[1]李雯,赵君颖,章亚冬,等.一水合-L-(2R,3R)-(-)-二苯甲酰酒石酸的合成[J].郑州大学学报(工学版),2006,27(02):62-64.[doi:10.3969/j.issn.1671-6833.2006.02.015]
　LI Wen,ZHAO Junying,Zhang Yadong,et al.Synthesis of -L-(2R,3R)-(-)-dibenzoyl tartaric acid monohydrate[J].Journal of Zhengzhou University (Engineering Science),2006,27(02):62-64.[doi:10.3969/j.issn.1671-6833.2006.02.015]

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一水合-L-(2R,3R)-(-)-二苯甲酰酒石酸的合成()

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《郑州大学学报(工学版)》[ISSN:1671-6833/CN:41-1339/T]

卷:

27卷

期数:

2006年02期

页码:

62-64

栏目:

出版日期:

1900-01-01

文章信息/Info

Title:

Synthesis of -L-(2R,3R)-(-)-dibenzoyl tartaric acid monohydrate

作者:

李雯; 赵君颖; 章亚冬; 等.

郑州大学化工学院,河南,郑州,450002, 河南省中医学院第二附属医院,河南,郑州,450008

Author(s):

LI Wen; ZHAO Junying; Zhang Yadong; etc

关键词:

酒石酸;  苯甲酸;  亚硫酰氯;  二苯甲酰酒石酸;  合成

Keywords:

tartaric acid;  Benzoic acid;  Thionyl chloride;  Dibenzoyl tartaric acid;  Synthesis

DOI:

10.3969/j.issn.1671-6833.2006.02.015

文献标志码:

A

摘要:

一水合-L-(2R,3R)-(-)-二苯甲酰酒石酸是重要的手性药物拆分剂,但其价格昂贵,因此,我们对其合成方法进行了研究.采用2R,3R-酒石酸、苯甲酸、亚硫酰氯为原料,苯甲酰化伴随脱水反应生成二苯甲酰酒石酸酐,然后酸酐水解得到目标产物,以酒石酸计,一水合二苯甲酰酒石酸的总收率为70.9%,该方法采用亚硫酰氯将反应生成的苯甲酸酰化后重新利用,反应收率高、后处理简便.产物结构经旋光度的测定,与报道结果一致.该方法工艺条件易于控制,污染少.

Abstract:

L-(2R,3R)-(-)-dibenzoyl tartaric acid monohydrate is an important chiral drug splitting agent, but it is expensive, so we have investigated its synthesis method. Using 2R, 3R-tartaric acid, benzoic acid, thionyl chloride as raw materials, benzoylation with dehydration reaction to generate dibenzoyl tartaric anhydride, and then hydrolysis of acid anhydride to obtain the target product, in terms of tartaric acid, the total yield of dibenzoyl tartaric acid monohydrate is 70.9%, the method uses thionyl chloride to acyllate the reaction generated by benzoic acid and reuse, the reaction yield is high, the post-treatment is simple. The structure of the product was determined by optical rotation, which was consistent with the reported results. The process conditions of this method are easy to control and the pollution is less.

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