DEVELOPMENT OF A MANUFACTURING PROCESS FOR ZATOSETRON MALEATE

Zatosetron maleate is a potent, selective 5-hydroxytryptamine receptor antagonist, In anticipation of commercialization, a manufacturing syn thesis of zatosetron from tropinone and 5-chlorosalicylic acid was dev eloped, Development efforts focused on addressing several key issues i ncluding the supply and quality of the critical raw material tropinone , improvements in the stereoselective formation of 3-endo-tropanamine and the compatibility with existing manufacturing capabilities of proc ess requirements for the Claisen rearrangement used to produce a cruci al benzofuran intermediate, The results of these studies and an improv ed route to zatosetron maleate are described.