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Solifenacin succinate new preparation method

A technology of solifenacin succinate and succinic acid, which is applied in the field of preparation of raw materials, can solve the problems of instability of raw material formula X compound and unsuitability for industrial production, etc., and achieves the advantages of easy operation, simple preparation process and high yield Effect

Pending Publication Date: 2018-07-24
BEIJING LABWORLD BIO MEDICINE TECH
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Problems solved by technology

The shortcoming is that the compound of the raw material formula X is unstable, and the next step is carried out without treatment in each step, so it is not suitable for industrial production

Method used

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  • Solifenacin succinate new preparation method
  • Solifenacin succinate new preparation method
  • Solifenacin succinate new preparation method

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Embodiment 1

[0030] 1) At 0°C, suspend 127.2g of formula III compound R)-(-)-quinuclidin-3-ol in 2L of dichloromethane, and add 194.6g of formula IV compound DCI; then, under inert gas Stir the reaction for 3 hours; after the reaction, add water and extract, the organic layer is dried with anhydrous sodium sulfate, and finally dichloromethane is distilled off under reduced pressure, and crystallized with isopropyl acetate (IPAC)-heptane to obtain 164.8 g of the compound of formula V , as a white solid with a yield of 85.4%.

[0031] 2) Under inert gas, cool the tetrahydrofuran solution to -10°C, add 148.9g of formula VI compound (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline, and then slowly add 164.8g of the compound of formula V was stirred and reacted for 2h; the temperature was raised to room temperature, water was added and extracted with tert-butyl methyl ether, the organic phase was dried over anhydrous sodium sulfate, and tetrahydrofuran was distilled off under reduced pressure to obt...

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PUM

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Abstract

The present invention relates to a solifenacin succinate new preparation method which mainly comprises the following steps: 1) formula III compound (R)-(-)-quinuclidin-3-ol and formula IV compound N,N,-N,N-carbonyldiimidazole are reacted to obtain formula V compound (R)-imidazole-1-carboxylic acid-1-azabicyclo[2,2,2] octyl ester; 2) the formula V compound (R)-imidazole-1-carboxylic acid-1-azabicyclo[2,2,2] octyl ester is reacted with formula VI compound (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline to obtain a formula II solifenacin alkaline body; 3) the formula II solifenacin alkaline body isreacted with succinic acid, refined and purified to obtain formula I solifenacin succinate. The preparation method has the advantages that the yield of the solifenacin succinate is high and the purityis high, and the process is simple and suitable for industrial production.

Description

technical field [0001] The invention relates to a new preparation method of solifenacin succinate, which belongs to the technical field of raw material medicine preparation. Background technique [0002] The chemical name of solifenacin succinate is (3R)-1-azabicyclo[2.2.2]octan-3-yl(1S)-1-phenyl-3,4-dihydroisoquinoline-2 -(1H)-Carboxylate succinate, the English name is Solifenacin Sccinate, and the trade name is VESIcare. It is a selective muscarinic M3 receptor antagonist developed by Japan Astellas Company. It is clinically used for the treatment of overactive bladder. Symptoms such as frequent urination, urgency and urinary incontinence. [0003] For the preparation method of solifenacin succinate: [0004] 1) GN Trinadhachari, AG Kamat, BV Balaji et al published in "Organic Process Research & Development" in 2014 entitled "An Improved Process for the Preparation of Highly Pure Solifenacin Succinate via Resolution through Diastereomeric Crystallisation", which prepared...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D453/02
CPCC07D453/02C07B2200/07
Inventor 温光辉宛六一付冀峰刘金玉
Owner BEIJING LABWORLD BIO MEDICINE TECH
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