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Optics pure milnacipran and production method of its salt

一种米那普仑、光学的技术，应用在米那普仑及其盐的制备领域，能够解决成本高、操作复杂等问题，达到成本低、操作简单、适合大规模生产使用的效果

Inactive Publication Date: 2008-06-11
SICHUAN ANTIBIOTIC IND RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In summary, although asymmetric synthesis or chromatographic separation can obtain optically pure milnacipran with a high e.e. value (enantiomeric excess), the operation is complicated and the cost is high

Method used

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  • Optics pure milnacipran and production method of its salt
  • Optics pure milnacipran and production method of its salt
  • Optics pure milnacipran and production method of its salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Resolution of dextrose milnacipran with D-resolving agent family T1

[0032] Suspend 5.000 g (17.65 mmol) of milnacipran hydrochloride in a mixture of 50 ml of aqueous solution and 50 ml of dichloromethane, and add 10% aqueous sodium hydroxide solution with stirring until the aqueous phase is alkaline (pH=11). Separate the organic phase, extract the aqueous phase with dichloromethane (40ml each time) for 3 times, combine the organic phases, wash the organic phase twice with saturated brine, then dry with anhydrous sodium sulfate, filter, and distill off the dichloromethane to obtain Racemic Milnacipran. The resulting racemic milnacipran and 7.10g (17.65mmol) D-resolving agent family T1 were dissolved in 225ml 98% acetone-water respectively, mixed, crystallized, filtered to obtain (+)-milnacipran and D-Resolution product 5.59 g, yield: 85.0% by resolving agent family T1, the optical purity of (+)-milnacipran contained in it is 99.8% e.e.

Embodiment 2

[0033] Embodiment 2 uses D-di-p-methoxybenzoyl tartaric acid to resolve cyclized milnacipran

[0034] With 5.000g (17.65mmol) vortex milnacipran hydrochloride, according to the method of embodiment 1, obtain racemic milnacipran. The obtained racemic milnacipran and 8.865g (17.65mmol) D-di-p-methoxybenzoyl tartaric acid were dissolved in 500ml 98% isopropanol-water respectively, mixed, crystallized, and filtered to obtain (+) - Milnacipran and D-di-p-methoxybenzoyl tartaric acid 5.66g resolution product, yield: 86.0%, the optical purity of (+)-milnacipran contained in it is 99.9% e.e.

Embodiment 3

[0035] Embodiment 3 uses L-resolving agent family T to resolve the cyclized milnacipran

[0036] With 1.000g (3.53mmol) mixed milnacipran hydrochloride, according to the method of embodiment 1, obtain racemic milnacipran. The resulting racemic milnacipran and 1.420g (3.53mmol) L-resolving agent family T were dissolved in 45ml 98% acetone-water respectively, mixed, crystallized, filtered to obtain (-)-milnacipran and The resolution product of L-resolving agent family T1 was 1.094 g, yield: 83.1%, and the optical purity of (-)-milnacipran contained in it was 69.0% e.e.

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Abstract

The invention discloses a method for preparing optical pure milnacipran and medicinally acceptable salt, which adopts racemic milnacipran as raw material, tartaric acid derivative and composition as resolution agent to resolve.

Description

technical field [0001] The invention relates to a preparation method of optically pure milnacipran or milnacipran enriched in a specific configuration and a salt thereof. Background technique [0002] Milnacipran (milnacipran, trade name is Ixel, chemical name is 1-phenyl-2-aminomethylcyclopropane-N, N-diethylformamide,) is developed by French Pierre Fabre pharmaceutical company A drug for the treatment of depression developed and launched in 1997. It is reported that this product can also be used in the treatment of diseases such as fatigue, pain, fibromyalgia and irritable bowel syndrome. Currently commercially available mostly milnacipran hydrochloride. Milnacipran belongs to the serotonin and norepinephrine reuptake inhibitor (SNRI), which is a fourth-generation antidepressant that can simultaneously inhibit the reabsorption of serotonin and norepinephrine by neurons, and The strength of action is similar. It is mainly used for the treatment of depression, especially...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C237/24C07C231/20C07C231/24
CPCC07B2200/07C07C2101/02C07C231/20A61P25/24C07C2601/02C07C237/24
Inventor 艾林刘啸
Owner SICHUAN ANTIBIOTIC IND RES INST CO LTD
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