一种合成氢溴酸达菲那新的新方法

摘要

Darifenacin hydrobromide was synthesized from ( S )-N-Boc-3-hydroxypyrrolidine by Mit-sunobu reaction , amidation , deprotection , followed by condensation with 5-( 2-chloroethyl )-2 , 3-di-hydrobenzofuran and salt formation with an overall yield of 35%.The structure was confirmed by 1 H NMR, MS( ESI) and elemental analysis .%以(S)-N-BOC-3-羟基吡咯烷为原料,依次经Mitsunobu反应,酰胺化和脱保护反应,再与5-(2-氯乙基)-2,3-二氢苯并呋喃缩合后成盐合成了高纯度的氢溴酸达菲那新,其结构经1 H NMR,MS(ESI)和元素分析确证,总收率约35%.