Synthesis of 1,2-Benzothiazines by a Rhodium-Catalyzed Domino C–H Activation/Cyclization/Elimination Process from S-Aryl Sulfoximines and Pyridotriazoles

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• 作者：Woo Hyung Jeon ; Jeong-Yu Son ; Ji Eun Kim ; Phil Ho Lee
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：July 15, 2016
• 年：2016
• 卷：18
• 期：14
• 页码：3498-3501
• 全文大小：403K
• 年卷期：0
• ISSN：1523-7052

文摘

A method for the synthesis of a large number of 1,2-benzothiazines bearing pyridyl as well as carbonyl groups is developed from rhodium-catalyzed carbene insertions into aromatic C–H bonds of S-aryl sulfoximines using pyridotriazoles by denitrogenative cyclization followed by the elimination of alcohols. The present method involves the N–H/C–H activation of simple alkyl aryl sulfoximines and has the advantages of a broad substrate scope, high functional group tolerance, and good regioselectivity.