Preparation method of pyridine derivative

A technology of pyridine and hydroxypyridine, which is applied in the field of new preparation of pharmaceutical intermediates, and can solve problems such as multi-drug resistance, abuse, and irrational application

Inactive Publication Date: 2014-11-26
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

At present, there are many kinds of antimicrobial drugs in clinical use, but with the large number of antimicrobial drugs,

Method used

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  • Preparation method of pyridine derivative
  • Preparation method of pyridine derivative
  • Preparation method of pyridine derivative

Examples

Experimental program
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Effect test

Embodiment 1

[0024] (1) Synthesis of 1-(2-hydroxyethyl)pyridin-2(1H)-one

[0025] Add 20g of 2-hydroxypyridine to 500ml of N,N-dimethylformamide, add 9g of anhydrous potassium carbonate, then add 40g of 2-bromoethanol, heat and reflux and stir for 8 hours, cool to room temperature, add water for extraction, and separate the liquids , dried, concentrated, and the residue was subjected to column separation to obtain 23 g of 1-(2-hydroxyethyl)pyridin-2(1H)-one.

[0026] (2) Synthesis of 1-(2-chloroethyl)pyridin-2(1H)-one

[0027] Add 22g of 1-(2-hydroxyethyl)pyridin-2(1H)-one to 140ml of thionyl chloride, heat to reflux for 6 hours, cool to room temperature, remove excess thionyl chloride under reduced pressure, then add water and Ethyl acetate, extraction and separation, the organic phase was collected, liquid separation, drying, and concentration, and the residue was separated on a silica gel column to obtain 18 g of 1-(2-chloroethyl)pyridin-2(1H)-one.

[0028] (3) Synthesis of tert-butyl...

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Abstract

The invention discloses a preparation method of a pyridine derivative, and especially relates to a preparation method of 1-(2-(piperazine-1-group)ethyl)pyridine-2(1H)-ketone, the method takes 2-pyridone as an initial raw material, and 2-pyridone is subjected to nucleophilic substitution, chlorination, nucleophilic substitution and Boc removal to obtain the target product, and the compound is an important medicine intermediate.

Description

technical field [0001] The invention relates to a novel preparation method of a pharmaceutical intermediate, especially a preparation method of 1-(2-(piperazin-1-yl)ethyl)pyridin-2(1H)-one. technical background [0002] Compound 1-(2-(piperazin-1-yl)ethyl)pyridine-2(1H)-one, the English name is 1-(2-(piperazin-1-yl)ethyl)pyridine-2(1H)- one, the structural formula is: [0003] [0004] Antimicrobial drugs are a class of drugs that are widely used in clinical practice and used in large doses, and play an important role in the control and treatment of diseases. At present, there are many kinds of antimicrobial drugs in clinical use, but with the large number of antimicrobial drugs, they are widely used, especially in clinical irrational application, and even abuse, which eventually leads to multi-drug resistance. Therefore, how to overcome multi-drug resistance has become an important topic of antimicrobial drug research at home and abroad. There are many ways to solve d...

Claims

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Application Information

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IPC IPC(8): C07D213/64
CPCC07D213/64
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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