(S)-α-乙基-2-氧代-1-吡咯烷基乙酰胺的合成工艺进展

Advances in Preparation of (S)-α- Ehtyl-2-oxo-1-pyrrolidinylacetamide

(S) α 乙基 2 氧代 1 吡咯烷基乙酰胺是制造抗癫痫新药左乙拉西坦的原料药 ,它具有治疗局限性和原发全身性癫痫、预防癫痫发作的独特药理作用 ,且不影响其他抗癫痫药物在体内代谢 ,疗效高 ,耐受性好。评价了 (S) α 乙基 2 氧代 1 吡咯烷基乙酰胺的 6条合成工艺 ,认为以具有正确立体结构的 (S) 2 氨基 4 (甲硫基 )丁酸甲酯盐酸盐为起始原料 ,是合成 (S) α 乙基 2 氧代 1 吡咯烷基乙酰胺的较佳工艺。

S ) α Ehtyl 2 oxo 1 pyrrolidinylacetamide is used as a raw material for manufacturing a new therapeutic agent (Levetiracetam) featuring special pharmacology efficiency for treatment or prevention of epilepsy and other neurological disorders, it has high curative effect, good endurance and without any action on metabolism in vivo of other anti epileptic medicines. The processes totally 6 routes for preparation of (S ) α ehtyl 2 oxo 1 pyrrolidinylacetamide are reviewed. An improved process by using methyl (S ) 2 amino 4 (methylthio)butyrate hydrochloride having normal stereo structure as starting material is recommended.