利可君合成工艺改进

目的:利可君合成工艺改进.方法:将中间体先生成钠盐,通过萃取,洗涤,除去残余的苯乙酸乙酯和酯溶性杂质,然后游离获得固态的α-甲酰基苯乙酸乙酯.改进的工艺很好地解决了中间体固化的问题,且纯度非常高,无苯乙酸乙酯残留,继而通过和L-半胱氨酸盐酸盐反应获得的利可君成品.结果与结论:获得高纯度的利可君,工艺适合工业化生产.

Improvement of the Technological Method for the Synthesis of Leucogen

Objective: To synthesis leucogen.Methods: First of all,intermediates were synthesized as sodium 3-oxo-2-phenyl-ethyl acrylate.Then,ethyl-formyl-benzeneacetate could be purified via extraction and scrubbing to remove the ethyl phenylacetate and oil-soluble impurities.The intermediates as solids with high purity and little ethyl phenylacetate were obtained as the result of the improved technological method.Leucogen was then prepared by the reaction of ethyl-formyl-benzeneacetate and L-cysteine hydrochloride.Result and conclusion: The improvement can get leucogen with high purity and is more attractive for the manufacture on a large scale.