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Related substance for synthetic building block of Afoxolaner and Fluralaner and synthetic method thereof

A technology related to substances and compounds, applied in the field of medical technology and drug synthesis, can solve the problems of compound synthesis and purification quality research and pharmacology and toxicology research that have not achieved satisfactory results

Pending Publication Date: 2021-07-16
WISDOM PHARM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the research on the related substances of Afraner and Freilaner at home and abroad is in the early stage, and the synthesis and purification of the compounds, the quality research of the finished products and the pharmacology and toxicology research have not achieved satisfactory results.

Method used

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  • Related substance for synthetic building block of Afoxolaner and Fluralaner and synthetic method thereof
  • Related substance for synthetic building block of Afoxolaner and Fluralaner and synthetic method thereof
  • Related substance for synthetic building block of Afoxolaner and Fluralaner and synthetic method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Add 10 mL of acetic anhydride and 2 g of 2-(1,3-dioxoisoindol-2-yl) acetic acid (Formula 3) into the reaction flask, replace with nitrogen 5 times, stir to raise the temperature to 100°C, and stir for 24 h. Slowly cool to 0°C, slowly add 100mL of water dropwise, stir for 3 hours and filter with suction to obtain a white solid, that is, impurity formula 6: 1.53g, yield 80%.

Embodiment 2

[0042]Add impurity formula 6 (96.7g), hydrazine hydrate (66.6g) and ethanol (300mL) into the reaction flask, heat up to 80°C for reflux reaction for 10h, cool the reaction solution to 45°C, filter with suction, remove insoluble matter, and obtain the filtrate, the filtrate Rotary evaporation under reduced pressure at around 60°C to remove the solvent, concentrate the resulting off-white solid, add 200mL of ethyl acetate to beat for 2h, filter with suction to obtain the filtrate, lower the temperature to 0°C, slowly add 375mL of hydrochloric acid in ethyl acetate solution dropwise, adjust the pH=5~6 , a large amount of white solid was precipitated. Filtrate with suction to obtain a white solid, and dry it in a blast oven at 40°C for 24 hours to obtain the impurity formula 9: 27.3g, with a yield of 42.6%.

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Abstract

The invention provides a synthetic method of related substances of 2-amino-N-(2, 2, 2-trifluoroethyl) acetamide which is a common key fragment for preparing raw material medicines, i.e., Afoxolaner and Fluralaner. The synthesis and research of the related substances are beneficial to improving the quality and medication safety of the raw material medicines, namely Afoxolaner and Fluralaner.

Description

technical field [0001] The invention belongs to the field of medical technology and drug synthesis, and more specifically relates to the common key fragment (also known as: synthetic building block, or Building Block) - 2-amino-N -Related substances of (2,2,2-trifluoroethyl)acetamide (related substances are also called impurities) and their preparation methods, and the related substances as key fragments of Frellana and Afraner--- -Use of 2-amino-N-(2,2,2-trifluoroethyl)acetamide product quality control standard. Background technique [0002] With the rapid development of my country's social economy, people's requirements for the quality of life are increasing day by day, and more and more families join the team of scientifically raising pets. According to rough statistics, the number of registered pet dogs in China has exceeded 75 million. The quantity exceeds 55 million pieces. However, pet dogs are active, like to play around, smell and lick, and are very susceptible to ...

Claims

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Application Information

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IPC IPC(8): C07C243/34C07C241/04C07D209/48
CPCC07C241/04C07C243/34C07D209/48
Inventor 杨志宇徐涛邱小龙张义森胡林邹平储玲玲左智伟刘文博曹雷
Owner WISDOM PHARM CO LTD
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