Synthesis method of brivaracetam impurity

A synthesis method and impurity technology are applied in the field of synthesis of brivaracetam impurities, can solve the problems of low drug content, reduced drug activity, increased toxic and side effects, etc., and achieve the effects of low cost, high yield and simple operation process

Pending Publication Date: 2022-03-22
南京望知星医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Too much impurities will make the content of the drug low, and at the same time, the activity of the drug will be reduced, and the toxic and side effects will increase significantly.

Method used

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  • Synthesis method of brivaracetam impurity
  • Synthesis method of brivaracetam impurity
  • Synthesis method of brivaracetam impurity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Dissolve 20 g of compound ① in 500 ml of ethanol, add 9.00 g of sodium ethoxide, and react at 50°C for 8 hours. TLC monitored the completion of the reaction. Spin to dry, add 100 ml of water, extract with dichloromethane, dry and spin to obtain 20 g of pure compound ②, with a purity of 95% and a yield of 73.56%.

Embodiment 2

[0035] Dissolve 30 g of compound ① in 500 ml of ethanol, add 40 g of sodium acetate, and react at 80°C for 24 hours. TLC monitored the completion of the reaction. Spin to dry, extract with dichloromethane, dry and spin to obtain 31 g of pure compound ②, with a purity of 96% and a yield of 76.01%.

Embodiment 3

[0037] Dissolve 50 g of compound ① in 1000 ml of ethanol, add 100 g of potassium acetate, and react at 90°C for 30 hours. TLC monitored the completion of the reaction. Spin to dry, extract with dichloromethane, dry and spin to obtain 55 g of pure compound ②, with a purity of 95% and a yield of 80.91%.

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Abstract

The invention belongs to the technical field of organic synthesis, and particularly relates to a brivaracetam impurity synthesis method which comprises the following specific steps: step 1, dissolving a raw material compound (1) in an organic solvent A, adding alkali, and reacting at 50-100 DEG C for 8-48 hours; step 2, dissolving the product compound (2) prepared in the step 1 in an organic solvent B, adding alkali and a silicon reagent, and reacting at 10-70 DEG C for 1-24 hours to prepare a target product compound (3); the brand new brivaracetam impurity synthesis method provided by the invention can accelerate the detection and analysis process of raw material medicines, and the synthesis method is reasonable in process design, simple in operation process, cheap in used raw materials, high in yield and low in cost.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis, in particular to a method for synthesizing brivaracetam impurities. Background technique [0002] Brivaracetam chemical name: (αS,4R)-α-ethyl-2-oxo-4-propyl-1-pyrrolidineacetamide, CAS: 357336-20-0, specific structural formula as follows: [0003] [0004] Brivaracetam was approved by the U.S. Food and Drug Administration (FDA) on February 19, mainly for the adjuvant treatment of partial seizures in patients aged 16 and above. Compared with the previous generation Chemicalbook drug levetiracetam, brivaracetam has a similar chemical structure and mechanism of action and is the first antiepileptic drug approved by the FDA for the treatment of partial seizures since 2013 [0005] Brivaracetam (brivaracetam) is a highly selective and affinity synaptic vesicle 2A ligand approved for the treatment of partial seizures in adults and adolescents over 16 years old with epilepsy, with or with...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F7/18
CPCC07F7/188
Inventor 陈国雨石庆然吕志敏
Owner 南京望知星医药科技有限公司
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