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苯并[d]噻唑啉-2-酮-6-甲酸的合成研究
引用本文:祝辉,罗自力,杨日芳,恽榴红. 苯并[d]噻唑啉-2-酮-6-甲酸的合成研究[J]. 解放军药学学报, 2011, 27(3): 197-198. DOI: 10.3969/j.issn.1008-9926.2011.03.03
作者姓名:祝辉  罗自力  杨日芳  恽榴红
作者单位:1. 成都军区联勤部药品仪器检验所,四川成都,610017
2. 军事医学科学院毒物药物研究所,北京,100850
摘    要:
目的 设计一条简便、高效的合成路线用于苯并[d]噻唑啉-2-酮-6-甲酸的合成.方法 对氨基苯甲腈经硫氰化、关环、水解制得4-氨基-3-巯基-苯甲酸,再与氯甲酸乙酯环合反应得到苯并[d]噻唑啉-2-酮-6-甲酸.结果 目标化合物经1H-NMR和MS确证,新设计路线的总收率约62.2%.结论 本研究采用价廉易得的对氨基苯...

关 键 词:苯并[d]噻唑啉-2-酮-6-甲酸  多巴胺D3受体  合成

A Study of the Synthesis of Benzo[d] Thiazolone-6-carboxylic Acid
ZHU Hui,LUO Zi-li,YANG Ri-fang,YUN Liu-hong. A Study of the Synthesis of Benzo[d] Thiazolone-6-carboxylic Acid[J]. Pharmaceutical Journal of Chinese People's Liberation Army, 2011, 27(3): 197-198. DOI: 10.3969/j.issn.1008-9926.2011.03.03
Authors:ZHU Hui  LUO Zi-li  YANG Ri-fang  YUN Liu-hong
Affiliation:②①Chengdu Military Institute for Drug Control,Chengdu610017,China;②Department of Medicinal Chemistry,Beijing Institute of Pharmacology and Toxicology,Beijing100850,China
Abstract:
Objective To design a simple and efficient synthetic method for benzo[d]thiazolone-6-carboxylic acid.Methods Benzo[d]thiazolone-6-carboxylic acid was prepared form 4-aminobenzonitrile through thiocyanation and hydrolysis to yield 4-amino-3-mercaptobenzoic acid,which was subjected to cyclization with an ethyl chlorocarbonate.Results The structure of benzo[d]thiazolone-6-carboxylic acid was identified by 1H-NMR and MS.The overall yield of the new method was 62.2%.Conclusion An efficient and high yielding proc...
Keywords:benzo[d]thiazolone-6-carboxylic acid  dopamine D3 receptor  synthesis  
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