第十章 酰基化（The tenth chapter acylation）.docVIP

第十章 酰基化（The tenth chapter acylation） The tenth chapter is acylation The first section is an overview Acylation reaction and its importance 1. definition: acylation refers to the reactions of organic compounds with hydrogen atoms in the molecules of carbon atoms, nitrogen atoms, oxygen atoms, or sulfur atoms. The remaining part of an acyl - hydroxy acid in the removal of hydroxyl radicals (RCO -): e.g.: 2. classification: 3. research significance: (1) the properties and functions of the original compounds can be changed after the introduction of acyl groups on hydroxyl or amino functional groups. If the dyeing properties and fastness index of dyes have changed, the introduction of acyl groups in drug molecules can change the drug properties (aspirin); (2) it can be used to protect the amino group. After the reaction is finished, the acyl hydrolysis is removed. For example, when we introduce nitro groups on aniline, we usually substitute aniline with mixed acids for electrophilic substitution. But very susceptible to oxidation of aniline, and oxygen in the air can be colorless transparent liquid aniline in a few hours of oxidation of benzoquinone of the black dye, mixed acid is a strong oxidizer, it must first be protected in order to use the amino acid mixture nitration. Two. The most commonly used acylation agents are carboxylic acids, anhydrides and chlorides. The order of activity is as follows: chloride anhydride carboxylic acid. Second section N acylation reaction First, the basic principle of N acylation reaction, N acylation, is an important method for the preparation of amides. 1. N acylation reaction process Electrophilic substitution reaction. First, the positively charged carbon atoms in the carbonyl group of the acylated agent are electrophilic attacks on the non common electron pairs of the primary amine amino nitrogen atoms, forming a transition complex, and then decarboxylation of HX to form a carboxyl amide. When the X is OH, the acylation agent is