化工时刊
化工時刊
화공시간
CHEMICAL INDUSTRY TIMES
2015年
3期
6-11
,共6页
陈美林%张珍明%王国成%王婷%王璇%徐云峰
陳美林%張珍明%王國成%王婷%王璇%徐雲峰
진미림%장진명%왕국성%왕정%왕선%서운봉
普瑞巴林%优化工艺%合成
普瑞巴林%優化工藝%閤成
보서파림%우화공예%합성
pregabalin optimization process synthesis
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.
本研究優化以R-( +) -α-苯乙胺為拆分劑將( ± )3-(氨甲酰甲基) -5-甲基己痠拆分後痠解為R-( -) -3-氨甲酰甲基-5-甲基己痠,再通過霍伕曼降解生成普瑞巴林的生產工藝,總收率為33. 7%,併用鎔點、純度,比鏇光度、LC-MS、IR、1H NMR對產物的結構和性質進行錶徵.
본연구우화이R-( +) -α-분을알위탁분제장( ± )3-(안갑선갑기) -5-갑기기산탁분후산해위R-( -) -3-안갑선갑기-5-갑기기산,재통과곽부만강해생성보서파림적생산공예,총수솔위33. 7%,병용용점、순도,비선광도、LC-MS、IR、1H NMR대산물적결구화성질진행표정.
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.
