Study On The Synthesis And Quality Of Palonosetron Hydrochloride

Palonosetron is a potent and highly selective serotonin 5-HT3 receptor antagonist that has been evaluated for the prevention of chemotherapy-induced nausea and vomiting. Palonosetron is a new 5-HT3 receptor antagonist with a longer half life and a higher binding affinity than older 5-HT3 receptor antagonists, with a comparable safety profile for all treatment groups.with its extended duration of action, excellent safety profile, and high response rates palonosetron is a safe and potentially more effective alternative to currently marketed first generation 5-HT3 receptor antagonists.After analyzing the literatures, this article design the synthesis routine by the method of anti-synthesis, and choose the available routine according to the compare and analysis, as well as experiment condition: synthesize it using 1- naphthoic acid,ethanoic acid,Pd/C as the starting material and the reduction reaction is the first step. After a series steps, we obtain the target compound- Palonosetron HCL. The structures of the target molecules determined by melting point, optical rotation are the same as the standard sample. The recovery yield is rather high by optiminzing the reaction condition.This article also studies the quality of the product, which fits with the standard raw medicine. Quality standard is basically determined after careful research on the identification, relative material limit, organic volatile impurities and effective ingredient contents. The stability research has also been performed under high temperature circumstances, high wet circumstances and highlight circumstances respectively.This synthetic technology has some advantages: easily available raw material, low cost, easy operation and mild reaction condition. Above all, this article provide a possible technology for the industrializing producing of stachdrine.