Simple method for synthesizing imidazo (1,2-a) pyridine derivatives

A technology for synthesizing imidazole and 2-a, which is applied in organic chemistry and other fields, can solve problems such as unfavorable industrial production, high reaction temperature, and long reaction time, and achieve good regioselectivity, mild reaction conditions, and short process flow
CN103848830AActive Publication Date: 2014-06-11JINTAN DEPEI CHEM
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
JINTAN DEPEI CHEM
Publication Date
2014-06-11

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Abstract

The invention relates to a simple method for synthesizing imidazo (1,2-a) pyridine derivatives. The method comprises the steps of: dissolving reactants including 2-aminopyridine or derivatives thereof and beta-nitrostyrolene or derivatives thereof into a solvent, and preparing the imidazo (1,2-a) pyridine at 25DEG C-150DEG C by taking iodine and pyridine as catalysts and t-butylhydroperoxide as an oxidant, wherein the mole ratio of 2-aminopyridine or derivatives thereof to beta-nitrostyrolene or derivatives thereof to iodine to t-butylhydroperoxide to pyridine is 1:(0.9-1.5):(0.1-0.5):(1-4):(0.3-1). The simple method uses low-cost and easily available reaction raw materials and catalysts, is short in technological process, mild in reaction conditions, and easy for the expansion of the product structure; the target product can be obtained in one step through the implemented serial reaction; the catalyst is a nonmetal system, thus having metal residue risk. The method is high-efficiency, economical and environmentally-friendly synthesis route.
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Description

technical field

[0001] The invention relates to the technical field of organic synthesis, in particular to the preparation of pharmaceutical compounds imidazo[1,2- a ] pyridine synthesis technology, specifically proposed the synthesis of imidazo[1,2- a ] A facile method for pyridine derivatives. Background technique

[0002] imidazo[1,2- a ] Pyridine, as an important class of heterocycles, is the core fragment of many important compounds in chemical agents. Because some derivatives containing these core fragment skeletons have antibacterial, antiviral, anti-inflammatory, anti-ulcer, anti-tuberculosis, anti-cancer and other active characteristics, they have attracted widespread attention in the fields of pharmacy, biology, and medicine. Prior art, for imidazo[1,2- a The synthetic techniques of ]pyridine have been studied to a certain extent, and it is reported that there are synthetic methods using a variety of different precursors and strategies: For example: using β-dic...

Claims

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