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Method for preparing 2- substituted pyrimidine derivative

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

Inactive Publication Date: 2015-07-22
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-(piperazin-1-ylmethyl)pyrimidine is difficult at present

Method used

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  • Method for preparing 2- substituted pyrimidine derivative
  • Method for preparing 2- substituted pyrimidine derivative
  • Method for preparing 2- substituted pyrimidine derivative

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0020] (1) Synthesis of 2-bromoacetamidine

[0021] Add 10g of bromoacetonitrile to 200ml of ethanol, cool to 0°C, add 14g of ammonium chloride and 5g of sodium methoxide, stir for 1 hour, then rise to room temperature and continue stirring for 4 hours, filter, concentrate the filtrate, and add Sodium bicarbonate aqueous solution and ethyl acetate, extraction and separation, the organic phase was collected, dried and concentrated to obtain 8 g of 2-bromoacetamidine.

[0022] (2) Synthesis of 2-(bromomethyl)pyrimidine

[0023] Add 8g of 2-bromoacetamidine to 120ml of toluene, add 14g of 1,1,3,3-tetramethoxypropane, heat to reflux for 3 hours, concentrate, add water to extract and separate the liquid, collect the organic phase, dry, concentrate, The residue was separated on a silica gel column to obtain 5 g of 2-(bromomethyl)pyrimidine.

[0024] (3) Synthesis of 2-(piperazin-1-ylmethyl)pyrimidine

[0025] Add 5g of 2-(bromomethyl)pyrimidine to 40ml of N,N-dimethylformamide, a...

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Abstract

The invention discloses a method for preparing a 2-substituted pyrimidine derivative 2-(piperazine-1-ylmethyl) pryimidine. The method comprises the following steps: by taking bromoacetonitrile as an initial raw material, performing addition, ring closing and substitution reactions, thereby obtaining a target product 4. The product prepared by using the method can be used as a template micromolecule for synthesizing various compound libraries.

Description

technical field [0001] The invention relates to a novel preparation method of a pharmaceutical intermediate, in particular to a preparation method of a 2-substituted pyrimidine derivative 2-(piperazin-1-ylmethyl)pyrimidine. technical background [0002] Compound 2-(piperazin-1-ylmethyl)pyrimidine, the structural formula is: [0003] [0004] The compound 2-(piperazin-1-ylmethyl)pyrimidine and related derivatives are widely used in medicinal chemistry and organic synthesis. Currently, the synthesis of 2-(piperazin-1-ylmethyl)pyrimidine 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 preparation method of a 2-position substituted pyrimidine derivative 2-(piperazin-1-ylmethyl)pyrimidine. The target product 4 is obtained through addition, ring closure and substitution reactions usi...

Claims

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Application Information

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IPC IPC(8): C07D239/26
CPCC07D239/26
Inventor 不公告发明人
Owner 湖南华腾制药有限公司
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