毕业论文课题相关文献综述
文 献 综 述 摘 要Lesinurad 是一种新型的痛风治疗药物，于2008 年由Ardea Biosciences 公司研发。
该药物主要通过抑制尿酸盐转运蛋白1（URAT1）增加尿酸的排泄来治疗痛风。
URAT1 被认为是存在于肾脏中用于转运尿酸盐的主要蛋白，能够将尿酸从管腔转入近曲小管上皮细胞并转化为单羧酸盐。
临床研究显示，Lesinurad 可被良好耐受，且能剂量相关性地降低血浆中的尿酸水平。
本论文主要介绍痛风相关背景、痛风的传统治疗药物、Lesinurad 的药物概况、合成路线，并着重介绍原料4-环丙基-1-萘胺盐酸盐的相关制备。
以1-溴萘为原料，通过格氏反应、硝化反应、硝基还原、成盐等一系列反应，合成Lesinurad的关键中间体4-环丙基-1-萘胺盐酸盐。
通过相关数据，对实验的设计进行优化，选出最佳的合成路线。
为将来Lesinurad新药的制备提供保障。
关键词：Lesinurad 痛风尿酸盐转运蛋白1中间体合成AbstractLesinurad is a new drug used for the treatment of gout. It was discovered fortuitously by Ardea Biosciences in 2008.Lesinurad could increase the excretion of uric acid by inhibiting the uric acid salt transport protein 1 (URAT1) to treat goutmainly.URAT1 isconsidered to be the main protein existing in kidney used to transport the uric acid s-alt, which is able to transfer theuric acid from the lumen proximal to tubule epithelialcells and translate into single carboxylic acid salt. In clinical trials,lesinuard has been well tolerated with dose-dependent reductions in serum uric acid. The drug situation,background, route of synthesis,and introduce route of synthesis of the 4-cyclopropyl-1-naphthylamine hydrochloride.1-bromine naphthalene as raw material, through grignardreaction, nitration, nitro reduction, into a series of reactions such as salt, synthesis int-ermediate of Lesinurad 4-cyclopropyl-1-naphthylamine hydrochloride.Through the relev-ant data, optimize the design of experiments, select the best synthetic route.The prepa-ration of Lesinurad new drugs in the future.key words: Lesinurad ;gout; uric acid salt transport protein 1;intermediate;synthesis痛风是一种全球性的代谢性疾病，无论是在欧美国家还是在亚洲各国，痛风的患病率都有逐年增高的趋势。
在我国男性和女性分别为1.26%～1.59%和0.30%～0.36%，而难治性痛风约占痛风总人数的1%，如在美国约610万例的痛风患者中，难治性痛风患者约有5万例左右。
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