A kind of preparation method of pyrimido[1,6-a]indole heterocyclic derivative

A technology of 6-a and derivatives, applied in the direction of organic chemistry, can solve the problems of complex synthesis process, harsh reaction conditions, rare reaction raw materials, etc., and achieve the effects of high reaction yield, easy purification, and easy preparation
CN105481865BInactive Publication Date: 2016-10-05GUANGDONG UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
GUANGDONG UNIV OF TECH
Publication Date
2016-10-05
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a preparation method of a pyrimidine [1,6-a] indole heterocyclic derivative. The method comprises the following steps: under the condition that a rhodium catalyst, an additive silver salt and an additive acid exist, enabling an N-formamide indole compound and an a-carbonyl diazo compound to perform a cascade reaction in an organic solvent, and after the reaction is ended, separating and purifying to obtain the pyrimidine [1,6-a] indole heterocyclic derivative. The preparation method is mild in reaction condition, anhydrous and anaerobic conditions are not needed, and the operation is simple and convenient; besides, the reaction materials are easily prepared, and the substrate application scope is wide. By-products in the reaction only include nitrogen and water, and an economical, practical, green and environment-friendly novel method is provided for synthesizing the pyrimidine [1,6-a] indole heterocyclic derivative.
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Description

technical field

[0001] The invention belongs to the technical field of organic synthesis. More specifically, it relates to a preparation method of pyrimido[1,6-a]indole heterocyclic derivatives. Background technique

[0002] Nitrogen heterocyclic compounds widely exist in natural products and have good pharmaceutical and biological activities. Most of the existing drug structures contain various types of nitrogen heterocyclic skeletons. Pyrimidine compounds are an important class of substances in life activities, and widely exist in the human body and other organisms. For example, common components in genetic material nucleic acids contain three kinds of pyrimidine structures. In addition, indole derivatives have important applications in drug design. Therefore, with the combined ring structure of these two nitrogen-containing heterocyclic compounds, that is, compounds with pyrimido[1,6-a]indole heterocyclic structural units are effective in antimalarial, anti-inflammatory...

Claims

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