The preparation method of nevirapine

A technology of nevirapine and crude product, applied in the field of preparation of nevirapine, can solve the problems of large amount of diethylene glycol dimethyl ether, complicated operation and high boiling point of diethylene glycol dimethyl ether
CN103183678BActive Publication Date: 2016-07-20SHANGHAI DESANO CHEM PHARMA +3
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI DESANO CHEM PHARMA
Publication Date
2016-07-20

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Abstract

The invention discloses a preparation method for nevirapine. The method comprises the following steps: 1) reacting 2-chloro-N-(2-chloro-4-methyl-3-pyridyl)-3-pyridinecarboxamide with cyclopropylamine in an organic solvent in the presence of alkylamine so as to obtain a reaction mixture containing 2-cyclopropylamino-N-(2-chloro-4-methyl-3-pyridyl)-3-pyridinecarboxamide; and 2) mixing the reaction mixture obtained in the step (1) with an ether solvent or with a mixed solvent of the ether solvent and an aromatic hydrocarbon solvent in the presence of a base and allowing 2-cyclopropylamino-N-(2-chloro-4-methyl-3-pyridyl)-3-pyridinecarboxamide to undergo a cyclization reaction so as to obtain a reaction mixture containing nevirapine. The method may further comprise a step of nevirapine purification. The method provided by the invention has mild reaction conditions and is easy to control; process operation of the method is simple and safe; and the product nevirapine has good yield and high purity.
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Description

technical field

[0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a preparation method of nevirapine. Background technique

[0002] Nevirapine is a non-nucleoside reverse transcriptase inhibitor (Non-Nucleoside Reverse Transcriptase Inhibitor, NNRTI) of HIV-1, the chemical name is 11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyridine And[3,2-b:2',3'-e][1,4]diazepine-6-one, its structural formula is shown in formula (I).

[0003]

[0004] The preparation method of nevirapine has been disclosed in the patent US5,366,972 earlier, as shown in Scheme 1.

[0005]

[0006] Process 1

[0007] The biggest shortcoming of this technique is that in the substitution reaction of compound (2-chloro-N-(2-chloro-4-methyl-3-pyridyl)-3-pyridinecarboxamide) and cyclopropylamine shown in formula (III), cyclopropylamine The amount of used is too large (nearly 4 times the molar weight), it is easy to produce the by-product shown in the c...

Claims

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