Method for generating amido bond

Abstract

A generation method of amido bond relates to a method for forming amido bond, which comprises in the presence of phosphoryl halide, N, N-dimethylpyridine (DMAP) and organic alkali, reacting dimethylpyridine and free amine or amine salt in organic solvent to generate amido bond, with low cost, simple process, high yield, non racemic generation, simple operation and support for industrial production. The invention comprises dissolving carboxyl acid and free amine or carboxyl acid and amine salt into organic solvent to be reacted, adding organic alkali and catalyst N, N-dimethylpyridine, adding phosphoryl halide, generating amido bond between the carboxy group of carboxyl acid and amido of amine to obtain the slat and hydrochlorate of relative amide and organic alkali.

Description

technical field The present invention relates to a method for forming an amide bond, comprising reacting a carboxylic acid with a free amine or an amine salt in an organic solvent in the presence of a phosphoryl halide, N,N-lutidine (DMAP) and an organic base to form amide bond method. Background technique Typically, amide bond formation is achieved by reacting a carboxylic acid with a free amine or amine salt in the presence of a coupling agent and a base. However, the existing coupling agents often encounter problems such as many operation steps, difficulty in dissolving, and high price. Especially when peptide bonds are formed, problems such as low yield and easy racemization are encountered (see: 1. Albericio, F.; Chinchilla, R.; Dodsworth, D.J. Najera, C. Org. Prep. Proced. Int. 2001, 33, 203-303; 2. Montalbetti. C.A.G.N.; Falque, V. Tetrahedron, 2005, 61, 10827-10852). Therefore, need a kind of method that raw material is cheap and easy to obtain, productive rate i...

AI Technical Summary

Problems solved by technology

However, the existing coupling agents often encounter problems such as many operation steps, difficulty in dissolving, and high price.

Especially when peptide bonds are formed, problems such as low yield and easy racemization are encountered (see: 1. Albericio, F.; Chinchilla, R.; Dodsworth, D.J. Najera, C. Org. Prep. Proced. Int. .2001, 33, 203-303; 2. Montalbetti.C.A.G.N.; Falque, V.Tetrahedron, 2005, 61, 10827-10852)

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