Synthesis and antimicrobial evaluation of imidazo-[1',5':1,2]pyrimido [4,5-d]isoxazolo[2,3-a]pyrimidin-10-ones.

A new series of novel imidazo-[1',5':1,2]pyrimido[4,5-d]isoxazolo[2,3-a]pyrimidin-10-ones 5 has been accomplished by reaction of 3-amino-5-methyl-7aryl-7H-isoxazolo[2,3-a]pyrimidin-6-yl cyanides 2, with choloacetylchloride followed by treatment with aromatic primary amines and, then with formaldehyde. The key intermediate 2, is obtained by reaction of 3-amino-5-methylisoxazole 1 with aromatic aldehydes, and malononitrile by a three-component one-pot synthesis. The structures of newly synthesized compounds 2-5 have been established on the basis of spectral data, and evaluated for their in vitro antimicrobial activity. [ABSTRACT FROM AUTHOR]