Factor Xa and thrombin, two critical pro-coagulant enzymes of the clotting cascade, are the primary target of current anticoagulation research that aims to develop potent, orally bioavailable, synthetic small-molecule inhibitors. To determine structural features that might play important roles in factor Xa and thrombin recognition and oral bioavailability, quantitative structure-activity and st...

A series of 6,8-diiodocoumarin-3-N-carboxamides (4-11) were prepared. Treatment of ethyl 6,8-diiodocoumarin-3-carboxylate (1) with ethyl cyanoacetate/NH(4)OAc gave ethyl 2-(3-carbamoyl-6,8-diiodocoumarin-4-yl)-2-cyanoacetate (12) and 2-amino-4-hydroxy-7,9-diiodocoumarino[3,4-c]pyridine-1-carbonitrile (13), and treatment with acetone in the presence of NH(4)OAc or methylamine gave the ethyl 4-ox...

A new generation of chroman bearing heterocyclic five membered ring such as 1,2,4-triazoles and thiazolidinones was designed and synthesized. New chroman based nucleus 5-(6-fluorochroman-2-yl)-4-aryl-4H-1,2,4-triazole-3-thiol and 6-fluorochroman-N-(4-oxo-2-arylthiazolidinin-3-yl) chroman-2-carboxamides were synthesized. Aryl triazole compounds 4a-4j were synthesized from 6-fluorochroman-2-carbo...

To explore the anticancer activity of 2, 4, 5, 6-substituted pyrimidines, several ethyl 2-(1-aminocyclobutyl)-5-(benzoyloxy)-6-hydroxy-pyrimidine-4-carboxylate derivatives associated with the different substituted aromatic/aliphatic carboxamides and sulfonamides were synthesized. Different groups and position on phenyl ring attached to the carboxamide and sulfonamide of the pyrimidine led to tw...

An achiral Cp*Ir( iii )/chiral carboxylic acid-catalysed enantioselective C–H alkylation of ferrocene carboxamides with diazomalonates was achieved, providing planar chiral alkylated ferrocenes in up to 94 : 6 er.

An efficient method for the synthesis of N-aryl monosubstituted carboxamides via the Pd-catalyzed carbonylation of alkenes with CO and amines is described. Mechanistic insights for this highly selective reaction are provided.

Novel azepino[3,4-b]indol-1-ones were synthesized from alkyne-substituted indole-2-carboxamides by catalytic intramolecular cyclization in the presence of PtCl(2). The scope and limitations of this straightforward protocol are reported.