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目的:合成替比培南匹伏酯侧链1-(4,5-二氢-2-噻唑啉基)-3-巯基吖丁啶盐酸盐。方法:以2-甲硫基-2-噻唑啉为原料,经与3-羟基吖丁啶盐酸盐,甲烷磺酰氯,硫代乙酸钾以及水解4步反应合成1-(4,5-二氢-2-噻唑啉基)-3-巯基吖丁啶盐酸盐。结果:合成了1-(4,5-二氢-2-噻唑啉基)-3-巯基吖丁啶盐酸盐,总收率42%。结论:本方法可以方便地得到替比培南匹伏酯侧链1-(4,5-二氢-2-噻唑啉基)-3-巯基吖丁啶盐酸盐,提高了反应收率,简化了操作,降低了成本。
OBJECTIVE: To synthesize 1 - (4,5-dihydro-2-thiazolinyl) -3-mercaptoazetidine hydrochloride in the serotonin side of pepivacaine. Methods: 1- (4,5-bis (2-methylthio) -2-thiazoline was synthesized by the reaction with 3-hydroxyazetidine hydrochloride, methanesulfonyl chloride and potassium thioacetate in 4- Hydro-2-thiazolinyl) -3-mercaptoazetidine hydrochloride. Results: 1- (4,5-dihydro-2-thiazolinyl) -3-mercaptoazetidine hydrochloride was synthesized in 42% overall yield. Conclusion: This method can be easily obtained petipapirin side chain 1- (4,5-dihydro-2-thiazolinyl) -3-mercaptoazetidine hydrochloride, improve the yield of the reaction, Simplifies operation and reduces costs.