甲砜霉素氯乙酸酯Delepine反应的研究

Studies on Delepine reaction of thiamphenicol glycinate hydrochloride

目的：证实甲砜霉素氯乙酸酯（α卤代羧酸酯类化合物）能与乌洛托品进行Ｄｅｌｅｐｉｎｅ反应，最终生成甲砜霉素甘氨酸酯盐酸盐。方法：利用电导率的方法测定Ｄｅｌｅｐｉｎｅ反应中间过程乌洛托品盐生成前后溶液的电导率的变化。结果：甲砜霉素氯乙酸酯与乌洛托品在乙腈溶液中能形成乌洛托品盐，且反应前后的电导率有明显的变化。结论：证实了甲砜霉素氯乙酸酯如同活性α卤代酮一样，能较好地进行Ｄｅｌｅｐｉｎｅ反应。

BJECTIVE: To confirm that thiamphenicol chloroacetic ester (halo carboxylic esteres) can carry out Delepine reaction and was finally converted into the target compound thiamphenicol glycinate hydrochlorid. METHODS: Electrical conductivity method was applied to determine the differences of electrical conductivity after and before forming urotropine salt in the intermediate process of Delepine reaction. RESULTS: Thiamphenical chloroacetic ester reaced with urotropine in acetonitrile to form an urotropine salt.There were obvious difference of electrical conductivity after and before the reaction. CONCLUSIONS: It showed that Delepine reaction of thiamphenicol chloroacetic ester was processed,similar to halo ketones.