Method for preparing PINO (phthimide-n-oxyl) derivatives through directly coupling NHPI (n-hydroxyphthalimide)and benzyl-containing compounds under non-metal catalysis

Abstract

The invention discloses a method for preparing PINO (phthimide-n-oxyl) derivatives through directly coupling NHPI (n-hydroxyphthalimide) and benzyl-containing compounds under non-metal catalysis. According to the method, under the nitrogen protection, the benzyl-containing compounds, N-hydroxyphthalimide and K2S2O8 take a one-pot reaction under the catalysis of tetraalkyl ammonium salts to produce PINO derivatives. By using the method, the next step of reaction is performed under the mild condition; the PINO derivatives are synthesized at a high yield; in addition, the cost is low; the operation is simple; the industrial protection requirements are met.

Description

technical field [0001] The invention relates to a method for preparing PINO derivatives, in particular to a method for preparing PINO derivatives by direct coupling of NHPI and benzyl-containing compounds under non-metal catalysis, and belongs to the field of organic synthesis. Background technique [0002] Free radical chemistry has been a research hotspot for many years because it does play an important role in organic synthesis and industrial applications. It is well known in the art that N-hydroxyphthalimide (NHPI) can generate highly reactive N-oxyphthalimide (PINO) free radicals, which can be used as catalysts or participate in various types of coupling reactions. joint reaction. Some PINO compounds can be easily converted into the corresponding alcohols or hydroxylamines, both of which are very useful intermediates in drug synthesis. In the prior art, several methods for synthesizing PINO compounds have been reported, mainly by using metal salts to catalyze the reac...

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Problems solved by technology

[0008] In view of existing methods for synthesizing PINO derivatives, transition metal catalysts and highly active peroxides are used as oxidizing agents, and the cost is high, the safety factor is low, the yield is low, and it is difficult to be suitable for industrial production. The purpose of the present invention is to provide a A method for synthesizing PINO derivatives with NHPI and benzyl-containing compound raw materials in one step with high yield under mild conditions, the method is low in cost, simple in operation, and meets the requirements of industrial production

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