Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies
A series of 24 benzothiadiazine derivatives with structural novelty were designed, synthesized and biologically evaluated as PI3Kδ-selective inhibitors. As a consequence of the structure-activity relationship (SAR) study, compounds 63 and 71 were identifi
Ma, Xiaodong,Wei, Jun,Wang, Chang,Gu, Dongyan,Hu, Yongzhou,Sheng, Rong
p. 112 - 125
(2019/03/17)
Synthesis of isomeric fluoronitrobenzene-sulfonyl chlorides
The synthesis of five hitherto unknown isomeric fluoronitrobenzenesulfonyl chlorides is described. The compounds are prepared from difluoronitrobenzenes by a two-step procedure. In the first step the starting compounds undergo a regioselective reaction with phenylmethanethiol giving rise to the corresponding thioethers. The oxidative cleavage of the latter with chlorine results in the sulfonyl chlorides in good yields. One example of a threefold sequential functionalization of 2-fluoro-6-nitrobenzenesulfonyl chloride showing the synthetic utility of the title compounds is provided.