阅读说明：本技术 一种制备高纯度重酒石酸卡巴拉汀的方法 (Method for preparing high-purity rivastigmine bitartrate ) 是由 李恩民 赵国磊 于 2018-08-01 设计创作，主要内容包括：本发明涉及一种重酒石酸卡巴拉汀的精制方法,其特征是：将重酒石酸卡巴拉汀粗品用低级醇-水的混合溶剂搅拌均匀后,加热回流至全溶,降温搅拌析晶,控温25-30℃析晶,析晶完毕后抽滤烘干得到重酒石酸卡巴拉汀精制品。(The invention relates to a refining method of rivastigmine bitartrate, which is characterized by comprising the following steps: uniformly stirring the crude rivastigmine with a mixed solvent of lower alcohol and water, heating and refluxing to be completely dissolved, cooling, stirring, crystallizing, controlling the temperature to be 25-30 ℃ for crystallizing, and performing suction filtration and drying after crystallization to obtain a refined rivastigmine product.)

1. A refining method of rivastigmine bitartrate is characterized in that: uniformly stirring the crude rivastigmine with a mixed solvent of lower alcohol and water, heating and refluxing to be completely dissolved, cooling, stirring, crystallizing, controlling the temperature to be 25-30 ℃ for crystallizing, and performing suction filtration and drying after crystallization to obtain a refined rivastigmine product.

2. A method according to claim 1, characterized in that: the refining system is lower alcohol-water mixed system, and the lower alcohol is C1-4 side chain alcohol, preferably methanol-water system.

3. A method according to claim 2, characterized in that: the ratio of lower alcohol to water system is 95:5 to 80:20, most preferably the ratio is methanol: water =95: 5.

4. The method according to claim 1, wherein the mass ratio of the rivastigmine racemate to the mixed solvent is 1:3 to 1:7, preferably 1: 5.

Technical Field

The invention belongs to the field of pharmaceutical chemistry, and relates to refining of rivastigmine bitartrate.

Background

Rivastigmine (rivastigmine), also known as Rivastigmine, belongs to the second generation of central AChE inhibitor, has selective inhibition effect on AChE of cerebral cortex and hippocampus, has little influence on AChE of striatum and heart, and can slow down the formation of amyloid precursor (APP).

Because the preparation route of the rivastigmine is short, most of the adopted intermediates are crude chemicals, the impurity systems of the rivastigmine prepared by different processes are different, so that the search for a reaction condition for efficiently purifying the rivastigmine is crucial to the industrial production, and the quality of the product can be ensured to be free from great fluctuation caused by the change of materials to the maximum extent.

Aiming at the aspect, a great deal of experimental research is carried out by the company, and the impurities of the rivastigmine bitartrate can be better removed by using a lower alcohol-water mixed system, and meanwhile, the yield of the product is ensured.

Disclosure of Invention

The invention relates to a refining method of rivastigmine bitartrate, which is characterized by comprising the following steps: uniformly stirring the crude rivastigmine with a mixed solvent of lower alcohol and water, heating and refluxing to be completely dissolved, cooling, stirring, crystallizing, controlling the temperature to be 25-30 ℃ for crystallizing, and performing suction filtration and drying after crystallization to obtain a refined rivastigmine product.

Detailed Description

The invention is further illustrated by the following examples, which are not to be construed as limiting the invention thereto.