Process for producing intermediate of asenapine synthesis

A compound and reaction technology, applied in the preparation of organic compounds, carboxylate salts, carboxylic acid amides, etc., can solve the problems of complicated preparation and difficult use

Inactive Publication Date: 2009-10-21
SUMITOMO CHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] When adopting the above-mentioned approach to synthesize the final object asenapine (compound [IX]), there is the problem that it is necessary to use methyl 2-bromophenylacetate that is not easy to obtain and prepare complicated

Method used

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  • Process for producing intermediate of asenapine synthesis
  • Process for producing intermediate of asenapine synthesis
  • Process for producing intermediate of asenapine synthesis

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Embodiment

[0081] Hereinafter, although this invention is demonstrated concretely based on an Example, it cannot be overemphasized that this invention is not limited to these Examples.

[0082] [Example]

[0083] (1-a) Synthesis of 2-(2-(4-chlorophenoxy)phenyl)acetic acid [II]

[0084] 2-Chlorophenylacetic acid [I] (1.0g, 5.9mmol), 4-chlorophenol (0.78g, 6.5mmol), cesium carbonate (3.8g, 11.7mmol), copper bromide (I) (42mg, 0.29 mmol) and diethylene glycol dimethyl ether (5 ml) were mixed and heated at 145°C for 8 hours. After cooling, water (15ml) was poured into the reactant, then concentrated hydrochloric acid (about 2g) was added to make it acidic, and it was extracted with toluene (20ml×2). After the toluene layer is washed with water (20ml), saturated brine (20ml), dehydrate with anhydrous magnesium sulfate, remove magnesium sulfate by filtration then, obtain the toluene solution of [II] (the quantitative yield of using standard substance (standard product) is 59%). For use i...

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Abstract

A process for producing 2-(2-(4-chlorophenoxy)phenyl)acetic acid [II] through reaction of 2-chlorophenylacetic acid [I] with 4-chlorophenol.

Description

technical field [0001] The invention relates to a novel preparation method of a synthetic intermediate of Asenapine which can be used as a schizophrenic drug. Background technique [0002] Asenapine [Chemical name: trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino( oxepino) [4,5-c] pyrrole] is formula [IX] [0003] [0004] The compounds shown are compounds that can be used as schizophrenic drugs. [0005] Patent Document 1 describes a method for preparing asenapine [IX] through the following reaction route. [0006] [0007] When the final target product asenapine (compound [IX]) is synthesized by the above-mentioned route, there is a problem that it is necessary to use methyl 2-bromophenylacetate which is difficult to obtain and complicated to prepare. [0008] Patent Document 1: International Publication No. 2006 / 106136 Pamphlet Contents of the invention [0009] The object of the present invention is to provide a method for efficiently ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C51/367C07C231/02
CPCC07C51/367C07C231/02
Inventor 德田修王维奇池本哲哉
Owner SUMITOMO CHEM CO LTD
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