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Preparation method for triazole compound

A compound, triazole technology, applied in the field of new preparation of pharmaceutical intermediates, can solve problems such as synthesis difficulties

Inactive Publication Date: 2018-02-16
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 N-((5-(3-fluorophenyl)-2H-1,2,4-triazol-3-yl)methyl)-N-propylpropan-1-amine is difficult at present

Method used

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  • Preparation method for triazole compound
  • Preparation method for triazole compound
  • Preparation method for triazole compound

Examples

Experimental program
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Effect test

Embodiment 1

[0025] (1) Synthesis of ethyl 3-(3-fluorophenyl)propionate

[0026] Add 25g of 3-(3-fluorophenyl)ethyl acrylate to 260ml of methanol, add 19g of sodium borohydride, stir at room temperature for 3 hours, cool, concentrate, add water and ethyl acetate, extract and separate, collect the organic phase, Drying and concentration afforded 19 g of ethyl 3-(3-fluorophenyl)propionate.

[0027] (2) Synthesis of 3-(3-fluorophenyl)propionamide

[0028] Add 19g of ethyl 3-(3-fluorophenyl)propionate to 600ml of ammonia water, then add 200ml of water, heat to 80°C, stir for 10 hours, add ethyl acetate for extraction and separation, collect the organic phase, dry and concentrate 16 g of 3-(3-fluorophenyl)propanamide are obtained.

[0029] (3) Synthesis of 3-(3-fluorophenyl) propionimidate

[0030] Add 15g of 3-(3-fluorophenyl)propionamide to 180ml of tetrahydrofuran, slowly add 11g of triethyloxonium tetrafluoroboric acid, heat and reflux and stir for 6 hours, cool, filter, collect the filt...

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Abstract

The invention discloses a preparation method for a triazole compound namely N-((5-(3-fluorophenyl)-2H-1,2,4-triazole-3-yl)methyl)-N-propylprop-1-amine. The preparation method prepares a target product7 with 3-(3-fluorophenyl)ethyl acrylate as a starting material through reduction, acylation, imidization, cyclization, Boc removal and alkylation reactions. The product prepared by using the preparation method provided by the invention is used as a template micromolecule for synthesis of various compound libraries.

Description

technical field [0001] The present invention relates to a novel preparation method of a pharmaceutical intermediate, in particular to a triazole compound N-((5-(3-fluorophenyl)-2H-1,2,4-triazol-3-yl) The preparation method of methyl)-N-propyl propan-1-amine. technical background [0002] Compound N-((5-(3-fluorophenyl)-2H-1,2,4-triazol-3-yl)methyl)-N-propylpropan-1-amine, the structural formula is: [0003] [0004] The compound N-((5-(3-fluorophenyl)-2H-1,2,4-triazol-3-yl)methyl)-N-propylpropan-1-amine and related derivatives in It is widely used in medicinal chemistry and organic synthesis. Currently, the synthesis of N-((5-(3-fluorophenyl)-2H-1,2,4-triazol-3-yl)methyl)-N-propylpropan-1-amine is difficult. 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 triazole compound N-((5-(3-fluorop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D249/08
CPCC07D249/08
Inventor 不公告发明人
Owner 湖南华腾制药有限公司
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