Synthesis And Quality Control Of Sarpogrelate Hydrochloride

Sarpogrelate Hydrochloride is a serotonin receptor antagonist, which can effectively improve the state of peripheral circulation and the ischemic caused by chronic arterial occlusion. Clinically, it was used to improve the ischemic caused by chronic arterial occlusion such as ulcer, pain and cold feeling.Sarpogrelate is a listed species developed by Japanese Mitsubishi Pharma, given the trade name "Anplag". Sarpogrelate hydrochloride tablets were available in Japan in July 1993, while in March 1999 the corresponding fine granules were available in Japan. On October 29th,1998, Mitsubishi Pharma sarpogrelate tablets obtained administrative protection in China. The development of this product will contribute to a positive social significance and good economic benefits.This project refered to the related literatures for optimizing the synthetic route of sarpogrelate hydrochloride, employing 2-((3-methoxy) phenethyl) phenol as a starting material, followed by the epichlorohydrin, dimethylamine reaction with succinic anhydride esterification sarpogrelate base, and then with the hydrochloride salt, the hydrochloride sarpogrelate, and by organic elemental analysis, IR, UV, NMR, mass spectrometry and thermal analysis to confirm the structure.The issue of quality sarpogrelate hydrochloride from character, identification, examination and determination of the four aspects of the research system and a systematic and comprehensive verification of their related substances, epichlorohydrin and the residual solvent content, eventually a quality standard of hydrochloric acid sarpogrelate has been developed.By studying this project, the economical and simple process to obtain the hydrochloride sarpogrelate has been developed, and we have conducted a systematic and comprehensive study of the quality system, which can provide a reliable base for its future manufacture and research.