Synthetic method of novel N-methylated sulfoximine derivative

Abstract

A simple, clean and high-effective synthetic method of a novel N-methylated sulfoximine derivative is provided in the invention. The invention relates to the fields of pesticides, organic chemical engineering and fine chemical engineering. The method essentially is an organic synthesis reaction that a methyl free radical, which is generated from peroxides, and a sulfoximine compound are subjected to free radical coupling to form new C-N bonds. The method includes the step of carrying out a reaction to obtain the N-methylated sulfoximine derivative in a common organic solvent under a heating condition from the raw materials including diphenyl sulfoximine and a methylating reagent (peroxides) under the catalysis by copper. The method is 2-20 h in reaction time under a heating and stirring condition. The molar ratio of the raw materials is that the diphenyl sulfoximine to the methylating reagent is 1:0.5-3.0. The raw materials are reacted under the heating condition and then reaction products are subjected to simple after treatments to obtain the N-methylated sulfoximine derivative at a yield being 36-87%. The invention develops a series of N-methylating methods based on a free radical process to prepare a series of N-methylated sulfoximine derivatives. The method is simple in operation and after treatments, and is simple and practical in synthesis of these 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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