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Method for preparing 2-chlorobenzo [d] oxazole-5-formic acid

A technology of oxazole and formic acid, which is applied in the field of new preparation of pharmaceutical intermediates, and can solve problems such as difficult synthesis

Inactive Publication Date: 2017-11-28
湖南华腾制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The synthesis of 2-chlorobenzo[d]oxazole-5-carboxylic acid is relatively difficult at present

Method used

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  • Method for preparing 2-chlorobenzo [d] oxazole-5-formic acid
  • Method for preparing 2-chlorobenzo [d] oxazole-5-formic acid
  • Method for preparing 2-chlorobenzo [d] oxazole-5-formic acid

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Embodiment 1

[0021] (1) Synthesis of 2-amino-4-methylphenol

[0022] Add 15g of 2-nitro-4-methylphenol and 1g of 10% palladium carbon to 120ml of methanol, feed hydrogen, stir at room temperature for 8 hours, filter, collect the filtrate, and concentrate to obtain 13g of 2-amino-4-methyl base phenol.

[0023] (2) Synthesis of 5-methylbenzo[d]oxazole-2-(3H)-thilone

[0024] Add 12g of 2-amino-4-methylphenol and 18g of potassium ethyl xanthate to 180ml of pyridine, heat to reflux and stir for 3 hours, cool to room temperature, add 10% hydrochloric acid, then add ethyl acetate, extract and separate , the organic phase was collected, dried, concentrated, and the residue was separated on a silica gel column to obtain 9 g of 5-methylbenzo[d]oxazole-2-(3H)-thianone.

[0025] (3) Synthesis of 2-chloro-5-methylbenzo[d]oxazole

[0026] Add 8g of 5-methylbenzo[d]oxazole-2-(3H)-thione to 70ml of thionyl chloride, heat and reflux and stir for 22 hours, cool and concentrate to obtain 7.2g of 2-chloro...

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Abstract

The invention discloses a method for preparing 2-chlorobenzo [d] oxazole-5-formic acid. The method comprises the following steps: by taking 2-nitro-4-methylphenol as an initial raw material, performing reduction, ring closure, chlorination and oxidation, thereby obtaining a target product. The compound is a significant medicinal intermediate.

Description

technical field [0001] The invention relates to a novel preparation method of a pharmaceutical intermediate, in particular to a preparation method of 2-chlorobenzo[d]oxazole-5-carboxylic acid. technical background [0002] The compound 2-chlorobenzo[d]oxazole-5-carboxylic acid has the structural formula: [0003] [0004] The compound 2-chlorobenzo[d]oxazole-5-carboxylic acid and related derivatives are widely used in medicinal chemistry and organic synthesis. The synthesis of 2-chlorobenzo[d]oxazole-5-carboxylic acid is difficult at present. Therefore, it is necessary to develop a synthetic method with easy-to-obtain raw materials, convenient operation, easy-to-control reaction and suitable overall yield. Contents of the invention [0005] The invention discloses a method for preparing 2-chlorobenzo[d]oxazole-5-carboxylic acid, which uses 2-nitro-4-methylphenol as a starting material and undergoes reduction, ring closure, chlorination and oxidation To obtain the tar...

Claims

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Application Information

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IPC IPC(8): C07D263/58
CPCC07D263/58
Inventor 不公告发明人
Owner 湖南华腾制药有限公司
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