Chang Meng-Yang, Chen Han-Yu, Tsai Yu-Lin
Department of Medicinal and Applied Chemistry , Kaohsiung Medical University , Kaohsiung 807 , Taiwan.
Department of Medical Research , Kaohsiung Medical University Hospital , Kaohsiung 807 , Taiwan.
Org Lett. 2019 Mar 15;21(6):1832-1836. doi: 10.1021/acs.orglett.9b00422. Epub 2019 Feb 21.
In this paper, a novel and efficient route for the synthesis of α,β-bis-sulfonyl arylketones via an NHOH-HCl-mediated intermolecular umpolung α-methylsulfonylation of α-sulfonyl ketones with methylsulfoxides is described. A plausible mechanism is proposed and discussed. Various reaction conditions for this efficient, one-pot, environmentally friendly transformation were investigated.
本文描述了一种新颖且高效的合成α,β-双磺酰基芳基酮的路线，该路线通过NHOH-HCl介导的α-磺酰基酮与甲亚砜的分子间极性反转α-甲基磺酰化反应实现。提出并讨论了一种合理的反应机理。研究了这种高效、一锅法、环境友好型转化反应的各种反应条件。
