A kind of chiral sulfonamide derivative and its preparation method and application

A technology for sulfonamides and derivatives, applied in the field of chiral sulfonamide derivatives and their preparation, can solve the problems of unfavorable sulfonamide derivatives using industrial synthesis, non-recyclable chemical waste, low atom economy and the like , to achieve the effect of low cost, less waste and fewer reaction steps
CN109134402BActive Publication Date: 2022-05-24SUN YAT SEN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SUN YAT SEN UNIV
Publication Date
2022-05-24

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Abstract

The invention discloses a chiral sulfonamide derivative, the structural formula is as follows, wherein, R is an aryl group, an alkyl group, a cycloalkyl group, a heterocyclic group, a substituted aryl group, a substituted alkyl group, or a substituted heterocyclic group; Ar 1 Aryl, substituted aryl; Ar 2 Aryl, substituted aryl, heterocyclic aryl; Ar 3 Aryl, substituted aryl, heterocyclic aryl; the present invention uses sulfonamide, aryl diazoacetate, imine as raw material, 4Å molecular sieve as water absorbing agent, rhodium acetate, chiral phosphoric acid to form a catalytic system, In an organic solvent, the chiral sulfonamide derivatives are obtained through one-step reaction. The synthesis method of the invention has the advantages of high atom economy, high selectivity and high yield, and has mild reaction conditions and simple and safe operation. The chiral sulfonamide derivatives with two quaternary carbon centers of the present invention are potential drug active molecules, are widely used in the field of medicine, and have great application prospects.
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Description

technical field

[0001] The invention relates to the field of synthetic medicine and chemical industry, and mainly relates to an efficient, fast, concise and green chiral sulfonamide derivative and a preparation method and application thereof. Background technique

[0002] The sulfonamide structure is the core structural unit of a variety of drugs. It was recognized as an antibacterial drug by artificial synthesis from the very beginning, and now it has been widely used in antifungal, antiviral, antituberculous, antiparasitic, antitumor, and antiinflammatory. class of extremely important synthetic drugs. Based on their unique pharmacological activities, chiral sulfonamide derivatives also occupy an extremely important position in the development of new drugs. In the past few decades, a series of chiral induction, chiral resolution, etc. The method obtained chiral sulfonamide derivatives. However, the above-mentioned methods have problems such as harsh reaction conditions, c...

Claims

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