普瑞巴林的研究现状及其合成新方法

Recent advances in pregabalin and its new synthesis methods

目的概述普瑞巴林（Pregabalin）研究的新进展及其合成新方法。方法利用美国PubMed和FreePatentsOnline数据库以及中国知网（CNKI）和万方数据库检索关于普瑞巴林的研究，并参考新近的20余篇参考文献进行述评。结果美国PubMed数据库1997～2007年间累计收录了451篇与普瑞巴林有关的文献，英文文献400篇，占文献总数的88．69％，尚未检索到中文文献；Free Patents Online数据库统1994～2007年累计收录相关专利文献1012件，但是2004～2007年间，国内的CNKI和万方数据库与普瑞巴林有关的文献分别仅检索到10篇和14篇，2003年之前尚未检索到相关的文献报道；同时本文列举了10种普瑞巴林合成的新方法。结论普瑞巴林研究文献的快速增长及其合成新方法的不断涌现使与其治疗效果好，服用剂量少，几乎无副作用密切相关，但是中文的研究文献相对较少。

Aim To summarize the recent advances in pregabalin （ S-3-（aminomethyl）-5-methylhexanoic acid） and new synthesis methods. Method Online searches of the studies on pregabalin between 1994 and 2007 were performed with PubMed and FreePatentsOnline as well as China National Knowledge Infrastructure （CNKI） and Wanfang database＇s China Online Journals （COJ） between 1997 and 2007. The search term only included pregabalin. The review is written with more than 20 references on pregabalin. Results The statistical analysis of the articles on pregabalin indexed in PubMed, FreePatents Online, CNKI and Wanfang database＇s COJ showed that among the 451 papers in PubMed database between 1994 and 2007, the English papers account for 88.7%, no publication produced in the Chinese language was found. The FreePatentsOnline database embodied 1 012 patent bibliographies from 1994 to 2007, but during the period 2004 to 2007, only 10 and 14 articles related to pregabalin were found in CNKI and Wanfang database＇s COJ respectively, and no literature was found before the year 2003. New ten synthetic methods of pregabalin were presented. Conclusion The rapid increasing of publications （research papers and patents） on pregabalin is related to its satisfying therapeutic effect and fewer side effects, but the Chinese articles on pregabalin is relatively less.