【摘要】 2-甲基-2-羟基丙腈(2)经三甲基硅基(TMS)保护后,经Blaise反应并脱三甲基硅烷基保护,在亚硝酸钠和乙酸作用下肟化和Pd/C催化还原得到2-氨基-4-羟基-4-甲基-3-氧代戊酸乙酯三氟乙酸盐,再与丁酰亚氨酸甲酯盐酸盐环合得到奥美沙坦酯关键中间体4-(1-羟基-1-甲基乙基)-2-丙基-1H-咪唑-5-羧酸乙酯,总收率约40%。更多还原

【Abstract】 Ethyl 4-(1-Hydroxy-1-methylethyl)-2-propyl-4,5-dihydro-1H-imidazole-5-carboxylate,a key intermediate of olmesartan medoxomil,was synthesized from 2-hydroxy-2-methylpropanenitrile by protection with trimethylsilyl,Blaise reaction,deprotection,oximation with sodium nitrite and acetic acid,reduction with Pd/C as catalyst and cyclization with methyl butanimidate hydrochloride with an overall yield of about 40%.更多还原