Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT2c agonists

Abstract This Letter reports the design and synthesis of several novel series of piperazinyl pyrimidinones as 5-HT 2C agonists. Several of the compounds presented exhibit good in vitro potency and selectivity over the closely related 5-HT 2A and 5-HT 2B receptors. Compound 11 was active in in vivo models of stress urinary incontinence.