A kind of synthetic method of aryl sulfone derivative
A synthesis method and a derivative technology are applied in the field of preparation of aryl sulfone derivatives, and can solve the problems of harsh reaction conditions, narrow substrate adaptation range, expensive catalytic system and the like
Active Publication Date: 2021-01-05
NANCHANG HANGKONG UNIVERSITY
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Problems solved by technology
[0010] The purpose of the present invention is to propose a novel method for preparing aryl sulfone derivatives in order to overcome the technical problems of narrow substrate adaptation range, expensive catalytic system, high reaction cost and harsh reaction conditions in the existing preparation method of aryl sulfone derivatives. Methods
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Embodiment 43
[0068] Add TEMPO (4 equivalents), and the remaining reaction conditions are the same as in Example 1. The target product was not generated as detected by GC.
Embodiment 44
[0070] Butylated hydroxytoluene (4 equivalents) was added, and the rest of the reaction conditions were the same as in Example 1. The isolated yield of target product was reduced to 23%.
[0071] The possible reaction mechanism is shown in the following formula:
[0072]
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The invention discloses a synthesis method of aryl sulfone derivatives. The method adopts organic electrosynthesis means, uses aromatic amine compounds as raw materials, reacts with sodium sulfinate compounds, and prepares various sulfonylated products. It has the advantages of wide adaptability and high yield of target product.
Description
technical field [0001] The application belongs to the field of organic electrosynthesis, and in particular relates to a preparation method of aryl sulfone derivatives. Background technique [0002] Aryl sulfone derivatives are important organic molecules that have been proven to have a variety of biological activities and are widely used in many fields such as organic synthesis, medicine, antibacterial, and dyes. For example, as a 5-HT6 receptor ligand for the treatment of central nervous system diseases or disorders (see 1) CN1217938C; 2) Synthesis of substituted diphenylsulfones and their structure-activity relationship with the antagonist of 5-HT6 receptors, Ilya Okun et al. Bioorg.Med.Chem.21 (2013) 4614-4627; 3) WO2005 / 051398A1; 4) US2013 / 0267536A1), as an antibacterial agent (see 5) US4829058), and / or as a dye component applied to keratin fibers Staining (see 6) US2016 / 0143826A1) and the like. [0003] Due to the wide application value of aryl sulfone derivatives, mo...
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IPC IPC(8): C25B3/00
CPCC25B3/00
Inventor 宋仁杰吴彦辰李金恒
Owner NANCHANG HANGKONG UNIVERSITY