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佐美酸钠(Zomepirac)为较新的镇痛、解热、抗炎药,化学名:5-(对氯苯甲酰基)-1,4-二甲基-1H-吡咯烷-2-乙酸钠二水合物。该药系美国McNeil公司于1972年创制,经动物试验表明,其镇痛作用与吗啡相当。口服后1小时可达最高血浓度。临床用于缓解癌症等的疼痛而无成瘾性,未见对肝和血象有损害,镇痛效果良好,已由美国食品及药物管理局于1981年批准上市。据文献报道合成佐美酸钠有多种方法,我们以不同的方法试制结果,认为以采用下列合成路线较为合适,因该路线工艺操作简便,收率稳定,且中间体原料易得。
Zomepirac is a relatively new analgesic, antipyretic, anti-inflammatory drug with the chemical name: sodium 5- (p-chlorobenzoyl) -1,4-dimethyl- 1 H-pyrrolidine-2-acetate Dihydrate. The drug is the United States McNeil company created in 1972, animal experiments show that its analgesic effect and morphine are quite. 1 hour after oral administration up to the highest blood concentration. Clinically used to relieve the pain of cancer without addiction, no damage to the liver and blood, analgesic effect is good, by the US Food and Drug Administration in 1981 approved the listing. It has been reported in the literature that there are many ways to synthesize sodium sodate, and we try the results in different ways. We think it is more suitable to adopt the following synthetic route because the route is simple, stable and the raw materials of the intermediate are easily available.