摘要
用正丁酸与邻苯二胺为原料,在微波照射下缩合成2-丙基苯并咪唑,再氧化开环制得2-丙基咪唑二羧酸,再经酯化、Gringard反应制得抗高血压药物奥美沙坦的关键中间体2-丙基-4-[(1-羟基-1-甲基)乙基]-1H-咪唑-5-羧酸乙酯,总收率32.2%。
Ethyl 4-[(1-hydroxy-1-methyl)ethyl]-2-propyl-1H-imidazole-5-carboxylate,the key intermediate of Olmesartan,was synthesized from butanoic acid and o-phenylenediamine via condensation under microwave-irradiation,oxidation,esterification and the Gringard reaction.The overall yield of target product was 32.2%.
出处
《化学试剂》
CAS
CSCD
北大核心
2007年第11期679-680,共2页
Chemical Reagents
基金
浙江省科技厅面上项目(2005F13G5250019)