噻拉米特合成工艺的优化

Optimization of synthesis process of thiaramide

目的合成噻拉米特对其合成工艺进行优化。方法以5-氯-2(3H)-苯并噻唑啉酮、溴乙酸乙酯、2-哌嗪基-1-乙醇为起始原料,通过取代、水解、酰胺化反应得到目标化合物噻拉米特。结果经过3步反应以23.96%的总收率得到噻拉米特,结构经过1H NMR及MS确证。结论该路线优化了实验条件,为工业化应用提供了实验基础。

Objective To synthesize thiaramide and optimize its synthesis process.Methods Thiaramide was synthesized from 5-chloro-2(3H)-benzothiazolinone,ethyl bromoacetate and 2-piperazinyl-1-ethanol by substitution,hydrolysis and amidation.Results Thiaramide was obtained in 23.96%yield in three steps.Its structure was confirmed by 1H NMR and MS.Conclusion The route optimizes the experimental conditions and provides the experimental basis for industrial application.