AN EFFICIENT, GREENER MICROWAVE ASSISTED MULTI-COMPONENT ONE POT SYNTHESIS OF [1, 3, 4] THIADIAZIN-2-YL-THIAZOLIDIN-4-ONES

This work involves synthesis of [1, 3, 4] thiadiazin-2-ylamine 3(a-c) derivatives from various substituted acetophenone derivatives 1(a-c), and thiosemicarbazide 2 mixed in ethanol and irradiation with microwaves which were directly used for next step. [1, 3, 4]Thiadiazin-2-yl)-thiazolidin-4-one 6(a-f) were synthesized in the second step from substituted-6H-[1, 3, 4] thiadiazin-2-ylamine 3(a-c), substituted aromatic aldehyde 4(a-b), and thioglycolic acid mixed in ethanol. After completion of the reaction products obtained 6(a-f) was confirmed by spectroscopy. Library of such [1, 3, 4] thiadiazin-2-ylamine and [1, 3, 4] thiadiazin-2-yl)-thiazolidin-4-one derivatives has been generated and the structures were subjected to PASS for their probabilities of being biologically active. Biological prediction study of the library was done to find out most active molecules. Computer programme PASS predicted for three activities with top probability for compound 3(a-c) as- 1. Mucomembranous protector, 2. Arylacetonitrilase inhibitor, 3. Macrophage elastase inhibitor. Similarly Compounds 6(a-f) were predicted for two activities with top probability as- 1. CC chemokine-4-receptor antagonist, 2. Phosphatase inhibitor.