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Synthesis method of diastereoisomer impurities in dolutegravir raw materials and intermediates

A technology of diastereoisomers and synthetic methods, which is applied in the field of synthesis of diastereomer impurities in dolutegravir raw materials and intermediates, can solve difficult problems and improve the quality of dolutegravir, etc. Achieve the effect of simple process and improved quality standard

Inactive Publication Date: 2019-08-16
BIONNA (BEIJING) MEDICAL TECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The research on the impurities of dolutegravir can be used for the qualitative and quantitative analysis of impurities in the production of dolutegravir, so as to improve the quality standard of dolutegravir and provide important guidance for the safe drug use of the people; while the existing Research rarely mentions the impurities of dolutegravir, so it is difficult to further improve the quality of dolutegravir

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  • Synthesis method of diastereoisomer impurities in dolutegravir raw materials and intermediates
  • Synthesis method of diastereoisomer impurities in dolutegravir raw materials and intermediates
  • Synthesis method of diastereoisomer impurities in dolutegravir raw materials and intermediates

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Embodiment Construction

[0028] In order to make the purpose, technical solutions and advantages of the embodiments of the present invention more clear, the technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments It is a part of embodiments of the present invention, but not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0029] figure 1 A flow chart showing the synthesis of diastereomeric impurities in the dolutegravir intermediate of the embodiment of the present invention. Such as figure 1 Shown, a kind of synthetic method of diastereomer impurity in dolutegravir intermediate, wherein said impurity of synthesis has the structure of followi...

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Abstract

The invention provides a synthesis method of diastereoisomer impurities in dolutegravir raw materials and intermediates. The synthesis method comprises the following steps: 1) with a compound V as a starting raw material, performing a reaction with a large-steric-hindrance protecting group under an alkaline condition to generate a compound VII; 2) carrying out alcoholysis on the compound VII and areaction solvent under an alkaline condition to generate a compound VIII; and 3) carrying out hydrolysis on the compound VIII and an alcohol solvent under an alkaline condition to obtain a compound IX. The invention provides the synthesis method of the diastereoisomer impurities in dolutegravir raw materials and intermediates, which is simple in process and easily available in raw materials. Theprepared new impurity can provide a reference substance for quality analysis of dolutegravir, so that the quality standard of dolutegravir is improved.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular to a method for synthesizing dolutegravir raw materials and diastereomer impurities in intermediates. Background technique [0002] Dolutegravir (DTG) is an antiviral drug developed and marketed by GSK in August 2013 for the treatment of HIV-1. It is a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor used in combination with other antiretroviral drugs to treat HIV-1 infection. DTG inhibits HIV integrase by binding to the integrase active site to block the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration; currently dolutegravir can be used alone or in combination with other drugs for the treatment of adults and HIV-1 infection in adolescents over 12 years old and children weighing more than 40 kg; therefore, it is of great significance to conduct research on dolutegravir. [0003] The research on the impurities of dolutegra...

Claims

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Application Information

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IPC IPC(8): C07D498/14
CPCC07D498/14Y02P20/55
Inventor 蔡报彬马晓光丁少珂杨静段红玉
Owner BIONNA (BEIJING) MEDICAL TECH CO LTD
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