Synthetic method of novel n-methylated sulfoximine derivatives

Abstract

A simple, clean and efficient method for preparing N-methylated sulfoximine derivatives is invented, which relates to the fields of pesticides, organic chemicals and fine chemicals. The method is essentially an organic synthesis reaction in which methyl radicals generated from peroxides are coupled with sulfoximine compounds to form new carbon-nitrogen bonds. The raw materials used are diphenyl sulfoximine and methylating reagent (peroxide) under the catalysis of copper, in common organic solvents, under heating conditions, react to obtain N-methylated sulfoximine derivatives thing. Using the method proposed by the present invention under heating and stirring conditions, the reaction time is 2-20 hours. The molar ratio of the raw materials is diphenylsulfoximine: methylating reagent = 1:0.5-3.0, reacting under heating conditions, and then undergoing simple post-treatment, the corresponding N-methyl can be obtained in a higher yield sulfoximine derivatives with a yield of 36‑87%. The present invention develops a novel N-methylation method based on a free radical process to obtain a series of N-methyl sulfoximine derivatives, which is simple in operation and convenient in post-processing. It is a simple and practical method for synthesizing such compounds.

Description

technical field [0001] The invention relates to the fields of pesticides, organic chemicals and fine chemicals, in particular to a carbon-nitrogen bond formation reaction using peroxide as a methylating reagent, and is a novel synthesis of N-methylated sulfoximine derivatives. method. Background technique [0002] As a very important functional group, the methyl group widely exists in many drug molecules and molecules of natural products. The introduction of the methyl group can significantly improve the solubility and physiological activity of the molecule. Traditional methylation methods mainly focus on using methyl iodide or methyl boron reagents as methylating reagents, but these traditional methylating reagents are toxic, volatile, unstable or easy to cause environmental pollution. disadvantages. In recent years, with the vigorous development of free radical chemistry, the research on methylation reaction has entered a new stage. Since Li's research group reported t...

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Problems solved by technology

In this method, the reaction time is long, and toxic substances such as formaldehyde are utilized

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