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A kind of preparation method of 1-substituted benzimidazole derivative

A technology of benzimidazole and derivatives, which is applied in the field of new preparation of pharmaceutical intermediates, and can solve problems such as synthesis difficulties

Active Publication Date: 2016-06-29
湖南华腾制药有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The synthesis of (4-(1H-benzo[d]imidazol-1-yl)phenylmethylamine is relatively difficult at present

Method used

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  • A kind of preparation method of 1-substituted benzimidazole derivative
  • A kind of preparation method of 1-substituted benzimidazole derivative
  • A kind of preparation method of 1-substituted benzimidazole derivative

Examples

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Effect test

Embodiment 1

[0022] (1) Synthesis of 4-fluoro-methyl benzoate

[0023] Add 26g of 4-fluorobenzoic acid to 200ml of methanol, add 50ml of thionyl chloride, stir overnight, and concentrate to obtain 29g of 4-fluoro-benzoic acid methyl ester.

[0024] (2) Synthesis of methyl 4-(1H-benzo[d]imidazol-1-yl)benzoate

[0025] Add 28g of 4-fluoro-methyl benzoate to 320ml of N,N-dimethylformamide, add 19g of potassium carbonate and 36g of benzimidazole, heat and reflux and stir for 5 hours, cool, concentrate, add water and ethyl acetate to extract liquid, the organic phase was collected, dried, and concentrated to obtain 36 g of methyl 4-(1H-benzo[d]imidazol-1-yl)benzoate.

[0026] (3) Synthesis of 4-(1H-benzo[d]imidazol-1-yl)phenylcarboxamide

[0027] Add 35g of methyl 4-(1H-benzo[d]imidazol-1-yl)phenylcarboxylate into 200ml of ammonia water, heat to reflux and stir for 3 hours, cool, add ethyl acetate, extract and separate, collect the organic phase, and dry , concentrated, and the residue was s...

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Abstract

The invention discloses a preparation method of a 1-site-sbsituted benzimidazole derivative (4-(1H-benzo[d] imidazole-1-yl) phenylmethylamine 1. By using 4-fluorobenzoic acid as an initial raw material, a target product is obtained by esterification, condensation, amidation and reduction reaction. The compound is an important medical intermediate.

Description

technical field [0001] The invention relates to a novel preparation method of a pharmaceutical intermediate, in particular to a preparation method of a 1-substituted benzimidazole derivative (4-(1H-benzo[d]imidazol-1-yl)phenylmethylamine. technical background [0002] Compound (4-(1H-benzo[d]imidazol-1-yl)phenylmethylamine, the structural formula is: [0003] [0004] This compound (4-(1H-benzo[d]imidazol-1-yl)phenylmethylamine and related derivatives are widely used in medicinal chemistry and organic synthesis. Currently (4-(1H-benzo[d] ] imidazol-1-yl) phenylmethylamine is relatively difficult to synthesize.Therefore, it is necessary to develop a synthetic method that is easy to get, easy to operate, easy to control, and overall yield suitable. Contents of the invention [0005] The invention discloses a preparation method of a 1-position substituted benzimidazole derivative 4-(1H-benzo[d]imidazol-1-yl)phenylmethanamine, which uses 4-fluorobenzoic acid as a starting ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D235/06
CPCC07D235/06
Inventor 陈芳军
Owner 湖南华腾制药有限公司
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