中文摘要：

Pregabalin 1 (3-aminomethyl-5-methyl hexanoic acid) is a potent anticonvulsant related to the inhibitory neurotransmitter a-aminobutyric acid (GABA).1 In preclinical trials of anticonvulsant activity, pregabalin is three to ten times more potent than gabapentin. Therefore,pregabalin can be used for the potential treatment of several central nervous system (CNS) disorders including epilepsy, neuropathic pain, anxiety and social phobia. Many synthetic routes have been developed to prepare pregabalin.2-3 However, there is a need to explore novel, practical and better synthetic approaches to pregabalin. Herein we report a concise synthesis of (±)-pregabalin from hydrolysis of corresponding (a)-lactam, which was obtained from the intramolecular C-H insertion of N-cumyl a-diazoacetamide 4.