Synthesis, spectral characterization, docking studies and biological activity of urea, thiourea, sulfonamide and carbamate derivatives of imatinib intermediate.

A series of new urea/thiourea derivatives 3a-j were synthesized by simple addition reaction of functionalized phenyl isocyanates/isothiocyanates 2a-j with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine (imatinib intermediate) (1) in the presence of 1,4-dimethyl piperazine (DMPZ) as a base, and another series of new sulfonamide/carbamate derivatives 5a-k were synthesized by reacting 1 with various substituted aromatic sulfonyl chlorides 4a-f and aromatic/aliphatic chloroformates 4g-k in the presence of DMPZ as a base. The title compounds 3a-j and 5a-k were characterized by IR, 1H, 13C NMR and mass spectral data. Antimicrobial, antioxidant and in silico molecular docking studies were made against aromatase.

Phase-transfer catalytic dichlorocyclopropanation of styrene under the influence of ultrasound conditions - A kinetic study.

The kinetics for dichlorocyclopropanation of styrene with an excess of chloroform were studied under phase-transfer catalysis and ultrasound irradiation conditions using aqueous sodium hydroxide as the base and benzyltriethylammonium bromide as a catalyst. The reaction was carried out at 35°C under pseudo-first order conditions by keeping aqueous sodium hydroxide and chloroform in excess and was monitored by gas chromatography (GC). The effects of agitation speed, quaternary ammonium salts, amount of catalyst, amount of sodium hydroxide and temperature on the kinetics of the conversion were investigated.