Technique for producing rivastigmine hydrogen tartrate

A kind of rivastigmine bitartrate, the technology of production technology, is applied in the field of the production technique of rivastigmine bitartrate, can solve the problems of high market price, high production cost of rivastigmine bitartrate, etc., to achieve improved utilization rate, low cost, pollution small effect

Inactive Publication Date: 2008-08-13
苏州凯达生物医药技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the high production cost of rivastigmine bitartrate leads to high market price, so it is necessary to stu...

Method used

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  • Technique for producing rivastigmine hydrogen tartrate
  • Technique for producing rivastigmine hydrogen tartrate
  • Technique for producing rivastigmine hydrogen tartrate

Examples

Experimental program
Comparison scheme
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Embodiment

[0035] 1. Preparation of (S)-1-(3-methoxyphenyl)ethylamine (compound 1)

[0036] 15g (0.1mol, purity 98%) of m-methoxyacetophenone was dropped into the reactor, ethyl acetate 200mL and chiral auxiliary agent 0.12mol were heated to reflux, and HPLC monitoring m-methoxyacetophenone had reacted completely. The compound obtained by the reaction treatment is put into a reactor for catalytic hydrogenation. Put the hydrogenated product into the reactor, add 300mL of THF to dissolve it, and control the temperature at 0-10°C. 50.6 g (0.5 mol, reagent grade) of triethylamine was added, followed by dropwise addition of 61.3 g (0.4 mol, reagent grade) of phosphorus oxychloride, and then the temperature was raised to reflux for 5 h. Concentrate and recover THF, and extract with dichloromethane to obtain compound 1 with a yield of 80.6% and a purity of 98%.

[0037] 2. Preparation of (S)-1-(3-methoxyphenyl)-N,N-dimethylethylamine (compound 2)

[0038] In a 100mL three-necked flask, add c...

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Abstract

The invention discloses a production process of rivastigmine, comprising using m-methoxy hypnone as raw material, adding chiral auxiliary, reducing and aminating through an asymmetry synthesis method to obtain chiral amine, then demethylatig and acylating to prepare rivastigmine, and finally reacting rivastigmine with tartaric acid to obtain rivastigmine. The invention has advantages of simple operation, low cost, high yield, small pollution, and is suitable for industrialisation production.

Description

technical field [0001] The invention relates to a production process of rivastigmine bitartrate, in particular to a production process of anti-senile dementia drug rivastigmine bitartrate. Background technique [0002] Rivastigmine bitartrate is a second-generation selective central, reversible, long-acting non-competitive acetylcholinesterase (AchE) and butyrylcholinesterase (BchE) inhibitor developed by Novartis. It can not only be used to treat mild and moderate Alzheimer's dementia, but also has a more significant effect on patients with advanced severe AD. However, the high production cost of rivastigmine bitartrate leads to high market price, so it is necessary to study its synthetic route, find a better synthetic method, reduce the cost and make it more suitable for domestic production. Contents of the invention [0003] The purpose of the present invention is to provide a kind of production technology of rivastigmine hydrotartrate, and its operation is simple and ...

Claims

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Application Information

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IPC IPC(8): C07C271/44C07C269/00
Inventor 沈宗璇张燕飞陆霜肖本良
Owner 苏州凯达生物医药技术有限公司
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