Efficient and scalable synthesis of ethyl 2,6-dichloro-5-fluoronicotinoyl acetate using the Blaise reaction as a key step

被引：14

作者：

Choi, BS ^{[1
]}

Chang, JH ^{[1
]}

Choi, HW ^{[1
]}

Kim, YK ^{[1
]}

Lee, KK ^{[1
]}

Lee, KW ^{[1
]}

Lee, JH ^{[1
]}

Heo, T ^{[1
]}

Nam, DH ^{[1
]}

Shin, H ^{[1
]}

机构：

[1] LG Life Sci Ltd R& D, Div Chem Dev, Taejon 305380, South Korea

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2005年 / 9卷 / 03期

关键词：

D O I：

10.1021/op050012a

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

An efficient synthesis of 2,6-dichloro-5-fluoronicotinoyl acetate (1) has been accomplished in a single step using the Blaise reaction of ethyl bromoacetate with 3-cyano-2,6-dichloro-5-fluoropyridine (4). Use of methanesulfonic acid as an in situ activator of zinc removed the induction period of the Blaise reaction to render it safe and viable for a large-scale operation.

引用

页码：311 / 313

页数：3

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