抗癫痫药左乙拉西坦的工艺优化新方法
A Novel Method on the Process Optimization of Synthesizing Levetiracetam
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摘要: 以(S) α 乙基 氧代 1 吡咯烷乙酸为起始原料,在活化剂和氨气作用下,用两步一锅法制备左乙拉西坦。探讨了不同的活化剂、缚酸剂等因素对活性酯法成酰胺反应过程的影响,确定了最优物料投放比例;当以甲磺酰氯作为活化剂时,反应收率可达到约92.0%;改良后的工艺收率稳定,适合工厂工业化大规模生产。Abstract: Levetiracetam is prepared from (S) alpha ethyl oxo 1 pyrrolidineacetic acid by the use of activating reagents and gaseous ammonia in one pot reaction. Bases on the influence of active ester method, the factors such as activating agents and bases were discussed, and then the optimal ratio of raw materials was determined. The yield can be about 92.0% using methane sulfonyl chloride as activating agent. The improved process is suitable for mass industrialized production.