盐酸克林霉素的合成研究

SYNTHETIC STUDY ON CLINDAMYCIN HYDRODHLORIDE

研究成功盐酸克林霉素的一种简便而经济的合成方法。此法系采用二氯亚砜与DMF形成vilsmeier试剂的改进法,并试验四种抗氧化剂参与氯化反应,从中选出一种较理想的抗氧化剂,使中间体盐酸克林霉素醇合物的收率由原来的66％提高到75.6％,改进和简化了文献的后处理方法。

A simpler,more convenient and more economic synthetic method of Clindamycin hydrochloride was found through synthetic study. This was an improved method of the preparation of Vilsmeier agent, which was prepared from SOCl_2 and DMF. Four antioxidants were prepared and used in the process, and the best one was selected.The yield of Clindamycin hydrochloride ethanol solvate increased from 66％ to 75.6％ and the purification in the literature was simplified.