Aminoacid acidamide compounds and preparation thereof

A technology for amino acid amides and amine compounds, which is applied in the preparation of carboxylic acid amides, the preparation of organic compounds, chemical instruments and methods, etc. It can solve the problems of low reaction efficiency and stable protective groups, and achieve simple reaction methods and post-processing Easy and efficient effect
CN101328136AInactive Publication Date: 2008-12-24GUANGZHOU CHEM CO LTD CHINESE ACADEMY OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
GUANGZHOU CHEM CO LTD CHINESE ACADEMY OF SCI
Publication Date
2008-12-24
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses an amino acid amide compound and a preparation method thereof. Amino acid protected by FMOC and an acyl chloride reagent react to produce amino acid acyl chloride which is dissolved into a solvent with an appropriate polarity and reacts with a simple compound with primary amine and secondary amine so that the prepared amino acid amide compound can precipitate once forming in the reaction process, thereby reducing the contact of the FMOC and the amine; the whole process is short in the reaction time and fast in speed, thereby preventing the de-protection and realizing that the amino acid protected by the FMOC reacts with the simple amine on the premise without removing protective group; and the yield is up to more than 93 percent. The reaction method is simple, and has high efficiency and clean products as well as easy post treatment.
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Description

technical field

[0001] The invention relates to the field of organic synthesis, in particular to an amino acid amide compound and a preparation method thereof. Background technique

[0002] Amino acid amide compounds are a very important class of pharmaceutical intermediates and synthetic reagents, from which a variety of compounds with bactericidal and anti-tumor activities, enhanced immunity and fatigue resistance of biological organisms can be derived and synthesized, and are important for the synthesis of complex functional proteins. Raw materials are also important carriers for selective adsorption of chiral compounds, and have been widely concerned in the fields of chemistry, biology, and medicine.

[0003] At present, there are two main methods for synthesizing amino acid amides: one is to convert amino acid carboxyl groups into more active groups that are more conducive to ammonolysis, such as esters, acid anhydrides, etc., and then ammonolysis; Preparation by dehyd...

Claims

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