4.8 Article

Asymmetric Synthesis of Chiral Sulfoximines via the S-Arylation of Sulfinamides

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JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 141, 期 49, 页码 19263-19268

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AMER CHEMICAL SOC
DOI: 10.1021/jacs.9b11298

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  1. JSPS Kakenhi [JP17H06450, JP26220803, JP18H01975]
  2. Japan Society for the Promotion of Science (JSPS)

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Optically active sulfoximines are a promising substance in medicinal chemistry. However, a methodology for preparing chiral sulfoximines in a stereoselective manner has been underdeveloped. Here, we report an asymmetric synthesis of chiral sulfoximines having an aryl group by the newly developed sulfur-selective arylation of easily accessible chiral sulfinamides. The utility of the present method is demonstrated by the asymmetric synthesis of a key intermediate of a COX-2 inhibitor.

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