SYNTHESES AND BIOLOGICAL-ACTIVITIES OF OPTICAL ISOMERS OF RIDINO)PROPYL]-10,11-DIHYDRO-5H-DIBENZ[B,F]AZEPINE (MOSAPRAMINE) DIHYDROCHLORIDE

Mosapramine (1) is a new neuroleptic drug with an asymmetric carbon at om (8a) in its imidazopyridine ring. The enantiomers of this agent wer e synthesized to compare their biological activities, such as antiapom orphine activity, affinity for dopamine D2 receptor and acute toxicity . The key intermediates, (R)-(-)- and ydroimidazo[1,2-a]pyridine-3-spi ro-4'-piperidines, were prepared by optical resolution of the (+/-)-co mpound and were treated with onyloxypropyl)-10,11-dihydro-5H-dibenz[b, f]azepine to afford (R)-(-)-1 and (S)-(+)-1, respectively. There were few differences in the examined biological activities of the two enant iomers as thier dihydrochlorides.