摘要
普瑞巴林作为一种新型γ-氨基丁酸受体拮抗剂,用于外周神经痛的治疗、部分癫痫发作的辅助治疗以及糖尿病性外周神经病引起的疼痛及疱疹后神经痛的治疗。对其合成方法进行综述,重点介绍外消旋化合物的拆分制备和不对称合成制备,并介绍了一些不对称合成的新方法,同时对普瑞巴林的合成前景进行了展望。
Pregabalin is a new type of γ-aminobutyric acid receptor antagonist, which is developedfor the treatment of peripheral neuropathic pain, aided treatment of partial epileptic seizure as well as treatment of pain caused by diabetic peripheral neuropathy and postherpetic neuralgia. In this paper, we introduce the preparation of pregabalin mainly through the preparation of enantioseparation of racemic compounds, asymmetric synthesis, synthesis by chiral source and desymmetrisation reaction. Among them, resolution of racemic compounds and asymmetric synthesis are mainly introduced, and some new methods of asymmetric synthesis in recent years are also introduced. At last, we look forward to the future of the prospects of pregabalin synthesis.
出处
《安徽化工》
CAS
2015年第5期11-18,21,共9页
Anhui Chemical Industry
关键词
普瑞巴林
手性拆分
不对称合成
Pregabalin
chiral resolution
asymmetric synthesis
