超强质子酸催化下连续法制备7-氨基-3-乙烯基头孢烷酸及一步脱保护反应机理研究

Continuous preparation of 7-amino-3-vinylcephalosporanic acid catalyzed by superprotic acid and study on the mechanism of one-step deprotection

GVNE反应液经脱水后,经超强质子酸催化,可不经结晶出GVNE直接与苯酚反应水解掉4位保护基,从而实现连续制备,从而减少了制备过程中溶剂损耗及能量消耗,所制备出产品与原工艺的差别。介绍了连续法中2种竞速反应的反应机理。

After dehydration of GVNE reaction solution,catalyzed by super proton acid,GVNE reacts directly with phenol without crystallization to hydrolyze off the 4-position protective group,thus realizing continuous preparation,thus reducing the solvent loss and energy consumption in the preparation process,and the product prepared is different from the original technology.The reaction mechanism of two kinds of racing reaction was introduced in detail in the continuous reaction method.