and dialkylation of 6 under different conditions gave compounds 7-11. The hydrazine 12 produced from reaction of 9 with N₂H₄ was subjected to reac...

2-Amino-5-(2-aryl-2H-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles 2-4 have been synthesized by the reaction of 2-aryl-2H-1,2,3-triazole-4-carboxylic acids 1 with thiosemicarbazide. Their reaction with phenacyl (p-substituted phenacyl) bromides led to formation of the respective 6-aryl-2-(2-aryl-2H-1,2,3-triazol-4-yl)imidazo[2,1-b]-1,3,4-thiadiazoles 5. Reactivity of the latter fused ring towards reac...