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Preparation method of new crystal form tapentadol hydrochloride

A technology of tapentadol hydrochloride and crystal form, applied in the field of chemical drug synthesis

Inactive Publication Date: 2014-02-05
NANJING CORE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0013] In the prior art, there are few literatures on the research on the polymorphic form of tapentadol hydrochloride, and there are fewer literatures on the preparation process of the new crystal form of tapentadol hydrochloride. Therefore, a safe and easy-to-control new crystal form of hydrochloric acid should be developed through research The preparation method of tapentadol is very necessary

Method used

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  • Preparation method of new crystal form tapentadol hydrochloride
  • Preparation method of new crystal form tapentadol hydrochloride
  • Preparation method of new crystal form tapentadol hydrochloride

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Embodiment Construction

[0030] The above-mentioned content of the present invention will be described in further detail below through the embodiment form, but this should not be interpreted as the scope of the above-mentioned theme of the present invention is limited to the following embodiments, all technologies realized based on the above-mentioned content of the present invention belong to this invention the scope of the invention.

[0031] Embodiment Preparation of new crystal form of tapentadol hydrochloride

[0032] (1) Synthesis of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol (formula (Ⅲ))

[0033] Weigh 100g of (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethyl-pentylamine hydrochloride into a 1L three-neck flask, measure 200ml of HBr (48%) Add it into the reaction bottle, install a thermometer, reflux the condenser, turn on the mechanical stirring, heat to 90-95°C, stir for 6 hours, lower the temperature to room temperature, add 300ml of ethyl acetate, slowly add 400ml of saturated...

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Abstract

The invention discloses a preparation method of new crystal form tapentadol hydrochloride, which comprises the following steps of (1) converting (2R, 3R)-3-(3-methoxyphenyl)-N,N,2-trimethyl-amylamine hydrochloride by use of a demethylation reagent into the formula (III): (-)-(1R, 2R)-3-(3-dimethylamino-1-ethyl-2-methylphenyl)phenol; (2) salifying the compound of formula (III) with hydrochloric acid in a mixed solvent of acetonitrile and isopropyl alcohol to obtain a compound of formula (I): (-)-(1R, 2R)-3-(3-dimethylamino-1-ethyl-2-methylphenyl)phenol hydrochloride. By adopting the method disclosed by the invention, stable new crystal form tapentadol hydrochloride can be obtained; moreover, the process conditions are mild, the after-treatment is simple, the purity is high, the reaction cost is low, and industrial production is easy to realize.

Description

technical field [0001] The invention belongs to the technical field of chemical drug synthesis and relates to (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol hydrochloride (tapenta hydrochloride A preparation method of a new crystal form. Background technique [0002] Tapentadol hydrochloride (Imatinib Mesylate), chemical name (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol hydrochloride, structural formula As follows: [0003] [0004] Tapentadol hydrochloride was developed by Johnson & Johnson Company of the United States. It is a new type of central analgesic with dual effects. It is both a mu opioid receptor agonist and a norepinephrine reabsorption inhibitor. It has analgesic effect on various animal models of chronic neuropathic pain, its potency is between that of morphine and tramadol, and it can reach satisfactory blood concentration through intravenous injection or oral administration, and it is well tolerated. [0005] There are man...

Claims

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Application Information

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IPC IPC(8): C07C215/54C07C213/06
Inventor 王雪根何凌云郭莉芹周磊纪慧敏何凤琴吴邵嘉卢向阳
Owner NANJING CORE TECH CO LTD
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