盐酸头孢甲肟—锅法合成技术

One-step in-situ synthetic process of cefmenoxime hydrochloride

以3-[[(1-甲基-1H-四唑-5-基)硫]甲基]-7-氨基-头孢烷酸盐(7-ATCA)为原料,在C7的-NH_2位置上与AE活性酯发生缩合反应得到头孢甲肟,然后在不分离的情况下直接与盐酸成盐得到盐酸头孢甲肟。本方法简化了生产工艺,可以降低成本,增加经济效益,并减少了"三废"的处理数量。以7-ATCA·HCI为基准,克分子收率可达到66.5%以上,产品符合质量标准。

Cefmenoxime hydrochloride was synthesized by condensation reaction with the side chain compound 2-（2-amino-4-thiazol）-2（z）-methyloxy-imino acetic acid on C7-position and using 3-[（1-methyl-lH- tetrazol-5-yl-thio）-methyl]-7-amino-cephalosporanic acid hydrochloride as the starting material. Without separating cefmenoxime from the solution, it reacted with hydrochloride acid directly to convert to final product, cefmenoxime hydrochloride. The total yield of the process was higher than 66.5% （based on 7-ATCA · HCl） and its quality was up to the standard （YBH11822004）.