Tramadol, salts thereof and process for their preparation

A technology of tramadol and tramadol base, which is applied in the field of tramadol derivatives, can solve the problems of high content, low yield and the like, and achieves the effect of environmental friendliness

Inactive Publication Date: 2000-08-23
RUSSINSKY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, the yield of the cis(+ / -) isomer remains relatively low, and the content of the trans(+ / -) isomer remains relatively high in most cases

Method used

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  • Tramadol, salts thereof and process for their preparation
  • Tramadol, salts thereof and process for their preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0034] To prepare tramadol base hydrate, 69 kg of magnesium, 400 L of anhydrous tetrahydrofuran (THF) and 15 L of 3-bromoanisole were successively added to a reaction vessel.

[0035] Heat carefully to raise the reaction temperature to about 30°C. At this point the Grignard reagent was started and the temperature exothermed to about 50°C. Add another 5 L of bromoanisole and maintain reflux. Add 400 L of THF before the remaining bromoanisole. The remaining anisole was added slowly to maintain a gentle reflux. The reaction was refluxed after the addition of 3-bromoanisole was complete. The reaction vessel was cooled and Mannich base was added. When the addition was complete, the vessel was reheated to reflux for a total of 30 minutes to ensure completion of the reaction. After cooling to about 10°C, 2300 L of water was added to quench the reaction. When complete, part of the solvent was distilled under vacuum. Add approximately 260 L of concentrated hydrochloric acid at l...

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Abstract

Cis-Tramadol hydrochloride is prepared by forming a Mannich hydrochloride, liberating the Mannich base, reacting the Mannich base with a Grignard reagent to form a base hydrate of cis-Tramadol which is used to form pure cis-Tramadol hydrochloride. Also claimed is the base hydrate of cis-Tramadol per se and its use as a medicament.

Description

Background of the invention [0001] The present invention relates to novel, stable and pure derivatives of tramadol, specific processes for their preparation and their use. The present invention also relates to a method for preparing tramadol and its salts, especially tramadol hydrochloride, using the above-mentioned derivatives. [0002] Tramadol is the compound cis(+ / -)-2-[(dimethylamino)-methyl]-1-(3-methoxyphenyl)cyclohexanol, which has been It is widely used as an analgesic. [0003] Tramadol hydrochloride has a special place among centrally acting analgesics because the active substance is a very strong pain suppressant without the known side effects of morphine-like substances (T.Pharmacol.Exptl.Ther .267, 331 (1993)). [0004] The compound itself is described in US 3,652,589 and UK 997,399. Tramadol is obtained in the form of cis-racemate as the main synthesis product. In known processes, the trans-racemate is a minor constituent of the reaction mixture. US 3,652,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/135A61P25/04C07C213/00C07C213/10C07C217/74
CPCC07C217/74C07C2101/08C07C2601/08A61P25/04
Inventor 安杰洛·尼科洛普洛斯赫尔穆特·席卡内德
Owner RUSSINSKY
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