Preparation method of quetiapine intermediate

A technology of equations and reactions, applied in the direction of organic chemistry, etc., to achieve the effects of low cost, mild reaction conditions, and easy availability of raw materials

Active Publication Date: 2015-05-20
太仓市茜泾化工有限公司
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  • Abstract
  • Description
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Problems solved by technology

[0004] So far, there is no relevant patent report about the synthesis method of this intermediate

Method used

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  • Preparation method of quetiapine intermediate
  • Preparation method of quetiapine intermediate
  • Preparation method of quetiapine intermediate

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Embodiment Construction

[0027] The present invention will be described in further detail below in conjunction with specific embodiments.

[0028] A kind of [2-(2-amino-phenylmercapto)-phenyl]-{4-[2-(2-hydroxy-ethoxy)-ethyl]-piperazin-1-yl}-methanone hydrochloride The preparation method of salt (hereinafter referred to as Queti-III), it comprises the steps:

[0029] (1), preparation of 2-iodobenzoyl chloride

[0030]

[0031] Add 600g of toluene, 390g of 2-iodobenzoic acid and 380g of thionyl chloride into a 2000ml four-neck flask, heat the mixture for about 1-2 hours to boiling (68-75°C) and stir rapidly, a large amount of HCl and SO2 will be produced during heating . Heat to 90°C over 2-3 hours, stirring rapidly. Stir rapidly at 90°C for at least 6 hours. After the heat preservation, the reaction solution was cooled to 35±10°C. Evaporate excess SOCl2 and toluene under reduced pressure, under rapid stirring, until the final temperature is 90°C, and the final vacuum degree is less than -0.09MP...

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Abstract

The invention relates to a preparation method of (2-(2-amino-phenyl-mercapto)-phenyl)-(4-(2-(2-hydroxy-ethoxy)-ethyl)-piperazine-1-yl)-ketone and a hydrochloride thereof. The preparation method comprises the following steps of (1) enabling 2-iodobenzoic acid and thionyl chloride to perform substitution reaction so as to generate 2-iodoebenzoyl chloride; (2) enabling the 2-iodoebenzoyl chloride and 1-(2-(2-hydroxyethoxy)-ethyl)-piperazine to perform the substitution reaction so as to generate a compound 1; and (3) enabling the compound 1 and 2-amino-thiophenol to perform the substitution reaction in the presence of an acid binding agent so as to generate the (2-(2-amino-phenyl-mercapto)-phenyl)-(4-(2-(2-hydroxy-ethoxy)-ethyl)-piperazine-1-yl)-ketone. By adopting the synthesis route disclosed by the invention, the total yield can be above 40%, the purity of the obtained product can achieve 99%, and the preparation method disclosed by the invention has the advantages of easiness in obtaining the used raw materials, simplicity in operation, mild reaction conditions and lower cost.

Description

technical field [0001] The present invention relates to a kind of [2-(2-amino-phenylmercapto)-phenyl]-{4-[2-(2-hydroxy-ethoxy)-ethyl]-piperazin-1-yl}-methyl Process for the preparation of ketones and their hydrochlorides. Background technique [0002] [2-(2-Amino-phenylmercapto)-phenyl]-{4-[2-(2-hydroxy-ethoxy)-ethyl]-piperazin-1-yl}-methanone and its salts ( Hydrochloride) is an important intermediate for the synthesis of psychotic quetiapine, and its structural formula is as follows: [0003] [0004] So far, there is no relevant patent report about the synthesis method of this intermediate. Contents of the invention [0005] The technical problem to be solved by this invention is to overcome and provide a kind of [2-(2-amino-phenylmercapto)-phenyl]-{4-[2-(2-hydroxyl-ethoxy)-ethyl]-piperene A method for preparing oxazin-1-yl}-methanone and its hydrochloride, which has low cost. [0006] In order to solve the above technical problems, the present invention takes th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D295/192
Inventor 吴健明
Owner 太仓市茜泾化工有限公司
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