Use of (Z)-β-(2-Fluorobenzenesulfonyl) vinylamines as Novel Synthons in the Synthesis of 1, 4-Benzothiazine Derivatives

GC Tsui, Y Singjunla, M Lautens

Index: Tsui, Gavinchit; Singjunla, Yuttapong; Lautens, Mark Synthesis, 2012 , vol. 44, # 9 p. 1359 - 1364

Full Text: HTML

Citation Number: 6

Abstract

Abstract A novel synthetic route for arylated 1, 4-benzothiazine derivatives has been developed. This method utilizes a key intramolecular nucleophilic aromatic substitution step of the corresponding (Z)-β-(2-fluorobenzenesulfonyl) vinylamine intermediate to construct the benzothiazine ring. A wide range of aryl and heteroaryl substituent groups can be installed from commercial boronic acids. Both mono-and diarylated products have been ...