摘要
4-乙氧羰基-3-乙氧基苯乙酸(2)和对甲苯磺酰氯用碳酸钾为碱,氯化苄基三乙铵为相转移催化剂反应制得混酐,再与(S)-3-甲基-1-[2-(1-哌啶基)苯基]丁胺反应制得(S)-2-乙氧基-4-[2-[3-甲基-1-[2-(1-哌啶基)苯基]丁基氨基]-2-氧代乙基]苯甲酸乙酯,再在乙醇中经氢氧化钠水解即可制得瑞格列奈,总收率约74%(以2计)。
Repaglinide was synthesized from 4-ethoxycarbonyl-3-ethoxyphenylacetic acid by reaction with p-toluenesulfonyl chloride in the presence of potassium carbonate and benzyltriethylammonium chloride to give the mixed anhydride, which was subjected to condensation with （S）-3-methyl-l-（2-piperidin-l-ylphenyl）butylamine and then hydrolysis with NaOH with an overall yield of about 74 % （based on 4-ethoxycarbonyl-3-ethoxyphenylacetic acid）.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2012年第2期84-86,共3页
Chinese Journal of Pharmaceuticals
关键词
瑞格列奈
糖尿病治疗药
合成
repaglinide
antihypoglycemic drug
synthesis
