|本期目录/Table of Contents|

[1]饶历,刘凤嗣,官仕龙*,等.阿托伐他汀钙中间体的合成工艺研究[J].武汉工程大学学报,2010,(12):10-12.[doi:10.3969/j.issn.16742869.2010.12.003]
　RAO Li,LIU Feng si,GUAN Shi long,et al.Research on the synthesis of 4（4Fluorophenyl）2（2Methylpropanoyl）4OxoN,β Diphenylbutanamide[J].Journal of Wuhan Institute of Technology,2010,(12):10-12.[doi:10.3969/j.issn.16742869.2010.12.003]
点击复制

阿托伐他汀钙中间体的合成工艺研究(/HTML)
分享到：

《武汉工程大学学报》[ISSN:1674-2869/CN:42-1779/TQ]

卷:
期数:
2010年12期
页码:
10-12
栏目:
化学与化学工程
出版日期:
2010-12-31

文章信息/Info

Title:
Research on the synthesis of 4（4Fluorophenyl）2
（2Methylpropanoyl）4OxoN,β Diphenylbutanamide
文章编号:
16742869(2010)12001003
作者:
饶历; 刘凤嗣; 官仕龙*; 周楷
武汉工程大学绿色化工过程省部共建教育部重点实验室,
湖北省新型反应器与绿色化学工艺重点实验室,湖北 武汉 430074
Author(s):
RAO Li;  LIU Fengsi;  GUAN Shilong;  ZHOU Kai
Key Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Lab of Novel
Chemical Reactor and Green Chemical Technology, Wuhan Institute of Technology, Wuhan 430074, China
关键词:
药物化学; 化学合成; 阿托伐他汀; HMGCoA还原酶抑制剂
Keywords:
medicinal chemistry;  chemical synthesis;  atorvastatin;  HMGCOA reductase inhibitor
分类号:
TQ463;R972+.6
DOI:
10.3969/j.issn.16742869.2010.12.003
文献标志码:
A
摘要:
以异丁酰乙酸甲酯为原料经苯胺胺解得到4甲基3氧N苯戊酰胺,然后与苯甲醛发生反应,得到4甲基3氧 N苯2(苯亚甲基)戊酰胺,再以溴化噻唑为催化剂,与对氟苯甲醛发生Stetter反应,得到阿托伐他汀钙的关键中间体4（4氟苯基）2（2甲基丙酰基）4氧代N,β二苯基丁酰胺.该方法操作简便,收率较高,各主要化合物结构经核磁共振氢谱确证.
Abstract:
4（4Fluorophenyl）2（2methylpropanoyl）4oxoN,βdiphenylbutanamide is a key intermediate of atorvastatin. Methyl isobutyryl acetate was transformed into 4methyl3oxoNpentanamide by reaction with aniline; the resulting product could undergo Knoevenagel condensation with benzaldehyde giving 4mehtyl3oxoNPhenyl2(Phenylmethylene)Pentanamide,which could further undergo Stetter reation with pfluorobenzaldehyde thus giving aceess to the final molecule 4（4Fluorophenyl）2（2methylpropanoyl）4oxoN,β diphenylbutanamide. The synthetic route were easily available and the yield was reasonable. The structures of the main intermediates were identified by 1H NMR.

参考文献/References:

［1］黄震华.新型降脂药物阿托伐他汀［J］.中国新药杂志,2000（1）:5456.
［2］周晋武,汪钊.阿托伐他汀手性中间体合成研究进展［J］.化学与生物工程,2008（5）:14.
［3］尹大力,李春.（+）对氟2（2甲基丙酰胺）4氧N,3二苯基苯丁酰胺的新合成方法以及其中的中间体:中国,1325844A［P］.2001-12-12.
［4］Kelvin L, Baumann, Donald E, et al. The convergent synthesis of CI 981, an optically active, highly potent, tissue selective inhibitor of HMGCoA reductase［J］.Tetrahedron Letters,1992:22832284.
［5］Charles JK, Weissberger A.Organic Syntheses:Coll Vol 3 ［M］.New York:John Wiley Sons Inc,1961:108112.
［7］Butler D E,Deering C F,Millar A,et al. Process for trans6［2(substitutedPyorrlyl)alkyl］pyran2one inhibitors of cholesterol synthesis:US,5097045［P］.1992-3-17.

相似文献/References:

备注/Memo

备注/Memo:
作者简介：饶历（1986），女，湖北仙桃人，硕士研究生.研究方向：药物及药物中间体合成、药物制剂、水性涂料.指导老师：官仕龙，副教授，硕士研究生导师.研究方向：水性涂料、水性胶粘剂、各种助剂、医药和农药中间体、功能高分子材料.
更新日期/Last Update: