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Novel amination process

A technology of compounds and catalysts, applied in organic chemistry and other fields, can solve problems such as doubts about the feasibility of commercial production

Inactive Publication Date: 2007-05-02
ASTRAZENECA AB
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  • Abstract
  • Description
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Problems solved by technology

[0005] When this preparation involves amination of bromoesters, there are several drawbacks that make its commercial viability questionable

Method used

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Examples

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Embodiment Construction

[0124] Preparation of 1-(3-bromo-5-fluoro-2-hydroxyphenyl)ethanone

[0125] A mixture of 2-bromo-4-fluorophenol (64.0 kg, 1.00 mol equivalent) and acetyl chloride (62.5 kg, 2.39 mol equivalent) was stirred and heated at 50-55° C. for 1 hour. Excess acetyl chloride (10.8 kg) was removed by distillation, and the residue was cooled to 25-30°C and diluted with dichloromethane (120 L). The mixture was further cooled to 10-15° C., and aluminum chloride (51.0 kg, 1.15 mol equivalent) was added in two portions. Dichloromethane (80 L) was removed by distillation, during which time the mixture was heated to 130-135°C for 1 hour. The mixture was kept at 130-135°C for 1 hour, diluted with xylene (250 L) and cooled to 10-15°C. The reaction mixture was added to 30% w / w hydrochloric acid (25 L) / water (500 L). The layers were separated and the organic phase was extracted with 10% w / w sodium hydroxide solution (300 L). Cool the aqueous extract to 10-15° C., and adjust the pH value to 6.8-7...

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Abstract

Provided herein are novel processes for the preparation of intermediates that may be useful in the preparation of 5-Ht1b receptor antagonist useful in the treatment of depression, anxiety and other related diseases. The present processes may offer improved yields, purity, ease of preparation and isolation of intermediates and final product and more industrially useful reaction conditions and workability.

Description

technical field [0001] The present invention provides novel processes for the preparation of compounds of general formula I as defined below. [0002] Background technique [0003] The present invention relates to processes for the preparation of compounds useful in the manufacture of potentially effective orally active 5-Ht for the treatment of depression, anxiety and other related disorders 1b receptor antagonists. An example of this preparation method is shown below: [0004] [0005] When this preparation proceeds with the amination of bromoesters, there are several drawbacks which make its commercial viability doubtful. [0006] Applicants provide processes for the preparation of compounds of formula I which unexpectedly and surprisingly improve product yields and reaction times. Applicants also provide a process that is substantially free of by-products and impurities. For example, Applicant's process for the preparation of compounds of formula I does not exh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/02C07D405/04C07DC07D295/096
CPCC07D295/096C07D405/04C07D241/02C07D295/073
Inventor 莫劳德·德凯恩阿利森·诺顿安妮·奥基尔尼-麦克马伦格雷厄姆·鲁滨逊
Owner ASTRAZENECA AB
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