普瑞巴林的合成工艺研究摘要 癫痫是一类慢性、反复性、突然发作性的中枢神经系统疾病，发作时出现脑局部病灶兴奋性过高，产生高频放电并向周围扩散。
近年来，癫痫发病率逐渐上升，成为严重危害社会健康的一种疾病。
因此人们逐步将研究重点转移至关于癫痫的治疗方案上来。
加巴喷丁为GABA衍生物，口服吸收迅速，可通过血脑屏障，临床用于常规药物无法控制的或产生耐受性的癫痫，但加巴喷丁含有环己烷环，易于产生蓄积作用，毒性大，为此，辉瑞公司推出新药普瑞巴林，除治疗癫痫外，还对带状疱疹病毒引起的神经病变、三叉神经痛及其他非甾体镇痛药、吗啡等无效的疼痛有效，且能够缓解焦虑。
2010年，普瑞巴林被推荐为神经性疼痛的一线治疗药物。
本文通过查阅相关资料，选择最适于执行的合成路线，进行进一步研究。
关键词 普瑞巴林 合成 工艺 手性拆分AbstractEpilepsy is a kind of chronic central nervous system diseases which is repetitive andsudden-onsetable. When onset the local brain lesions excitement is too high, resulting in high frequency discharge and spread to the surrounding. In recent years, the incidence of epilepsy gradually increased with a serious harm to social health. So people gradually shift the focus of research on the treatment of epilepsy up. Gabapentin is a GABA derivative, which is rapidly absorbed by the blood brain barrier and is clinically used for epilepsy that can not be controlled or tolerated by conventional drugs. However, gabapentin contains a cyclohexane ring, which is prone to accumulate and is toxic. Then, Pfizer has launched a new drug pregabalin, not only on treatment of epilepsy, but also on herpes zoster virus-induced neuropathy, trigeminal neuralgia and other non-steroidal analgesics, morphine and other ineffective pain reducer. Whats more, it can ease anxiety. In 2010, pregabalin was recommended as a first-line treatment for neuropathic pain. This article through the relevant information, select the most suitable for the implementation of the synthetic route for further study.Key Pregabalin, Synthesis, Craft, Chiral split.癫痫是一类慢性、反复性、突然发作性的中枢神经系统疾病，发作时出现脑局部病灶兴奋性过高，产生高频放电并向周围扩散。
在发展中国家，每1000人中就有1～2人患病[1]，其中一种致病机制与gamma;-氨基丁酸（GABA）的分泌减少有关，对此，人们开发出拟GABA药物，作用于GABA受体，选择性阻断神经末梢Ca2 内流，从而降低神经细胞敏感性。
加巴喷丁为此类药物的代表。
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