National Creative Research Initiative Center for Catalytic Organic Reactions, Department of Chemistry, Kangwon National University , Chuncheon 24341, Republic of Korea.
Org Lett. 2016 Jul 15;18(14):3498-501. doi: 10.1021/acs.orglett.6b01750. Epub 2016 Jul 7.
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.
开发了一种从铑催化的碳烯插入 S-芳基亚磺酰胺的芳基 C-H 键，使用吡啶三唑通过脱氮环化以及醇消除来合成大量带有吡啶基和羰基的 1,2-苯并噻嗪的方法。该方法涉及简单的芳基烷基亚磺酰胺的 N-H/C-H 活化，具有广泛的底物范围、高官能团耐受性和良好的区域选择性。
