论文总字数：15432字

摘 要

据WHO近年来的统计数据来看,在全世界范围，丙型肝炎病毒（Hepatitis C Virus，简称HCV）感染携带者已经超过了1.7亿, 并依旧在增加中，感染者的增加速率为350万人/年¹。而在中国，HCV感染携带者也超过4千万（312%）。依巴司韦Elbasvir(MK-8742)是新一代的对慢性丙肝病毒(HCV)具有抑制功能的药物，它在2015年时通过美国FDA，是由美国默沙东公司研发的，目的与用途就是用于对慢性丙肝的治疗²。而在合成Elbasvir的过程中会产生烯酰胺中间体，本文就构建依巴司韦烯酰胺以及不同手性催化剂对其进行不对称氢化还原而得的产物结构及ee值进行了研究。

关键词：依巴司韦Elbasvir 烯酰胺 不对称氢化还原

Synthesis and asymmetric reduction of

Elbavir enamide

Abstract

More than 170 million people are infected with hepatitis c virus (HCV) worldwide,with 3.5 million new infections each year,according to the WHO.In China,nearly 40 million people (312%) are infected with HCV.Elbasvir(mk-8742) is a new generation of drugs that can inhibit chronic hepatitis c virus (HCV).It was developed by MSD and it was approved by the FDA in 2015.Elbasvir is used to treat the chronic hepatitis c.In the process of synthesizing it,the intermediate of enamine will be produced.In this paper,we have studied the synthesis of Elbasvir enamine.And we also have studied the structures and ee(%) of the products obtained by asymmetric hydrogenation reduction with different chiral catalysts.

Keywords:Elbasvir Enamine Asymmetric hydrogenation reduction

目录

摘要 ----------------------------------------------------------------------------------------------ǀ

Abstract -----------------------------------------------------------------------------------------ǁ

第一章 文献综述 --------------------------------------------------------------------------

1.1 引言 -----------------------------------------------------------------------------------------

1.2 Elbasvir的现代新合成法 ----------------------------------------------------------------

1.3 Elbasvir的结构特征 ----------------------------------------------------------------------

1.4 Elbasvir合成过程中产生的几种烯胺中间体 ----------------------------------------

1.5 本课题研究内容 --------------------------------------------------------------------------

1.5.1 研究内容 -------------------------------------------------------------------------------

1.5.2 拟采用合成手段 ----------------------------------------------------------------------

1.5.3 对烯胺进行不对称还原研究方法 -------------------------------------------------

第二章 烯胺的合成 ----------------------------------------------------------------------

2.1 概述 -----------------------------------------------------------------------------------------

2.2 合成2,5-二溴苯乙酸（以对溴苯胺为原料）-------------------------------------------

2.2.1 主要试剂与设备 ----------------------------------------------------------------------

2.2.2 实验步骤 -------------------------------------------------------------------------------

2.3 合成烯胺（以2,5-二溴苯乙酸为原料）-------------------------------------------------

2.3.1 主要试剂与设备 ----------------------------------------------------------------------

2.3.2 实验步骤 -------------------------------------------------------------------------------

2.4 结果与讨论 --------------------------------------------------------------------------------

第三章 烯胺的不对称氢化还原 ----------------------------------------------------

3.1 前言 -----------------------------------------------------------------------------------------

3.2 实验部分 -----------------------------------------------------------------------------------

3.2.1 主要试剂与设备 -------------------------------------------------------------------

3.2.2 实验步骤 ----------------------------------------------------------------------------

3.3 结果与讨论 --------------------------------------------------------------------------------

第四章 总结与展望 ----------------------------------------------------------------------

4.1 总结 -----------------------------------------------------------------------------------------

4.2 展望 -----------------------------------------------------------------------------------------

参考文献 ----------------------------------------------------------------------------------------

致谢 -----------------------------------------------------------------------------------------------

1. 文献综述

1.1 引言

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