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Preparation method for N-nitrosamine genotoxic impurity of varenicline tartrate

A technology of varenicline tartrate and genotoxicity, applied in the direction of organic chemistry and so on

Inactive Publication Date: 2021-12-14
JIANGSU SINOBIOPHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] There is no relevant literature report on the N-nitrosamine impurity or its preparation method in the prior art

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  • Preparation method for N-nitrosamine genotoxic impurity of varenicline tartrate
  • Preparation method for N-nitrosamine genotoxic impurity of varenicline tartrate
  • Preparation method for N-nitrosamine genotoxic impurity of varenicline tartrate

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Embodiment Construction

[0020] The technical solution of the present invention will be further described below in conjunction with the accompanying drawings. The embodiments and related experimental data described below with reference to the figures are only exemplary, and are intended to explain the present invention, but should not be construed as limiting the present invention. The disclosure below provides many different embodiments to be used for realizing technical effect of the present invention, in order to simplify the disclosure of the present invention, only provide several kinds of embodiments that adopt specific experimental parameters hereinafter, but those of ordinary skill in the art can realize Application of other processes and / or use of other materials. In this specification, references to a schematic representation of an embodiment do not necessarily refer to the same implementation or example. Furthermore, specific features or features described may be combined in any suitable m...

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Abstract

The invention provides a preparation method for an N-nitrosamine genotoxic impurity of varenicline tartrate. The preparation method comprises the following steps: with ammonium formate as a hydrogen donor, carrying out reduction reaction on dinitrate under the catalysis of palladium carbon to obtain a diamino compound, carrying out a cyclization reaction on the diamino compound and an aqueous glyoxal solution to obtain a cyclization product, carrying out a hydrolysis reaction on the cyclization product under the action of sodium hydroxide, removing trifluoroacetyl to obtain free alkali, and finally, subjecting the free alkali to reacting with sodium nitrite under the catalysis of protonic acid to obtain the N-nitrosamine impurity. According to the invention, the technical vacancy of preparation methods for the impurity at present is filled in, the prepared high-purity impurity can be applied as a control sample to the drug impurity research and production quality control process of varenicline tartrate, and a guarantee is provided for the genotoxicity research and comprehensive quality control of a varenicline tartrate bulk drug.

Description

technical field [0001] The invention relates to a preparation method of varenicline tartrate N-nitrosamine genotoxic impurity, which belongs to the technical field of chemical industry and pharmacy. Background technique [0002] Varenicline tartrate is a partial agonist that selectively acts on α4β2 nicotinic receptors, and is mainly used clinically as a drug for smoking cessation in adults. Varenicline selectively binds to the α4β2 nicotinic acetylcholine receptor, has a high affinity to the receptor, and subtype binding produces an agonistic effect, and at the same time blocks the binding of nicotine to the receptor to play a role in smoking cessation. [0003] The synthetic method of varenicline tartrate published in the prior art is basically the same, all of which are based on 2,3,4,5-tetrahydro-1,5-methylene-1H-3-benzazepine As the starting material, first protect the amino group with trifluoroacetyl group, then introduce two ortho nitro groups on the benzene ring th...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/08
CPCC07D471/08
Inventor 黄乐群汪静王磊
Owner JIANGSU SINOBIOPHARMA
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