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毛果芸香碱化学合成的实验研究始于本世纪三十年代。由于制得的产物是以异毛果芸香碱为主,而异毛果芸香碱的药理活性仅及毛果芸香碱的20～50分之一;加上合成路线冗长,显然不可能指望用这种方法制造毛果芸香碱供药用。近年来采用贵重金属触媒接触氢化的方法合成成功具有顺式结构的高匹罗匹酸(Ho-mopilopic acid),并经由这一重要的中间体取得以毛果芸香碱为主的产物,因此用化学合成方法制造毛果芸香碱的实验研究有了新的进展。我们参考这些文献资料,在实验室合成
The experimental study of chemical synthesis of pilocarpine began in the 1930s. Since the product obtained is based on isopullinoside, the pharmacological activity of isopullicin is only 20 to 50 times less than that of pilocarpine. With the lengthy synthesis route, it is obviously impossible to expect to use this method to produce pilocarpine for medicinal purposes. In recent years, Ho-mopilopic acid with a cis-structure has been successfully synthesized by catalytic hydrogenation of a noble metal catalyst, and a major product of pilocarpine has been obtained through this important intermediate, and therefore a chemical synthesis method has been used. The experimental research on the manufacture of pilocarpine has made new progress. We refer to these literature materials and synthesize them in the laboratory.