107517-59-9Relevant academic research and scientific papers
SO2F2-mediated deoxygenative C2-sulfonylation of quinoline N-oxides with sodium sulfinates
Ai, Chengmei,Liao, Xudong,Zhou, Yi,Yan, Zhaohua,Lin, Sen
, (2020)
A mild and efficient method for deoxygenative C2-sulfonylation of quinoline N-Oxides in the presence of a base has been developed employing extremely inexpensive SO2F2 as an activator and sodium sulfinate as nucleophilic sulfonylation source. It is noteworthy that the reaction proceeded well under metal- and oxidant-free conditions to give a variety of 2-sulfonylquinolines in medium to good yields.
Synthesis of substituted diphenyl sulfones and their structure-activity relationship with the antagonism of 5-HT6 receptors
Ivachtchenko, Alexandre,Golovina, Elena,Kadieva, Madina,Mitkin, Oleg,Tkachenko, Sergei,Okun, Ilya
, p. 4614 - 4627 (2013/07/26)
Substituted diphenyl sulfones (10a-n) were synthesised, and the structures were confirmed by NMR, LC-MS and X-ray crystallography. Their antagonistic activities towards 5-HT6 receptor were assessed in a cell-based functional assay. Diphenyl sulfone 10a, in spite of being the smallest and simplest known sulfonyl-containing 5-HT6R antagonist, showed a strong potency (Ki = 1.6 μM). Its derivative with a methylamine substituent, 10g (N-methyl-2-(phenylsulfonyl)aniline), was ～66-times as active as diphenyl sulfone (Ki = 24.3 nM). Addition of a piperazinyl moiety in the para-position relative to the sulfonyl group in compound 10m (N-methyl-2-(phenylsulfonyl)-5-piperazin-1-ylaniline) led to a further 150-fold increase in potency (Ki = 0.16 nM) to block the serotonin-induced response of HEK-293 cells that were stably transfected with the human recombinant 5-HT6 receptor.
