Selective Access to Heterocyclic Sulfonamides and Sulfonyl Fluorides via a Parallel Medicinal Chemistry Enabled Method

被引：19

作者：

Tucker, Joseph W. ^{[1
]}

Chenard, Lois ^{[1
]}

Young, Joseph M. ^{[1
]}

机构：

[1] Pfizer Worldwide Res & Dev, Worldwide Med Chem, Groton, CT 06340 USA

来源：

ACS COMBINATORIAL SCIENCE | 2015年 / 17卷 / 11期

关键词：

heterocyclic sulfonamides; sulfonyl fluorides; 3-step PMC protocol; rapid access; SULFUR-DIOXIDE; MILD; INHIBITORS; DISCOVERY; REAGENTS; DABSO; ROUTE; SALTS; ALKYL;

D O I：

10.1021/acscombsci.5b00120

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

A sulfur-functionalized aminoacrolein derivative is used for the efficient and selective synthesis of heterocyclic sulfonyl chlorides, sulfonyl fluorides, and sulfonamides. The development of a 3-step parallel medicinal chemistry (PMC) protocol for the synthesis of pyrazole-4-sulfonamides effectively demonstrates the utility of this reagent. This reactivity was expanded to provide rapid access to other heterocyclic sulfonyl fluorides, including pyrimidines and pyridines, whose corresponding sulfonyl chlorides lack suitable chemical stability.

引用

页码：653 / 657

页数：5

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