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2-(4-bromine benzyl) pyrrolidine preparation method

A technology of pyrrolidine and bromobenzyl is applied in the field of novel preparation of pharmaceutical intermediates and can solve problems such as difficulty in synthesis

Inactive Publication Date: 2015-01-21
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 2-(4-bromobenzyl)pyrrolidine is difficult at present

Method used

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  • 2-(4-bromine benzyl) pyrrolidine preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0024] (1) Synthesis of 2-(4-bromophenyl)methyl acetate

[0025] Add 20g of p-bromophenylacetic acid to 400ml of methanol, add 2g of toluenesulfonic acid, stir at room temperature for 24 hours, concentrate, add water and ethyl acetate to extract, separate, dry, concentrate, and separate the residue on a column to obtain 22g of 2 -methyl (4-bromophenyl)acetate.

[0026] (2) Synthesis of 3-(2-(4-bromophenyl)acetyl)pyrrolidin-2-one

[0027] Add 20g of methyl 2-(4-bromophenyl)acetate to 320ml of o-xylene, then add 14g of 2-ethylbutamidine, add 9g of potassium carbonate, heat to reflux overnight, cool to room temperature, concentrate, then add water and dichloromethane, extracted and separated, collected the organic phase, separated, dried and concentrated, and the residue was separated on a silica gel column to obtain 15 g of 3-(2-(4-bromophenyl)acetyl)pyrrolidin-2-one.

[0028] (3) Synthesis of 5-amino-1-(4-bromophenyl)pentan-2-one

[0029] Put 14g of 3-(2-(4-bromophenyl)acety...

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Abstract

The present invention discloses a 2-(4-bromine benzyl) pyrrolidine preparation method, a target product is prepared from by bromophenyl acetic acid as a starting material by esterification, coupling, ring opening, ring closing and reduction, and the compound is an important pharmaceutical 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-(4-bromobenzyl)pyrrolidine. technical background [0002] Compound 2-(4-bromobenzyl)pyrrolidine, the English name is 2-(4-bromobenzyl)pyrrolidine, and its structural formula is: [0003] [0004] The compound 2-(4-bromobenzyl)pyrrolidine and related derivatives are widely used in medicinal chemistry and organic synthesis. The synthesis of 2-(4-bromobenzyl)pyrrolidine is relatively 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-(4-bromobenzyl)pyrrolidine, which uses p-bromophenylacetic acid as a starting material, and undergoes esterification, coupling, ring opening, ring closing and reduction to o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/08
CPCC07D207/08
Inventor 陈芳军李书耘邓泽平
Owner 湖南华腾制药有限公司
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