Tri-coordinated phosphorus derivative, intermediate and preparation method thereof

Abstract

The invention discloses a tri-coordinated phosphorus derivative, an intermediate and a preparation method thereof, the structural formula of the tri-coordinated phosphorus derivative is as follows: R2 is phenol, pentafluorophenol and C1-4 alkoxy, and the alkoxy is optionally further substituted by 0-4 substituent groups of F, Cl, Br, I, C1-4 alkyl or C1-4 alkoxy; R3 is amino acids glycine, L-alanine, L-phenylalanine, L-isoleucine, L-leucine, L-valine, L-histidine, L-tryptophan and the methyl, ethyl, isopropyl, tert-butyl, diethyl ester groups and 2-ethylbutyl-L-alanine esters thereof; according to the invention, hexaethyl amine phosphite is taken as a starting raw material, the tri-coordinated phosphorus derivative is obtained through a one-pot three-step substitution reaction, no solvent needs to be replaced in the reaction, synthesis is simple, the intermediate does not need to be separated, and the problems of yield reduction and cost increase caused by post-treatment and purification, environmental pollution caused by three wastes and the like are reduced.

Description

technical field [0001] The invention relates to a tricoordinate phosphorus derivative, an intermediate and a preparation method. Background technique [0002] The tricoordinate phosphorus compound is sp 3 (Inequality) Hybrid triangular pyramid configuration, phosphorus atom with a lone pair of electrons. Trivalent phosphorus compounds have electrophilic, amphiphilic and dienophilic reaction characteristics, and can often form strong PO bonds during the reaction. For example, trialkylphosphines and trialkylphosphites are trivalent phosphorus compounds. Tricoordinate phosphorus compounds mainly include phosphorous acid (ester), phosphorous acid amide, trialkyl phosphite, phosphorus trihalide and the like. Among them, phosphite is phosphorous acid (HO) 3 Part or all of the hydroxyl hydrogen atoms in the P molecule are products of alkyl R substitution (esterification), which can be divided into monoalkyl phosphite ROP (OH) according to the degree of esterification 2 , dialk...

AI Technical Summary

Problems solved by technology

[0004] In the synthesis of the above-mentioned phosphorus-containing drugs, tetracoordinate phosphorus compounds are used as starting materials, the synthetic route is complex, the yield is low, the atom economy is poor, and the steps are cumbersome and produce a large amount of three wastes, which is not conducive to the sustainable development of the environment.

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