合成普瑞巴林优化工艺研究

摘要

本研究优化以R-( +) -α-苯乙胺为拆分剂将( ± )3-(氨甲酰甲基) -5-甲基己酸拆分后酸解为R-( -) -3-氨甲酰甲基-5-甲基己酸,再通过霍夫曼降解生成普瑞巴林的生产工艺,总收率为33. 7%,并用熔点、纯度,比旋光度、LC-MS、IR、1H NMR对产物的结构和性质进行表征.%The synthesis process of pregabalin by first ( R ) -( -) ( carbarnoylrnethyl ) -5 -methylhexanoic acid, ( R) -( + ) -α-phenylethylarnine salt was optimized from ( ± ) -3-Carbamoymethyl-5-methylhexano-ic acid and ( R) -( + ) -α-phenylethylarnine. Then ( R) -( -) ( carbarnoylrnethyl) -5-methylhexanoic acid was gained with acidolysis,and final pregabalin was produced throught Hofmann degradation. The total yield was up to 33. 7 %. The structures and properties were characterized by melting point, purity,specific rotation,LC -MS, IR and 1 H-NMR.