A kind of synthetic method of 2-substituted pyridine drug intermediate compound

A synthetic method and compound technology, which is applied in the synthesis of pharmaceutical intermediate compounds and the synthesis of 2-substituted pyridine drug intermediate compounds, which can solve the problem of unsatisfactory reaction yield and rare synthetic methods of 2-substituted pyridine compounds and other issues, to achieve the effect of good industrial application prospects and value
CN104529879BInactive Publication Date: 2016-09-07侯芳霖
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
侯芳霖
Publication Date
2016-09-07
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a synthesis method of a 2-substituted pyridine-class drug intermediate compound shown in the formula (I) (please see the formula in the specification). The method includes the steps that when catalysts, ligand, alkali and additives exist, a compound with the formula (II) and a compound with the formula (III) react in an organic solvent so that the compound shown in the formula (I) (please see the formula in the specification) can be obtained, wherein R1, R2 and R3 are independently selected from H, halogen or C-C6 alkyl groups; the formula (please see the formula in the specification) is a C6-C10 aryl group which is not substituted or has 1-2 substitutent groups or is a C4-C10 heterocyclic radical which is not substituted or has 1-2 substitutent groups, and the substitutent grous are halogen, nitro or C1-C6 alkyl groups; Hal serves as the halogen. According to the method, the catalysts, the ligand, the alkali and the additives are properly selected and combined, and therefore a high yield is achieved, and the method has good industrial prospects and good application potentiality.
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Description

technical field

[0001] The invention relates to a method for synthesizing a drug intermediate compound, more specifically to a method for synthesizing a 2-substituted pyridine drug intermediate compound, and belongs to the technical field of organic synthesis and medicinal chemistry intermediates. Background technique

[0002] In the field of organic chemistry, pyridine structural modules widely exist in synthetic drugs, natural products, and functional materials, especially in pharmaceutical compounds containing heterocyclic or fused rings. Therefore, the development of such compounds plays a very important role in the design and synthesis of drugs and their intermediates.

[0003] The traditional synthetic method of pyridines mainly involves the condensation reaction of carbonyl compounds, but this method has some limitations, such as poor substrate expansion. In recent years, in order to improve the limitations of such methods, many researchers have developed a variety o...

Claims

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