A novel and eco-friendly procedure for the synthesis of some pyrazolo-thiadiazolo-pyrimidinones and its in vitro anti-bacterial activity

A novel series of 2-substituted-aminomethyl-8-phenyl-pyrazolo3,4-d]1,3,4]thiadiazolo3,2-a]pyrimidin-4(1H)-ones have been synthesized by treating 2-chloromethyl-8-phenyl-pyrazolo3,4-d]1,3,4]thiadiazolo3,2-a]pyrimidin-4(1H)-one with various nucleophiles. The chloromethyl derivative was prepared by treating 2-amino-3-mercapto pyrazolo3,4-d]pyrimidine with one carbon donor, chloroacetic acid. The intermediate 2-amino-3-mercapto pyrazolo3,4-d]pyrimidine was prepared by a novel, eco-friendly route starting from 2-amino-3-carbethoxy-1-phenyl-pyrazole. The target compounds exhibited broad-spectrum antibacterial activity (Kirby Bauer’s Method).