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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%。
2-Methyl-2-hydroxypropionitrile (2) was protected by trimethylsilyl (TMS), reacted by Blaise reaction and deprotonated with trimethylsilyl, oximeized with sodium nitrite and acetic acid and Pd / C catalytic reduction to give 2-amino-4-hydroxy-4-methyl-3-oxopentanoate trifluoroacetate, followed by butyric acid methyl ester hydrochloride cyclization to Olmesartan Medoxomil The key intermediate was 4- (1-hydroxy-1-methylethyl) -2-propyl-1H-imidazole-5-carboxylate in about 40% yield.