苯并[d]噁唑啉-2-酮-5-羧酸的合成研究  

Study on Synthesis of Benzo[d]oxazolone-5-carboxylic Acid

作　　者：王卫娜[1,2] 杨日芳[1] 祝辉[1,3] 李斐[1] 李锦[1] 刘宏民[2] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850 [2]郑州大学药学院,郑州450000 [3]成都军区联勤部药品仪器检验所,成都610017

出　　处：《科学技术与工程》2012年第17期4250-4251,4270,共3页Science Technology and Engineering

基　　金：国家863重大新药创制专项基金(2011ZX09102-005-01)资助

摘　　要：利用较价廉的3-硝基-4-羟基苯甲酸在Pd/C催化下氢化还原得3-氨基-4-羟基苯甲酸,再与氯甲酸甲酯(或氯甲酸乙酯)成环得苯并[d]噁唑啉-2-酮-5-羧酸。目标化合物经1H NMR和MS确证,总收率为81.6%。该方法工艺简单,条件温和,收率较高,便于工业合成。A relatively cheap 4-hydroxy-3-nitrobenzoic acid was hydrogenated to yield 3-amino-4-hydroxy-benzoic acid,then the amino acid was condensed with met-hyl chloroformate（or ethyl chloroformate） to afford benzo[d]oxazoline-2-one-5-carboxylic acid.the structure of the title product was identified by 1H NMR and MS.The overall yield of the new method was 81.6%.The method is better with a simple process,mild conditions,high yield,and facilitate industrial synthesis.

关 键 词：苯并[d]噁唑啉-2-酮-5-羧酸 多巴胺D3受体选择性拮抗剂 合成 

分 类 号：O623.653[理学—有机化学]