Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists.

Abstract A series of 2,3,3a,4-tetrahydro-1 H -pyrrolo[3,4- c ] isoquinolin-5(9b H )-ones is described, several examples of which exhibit potent 5-HT 2C agonismwith excellent selectivity over the closely related 5-HT 2A and 5-HT 2B receptors. Compounds such as 38 and 44 were shown to be effective in reducing food intake in an acute rat feeding model.