摘 要

近年来，肠易激综合征一直没有专门治疗的特效药，一直困扰着全球的很多患者，本文简介了Eluxadoline，在医药领域有重要的意义，是针对腹泻型肠易激综合征的一种特效药物，Eluxadoline是一种口服μ-阿片受体激动剂和δ-阿片受体拮抗剂,有强大的止泻剂、镇痛活性。医药前景广大，市场需求很大，研究意义非凡，并详细介绍了Eluxadoline的合成路线，合成路线复杂，中间产生的杂质较多，反应包括取代，水解，氧化还原等反应类型，反应需要大量不同的催化剂，氧化剂，还原剂等。同时介绍了工业合成Eluxadoline的的步骤方法。以及对产品的检测。有液相色谱，质谱，核磁谱。

关键词：发展；前景；合成；制备，检测

The synthesis of Eluxadoline synthesis

ABSTRACT

Irritable bowel syndrome in recent years, there has been no specific, special treatment has been plagued by many patients around the world, this paper introduced the Eluxadoline, has an important significance in the field of medicine, against diarrhea type irritable bowel syndrome is a kind of special drug, Eluxadoline is an oral mu opioid agonist and delta - opioid receptor antagonist, has a strong antidiarrheal agent and analgesic activity. Pharmaceutical prospects for the market demand is very big, research significance, and introduced the synthetic route of Eluxadoline, complex synthetic route, the middle of impurity is more, including substitution, hydrolysis, oxidation reduction reaction type, such as reaction requires a lot of different catalyst, oxidant, reductant, etc. This paper introduces the steps of the industrial synthetic Eluxadoline. And product testing. There is liquid chromatography, mass spectra, nuclear magnetic spectrum.

Key words:development; Prospects; Synthesis; preparation;detection

目录

摘要...................................................................................................................................................2

ABSTRACT.......................................................................................................................................3

1. 简介................................................................................................................................................5

1.1背景.........................................................................................................................................5

1.1.1肠易激综合征..................................................................................................................5

1.1.2伊卢多啉..........................................................................................................................6

1.2伊卢多啉在医药领域运用.....................................................................................................6

1.3发展与展望.............................................................................................................................7

1.4研究意义.................................................................................................................................8

1. 伊卢多啉的合成............................................................................................................................9

2.1伊卢多啉的合成路线.............................................................................................................9

2.2注意事项.................................................................................................................................10

3.合成实验........................................................................................................................................10

3.1 Elu-3的合成...........................................................................................................................11

3.2 Elu-4的合成...........................................................................................................................12

3.3 Elu-5的合成...........................................................................................................................13

3.4 Elu-6的合成...........................................................................................................................13

3.5 Elu的合成..............................................................................................................................14

4.产品检测........................................................................................................................................14

4.1HPLC谱图................................................................................................................................14

4.2质谱........................................................................................................................................15

4.3核磁共振谱............................................................................................................................15