Study On The Synthesis Of Palonosetron

Palonosetron, a potent 5-HT3 receptor antagonist, which was developed by Helsinn Healthcare SA, with a characteristic of low dosage, high selectivity, low side effect, long half-life, has shown efficiency in preventing chemotherapy-induced nausea and vomiting (CINV). Palonosetron, named Aloxi as the trade name, launched in U.S.A and Japan chiefly after examination and approval by FDA in July 2003.In the paper, a relatively reasonable synthetic route via a eight-steps process starting with 3-quinuclidinone hydrochloride, was selected via analysis and comparison of synthesis process of Palonosetron which was certified by ¹HNMR, ¹³CNMR, IR and MS. The synthetic procedure of intermediates was studied carefully and optimized in order to reduce the cost and make the operation easy.