期刊
ACS COMBINATORIAL SCIENCE
卷 17, 期 11, 页码 653-657出版社
AMER CHEMICAL SOC
DOI: 10.1021/acscombsci.5b00120
关键词
heterocyclic sulfonamides; sulfonyl fluorides; 3-step PMC protocol; rapid access
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.
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