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抗氧化法制备高旋光度的新型手性拆分试剂R-四氢噻唑-2-硫酮-4-羧酸
引用本文:王婷婷,李俊峰,黄明刚,周鲁,宋航. 抗氧化法制备高旋光度的新型手性拆分试剂R-四氢噻唑-2-硫酮-4-羧酸[J]. 华西药学杂志, 2006, 21(3): 224-226
作者姓名:王婷婷  李俊峰  黄明刚  周鲁  宋航
作者单位:四川大学化学工程学院,四川,成都,610065;四川化工职业技术学院化工系,四川,泸州,646005
摘    要:目的对R-四氢噻唑-2-硫酮-4-羧酸合成产率的影响因素进行探讨,并通过抗氧化方法优化合成工艺。方法以L-半胱氨酸和二硫化碳为起始原料,在硫酸铜作催化剂的条件下合成目的化合物,比较不同抗氧化方法的结果,并对亚硫酸钠的抗氧化进行了优化。结果产品收率提高到75%,比旋度高达[α]2D0-102.1,均比原来提高了约10%,产物的化学结构经IR和1HNMR确定证。结论优化后的方法简便、有效。

关 键 词:R-四氢噻唑-2-硫酮-4-羧酸  抗氧化剂  亚硫酸钠  高旋光度  手性拆分剂  制备
文章编号:1006-0103(2006)03-0224-03
收稿时间:2005-10-01

Preparation of a new resolving agent R-2-thiothiazolidine-4-carboxylic acid with high specific polarity by antioxidation
WANG Ting-ting,LI Jun-feng,HUANG Ming-gang,ZHOU Lu,SONG Hang. Preparation of a new resolving agent R-2-thiothiazolidine-4-carboxylic acid with high specific polarity by antioxidation[J]. West China Journal of Pharmaceutical Sciences, 2006, 21(3): 224-226
Authors:WANG Ting-ting  LI Jun-feng  HUANG Ming-gang  ZHOU Lu  SONG Hang
Affiliation:1. Institute of Chemical Engineering, Sichuan University, Chengdu 610065, China ;2. Institute of Chemical Engineering, Sichuan Chemical Vocational School, Luzhou 646005, China
Abstract:OBJECTIVE To study the influence of the synthesis of R-2-thiothiazolidine-4-carboxylic acid on yield,and optimize the technique process by antioxidation.METHODS R-2-thiothiazolidine-4-carboxylic acid was synthesized with the reaction of L-Cysteine hydrochloride monohydrate and carbon bisulfide in the presence of hydrated cupric sulfate.All the antioxidation methods were compared,and then the amount condition of sodium sulfite was optimized.RESULTS The yield and specific polarity of the product were both higher than those of other methods.Chemical structure of the product was characterized by IR and ()~1HNMR.CONCLUSION This optimized technique is simple and feasible.
Keywords:R-2-Thiothiazolidine-4-carboxylic acid  Antioxidant  Sodium sulfite  High specific polarity  Resolving agent  Preparation
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