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Preparation method of piperazine derivative

A kind of derivative, piperazine technology, applied in the field of novel preparation of pharmaceutical intermediates, can solve problems such as difficult synthesis

Inactive Publication Date: 2015-03-04
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 (4-(4-methylbenzoyl)piperazin-1-yl)piperidine-1-carboxylic acid tert-butyl ester is relatively difficult at present

Method used

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  • Preparation method of piperazine derivative
  • Preparation method of piperazine derivative
  • Preparation method of piperazine derivative

Examples

Experimental program
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Effect test

Embodiment 1

[0022] (1) Synthesis of tert-butyl 4-hydroxypiperidine-1-carboxylate

[0023] Add 19g of 4-hydroxypiperazine to 250ml of dichloromethane, then add 12g of triethylamine, then slowly add 42g of di-tert-butyl dicarbonate, stir at room temperature for 5 hours, add water for extraction and liquid separation, collect the organic phase, and dry , Concentrated, and the residue was applied to a silica gel column to obtain 34 g of tert-butyl 4-hydroxypiperidine-1-carboxylate.

[0024] (2) Synthesis of tert-butyl 4-hydroxypiperidine-1-carboxylate

[0025] Add 30g tert-butyl 4-hydroxypiperidine-1-carboxylate to 400ml tetrahydrofuran, add 18g anhydrous potassium carbonate, add 20ml methanesulfonyl chloride dropwise, stir at room temperature for 12 hours, slowly add the reaction solution to saturated sodium bicarbonate Add ethyl acetate to extract the liquids, collect the organic phase, dry and concentrate to obtain 37 g of tert-butyl 4-hydroxypiperidine-1-carboxylate.

[0026] (3) Synthesis of te...

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Abstract

The invention discloses a preparation method of a piperazine (4-(4-methylbenzoyl)piperazine-1-yl)piperidine-1-tert-butoxycarbonyl. The preparation method comprises the steps of, with 4-hydroxypiperazine as a starting material, feeding Boc and performing condensation, nucleophilic substitution and amidation to obtain a target product. The compound is an important medical intermediate.

Description

Technical field [0001] The invention relates to a novel preparation method of pharmaceutical intermediates, in particular to a piperazine derivative (4-(4-methylbenzoyl)piperazin-1-yl)piperidine-1-carboxylic acid tert-butyl ester Preparation. technical background [0002] The compound (4-(4-methylbenzoyl)piperazin-1-yl)piperidine-1-carboxylic acid tert-butyl ester, the structural formula is: [0003] [0004] The compound (4-(4-methylbenzoyl) piperazin-1-yl) piperidine-1-carboxylic acid tert-butyl ester and related derivatives have a wide range of applications in medicinal chemistry and organic synthesis. At present, the synthesis of tert-butyl (4-(4-methylbenzoyl)piperazin-1-yl)piperidine-1-carboxylate is difficult. Therefore, it is necessary to develop a synthetic method that is easy to obtain, easy to operate, easy to control the reaction, and suitable for the overall yield. Summary of the invention [0005] The invention discloses a preparation method for preparing piperazine...

Claims

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Application Information

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IPC IPC(8): C07D211/58
CPCY02P20/55C07D211/58
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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