Scalabe Synthesis of the Azaperone Drug by Using Flow Chemistry

Azaperone is a neuroleptic drug with sedative and antiemetic effects, used as a sedative. We reported the development of a simple Synthesis of Azaperone that involves a four-step process using a micro-reactor device. They produced bis(2-chloroethylene)amine by converting alcohol groups into chloride using thionyl chloride, achieving a 96% yield. Next, 2-amino pyridine undergoes alkylation in TBAB to form 1-(pyridine-2-yl)piperazine with a 75% yield. This intermediate is further alkylated using 4-chloro-1-(4-fluorophenyl)butane-1-one to achieve Azaperone with a 65% yield.