重要的半合成头孢菌素中间体——7-ADCA

An Important Semisynthetic Cephalosporin Intermediate:7-ADCA

7-氨基-3-去乙酰氧基头孢烷酸(7-ADCA)是以青霉素G为原料,经氧化、扩环重排、裂解3步反应制得。目前用于裂解反应的固定化酰化酶技术日益成熟,因而化学法裂解的生产工艺已逐渐被淘汰。世界上主要生产厂家有荷兰GIST公司、美国TEVA公司、意大利DOBFA公司、台湾骏祥公司和印度LUPIN公司等。国内华北制药倍达公司开发了酶法生产7-ADCA的工艺,并建立了250t/a的生产能力,产品质量与进口产品相当。我国7-AD-CA年需求量约900t,而生产能力不足300t/a。国内企业应改进回收工艺、降低生产成本、实现规模化生产,以改变市场依赖进口的局面。

7-aminodesacetoxy cephalosproanic acid (7-ADCA) is made from penicillin G via oxidation, ring enlargement rearrangement and fragmentation. At present, immobilized amidate enzyme technology used in fragmentation reaction is coming increasingly to maturity and the chemical fragmentation process is gradually being obsolete. The important producers are GIST of Dutch, TEVA of the US, DOBFA of Italy and LUPIN of India as well as Junxiang Co. of Taiwan province. In China, NCPC BETA Co. has developed enzyme method for manufacturing 7-ADCA, and a plant with production capacity of 250t/a has been built, its product quality is comparable to that made abroad. China's annual demand for 7-ADCA is about 900t, however, production capacity is less than 300t/a. The producers at home should improve the recovery process, decrease the costs and expand production scale to change the market dependence on imports.