克林霉素磷酸酯关键中间体3,4-异亚丙基克林霉素的合成

Synthesis of Clindamycin Phosphate Key Intermediate Clindamycin 3,4-Isoproylidene

本研究以盐酸克林霉素醇化物为原料,原甲酸三乙酯为羟基保护剂,在三氟甲磺酸二苯胺盐(DPAT)催化下,反应值得3,4-异亚丙基克林霉素,收率大于93%。工艺操作简单,反应条件温和,收率高,催化剂用量少并可循环套用,适合工业化生产。

The existing way to produce clindamycin 3,4-isoproyidene, the key intermediate of clindamycin phosphate, has some limitations such as the high cost, low quality, and high toxicity caused by POC13, serious pollution and high environmental pressure. With the competition of the active pharmaceutical ingredient （API） market and the improvement of quality standard, developing cleaner way to produce clindamycin 3,4-isoproyidene is very important to improve quality, ensure the safe use of drugs, reduce costs. To solve the above problems, clindamycin 3,4-isoproyidene was obtained by hydroxyl protection reaction from clindamycin alcoholate hydrochloride with triethoxy methane in the presence of diphenylammonium trifluoromethanesulfonate （DPAT） in 93.1% yield. The amount of catalyst is small, and DPAT can be recycled. This process is simple, moderate, high yield, and suitable for industrialization.