盐酸加巴喷丁的合成

Synthesis of Gabapentin Hydrochloride

环己酮与乙腈经Knoevenagel反应、Michael加成反应、Pd-C催化氢化还原和水解反应制得2-羟基-2-氮杂螺[4.5]癸烷-3-酮,再经RaneyNi催化氢化还原和水解、成盐制得抗癫痫药盐酸加巴喷丁,总收率14%。

Gabapentin hydrochloride, an antiepileptic drug, was synthesized by Knoevenagel reaction from cyclohexanone and acetonitrile, Michael addition reaction, Pd-C catalytic hydrogenation and hydrolysis to give 2-hydroxy-2-azaspiro [4.5] decan-3-one, which was subjected to reduction by Raney Ni catalytic hydrogenation, hydrolysis and salt formation with an overall yield of 14 %.