以2-氨基噻唑为原料,经Boc保护、溴代、氟代和脱保护成盐反应合成了制备葡萄糖激酶激活剂的重要中间体——2-氨基-5-氟噻唑盐酸盐,总收率55%,其结构经1H NMR表征。
A key medicine intermedia,2-amino-5-fluorothiazole hydrochloride,was synthesized from 2-aminothiazole by a four-step reaction of Boc-protection,bromination,fluoridation and N-Boc deprotection in total yield of 55%.The structure was characterized by 1H NMR.