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以3,4-二羟基苯甲醛为原料,经苄基保护、与甘氨酸缩合、苄氧羰基保护得到关键中间体外消旋苏赤式-3-(3,4-二苄氧基苯基)-N-苄氧羰基丝氨酸(3);3经二环己胺和S-2-氨基-1,1-二苯基-1-丙醇拆分得到屈昔多巴,总收率11.3%,其结构经1H NMR,MS和元素分析确证。
Droxidopa in total yield of 11.3% was synthesized by the resolution of dicyclohexylamine and S-2-amino-1,1-diphenyl-propanol from racimic-threo/erythro-(3,4-dibenzyloxyphenyl)serine,which was prepared from 3,4-dihydroxybenzaldehyde by protection of benzyl,condensation with glycine and protection of benzyloxycarbonyl.The structures were confirmed by ~1H NMR,MS and elemental analysis.
