埃罗替尼盐酸盐的全合成

Total Synthesis of Erlotinib Hydrochloride

以3,4-二羟基苯甲酸为起始原料,经醚化、酰胺化、酰胺脱水、硝化、还原、汇聚成环和成盐等7步反应合成了埃罗替尼盐酸盐,总收率10.2%,其结构经1H NMR,IR和MS确证。

Erlotinib hydrochloride in total yield of 10.2% was synthesized by a seven-step reaction including etherification,amidation,dehydration,nitration,reduction,convergent cyclization and salt formation using 3,4-dihydroxybenzoic acid as the starting material.The structure was confirmed by1 H NMR,IR and MS.