头孢匹胺关键中间体(F)的合成研究

The Synthesis of Cefpiramide Key Intermediate (F)

以脱氢醋酸及对羟基苯甘氨酸为主原料,经过脱酸、缩合、开环重排、酯化、酰胺化、水解等6步反应制备头孢匹胺的关键中间体,其中酯化采用氯化亚砜替代难于运输及储存的氯化氢乙醇溶液方便工业化大生产;酰胺化及水解采用"一锅法"则大大降低溶剂二氯甲烷的损耗,减少了工序,提高了设备的使用效率,且使收率提高10%以上,产品质量也合格;产品结晶采用加热重结晶方法可大大缩短干燥时间,提高生产效率。

Dehydroacetate and p -hydroxyphenyl sation, ring - opening rearrangement, esterification, （F） was systhsized, wherein the esterification reaction glycine as the main raw material, through the deacidified, conden- amidation, and hydrolysis 6 steps, Cefiramide key intermediates cefpiramide chloridesulfoxide instead of the large - scale production of hydrogen chloride ethanol solution convenient industrialized difficult to transport and store. Amidation and hydrolysis u- sing the ＂ one - pot＂ greatly reduced the loss of solvent methylene chloride, reduced the process to improve the efficiency in the use of the equipment, and made closingrate increase by 10%, and the product quality was also qualified. The prod- uct crystal can greatly shorten the drying time and improve production efficiency through heatin~ recrvstallization method