Preparation method of piribedil

A technology of piribedil and molar ratio, applied in the field of preparation of piribedil, can solve the problems of large amount of ruthenium reagent, high yield, low yield, etc., achieve mild reaction conditions, simple purification method, and product yield high rate effect
CN101735201BInactive Publication Date: 2012-05-30KANGYA OF NINGXIA PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
KANGYA OF NINGXIA PHARMA
Publication Date
2012-05-30
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a preparation method of piribedil. The method is characterized in that piperidine is used as a starting raw material, and piperonyl chlorine is prepared through a Blanc reaction; in addition, 2-cloro pyridine is used as a starting raw material to carry out single alkylation on piperazine to obtain 1-(2-pyrimidyl)piperazine; and the prepared piperonyl chlorine and the 1-(2-pyrimidyl)piperazine are subjected to an N-alkylation reaction to obtain the piribedil. The invention has the advantages that the raw material piperidine has low price and is easy to obtain; the reaction condition is moderate, and reactions of all steps can be quickly carried out at lower temperature without high temperature, high pressure or special catalysts; the yield of products is higher; a purification method is simple; the purity is better (the purity content of HPLC is not lower than 99.8 percent), and the like, thus the method is a route which has simple operation, higher yield, lower cost and stable quality and is suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the technical field of biopharmaceuticals, in particular to a preparation method of piribedil. Background technique

[0002] Pirabedil is suitable for Parkinson's patients and is a dopaminergic agonist that stimulates the post-synaptic D in the nigrostriatum of the brain. 2 Receptors and mesocortical, mesolimbic pathway D 2 and D 3 receptors, providing potent dopamine effects. Its structure is as follows:

[0003]

[0004] At present, the preparation of piribedil reported in the literature mainly contains the following methods:

[0005] Route 1

[0006]

[0007] route 2

[0008]

[0009] Route 3

[0010]

[0011] Route 4

[0012]

[0013] Route 5

[0014]

[0015] References: Route 1: CN1884280 (2006); Route 2: 1) J.Am.Chem.Soc.131(5), 1766-1774, 2009; 2) Tetrahetron letts.48(47), 8263-8265, 2007 ; Route 3: Tetrahedron Letts.47(15), 2549-2552, 2006; Route 4: 1) PL167397(1995); 2) Arch.Pharm.(weinheim...

Claims

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