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A kind of preparation method of 1-substituted piperidine derivatives

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

Active Publication Date: 2016-09-21
湖南华腾制药有限公司
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  • Abstract
  • Description
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Problems solved by technology

The synthesis of 2-(4-((ethylamino)methyl)piperidin-1-yl)ethanol is difficult at present

Method used

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  • A kind of preparation method of 1-substituted piperidine derivatives
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  • A kind of preparation method of 1-substituted piperidine derivatives

Examples

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Embodiment 1

[0020] (1) Synthesis of 1-(2-hydroxyethyl)piperidine-4-carboxamide

[0021] Add 21g of piperidine-4-carboxamide to 260ml of toluene, add 23g of 2-bromoethanol and 13g of sodium hydroxide, heat to reflux and stir overnight, cool, add water and ethyl acetate, extract and separate, collect the organic phase, and dry , and concentrated to obtain 17 g of 1-(2-hydroxyethyl)piperidine-4-carboxamide.

[0022] (2) Synthesis of 2-(4-(aminomethyl)piperidin-1-yl)ethanol

[0023] Add 17g of 1-(2-hydroxyethyl)piperidine-4-carboxamide into 200ml of tetrahydrofuran, cool down to 0°C, slowly add 9g of lithium tetrahydrohydride, stir at room temperature for 2 hours, add dilute sodium hydroxide aqueous solution, After filtration, the mother liquor was collected, dried, concentrated, and the residue was separated by column to obtain 12 g of 2-(4-(aminomethyl)piperidin-1-yl)ethanol.

[0024] (3) Synthesis of 2-(4-((ethylamino)methyl)piperidin-1-yl)ethanol

[0025] Add 12g of 2-(4-(aminomethyl)p...

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Abstract

The invention discloses a preparation method of one-bit-substituted piperidine derivative, i.e., 2-(4-((ethyl-amino)methyl)piperidine-1-radical)alcohol. The preparation method adopts piperidine-4-formamide as a starting material, and obtains a target product by substitution reaction, reduction reaction and substitution reaction. The compound is an important medical intermediate.

Description

technical field [0001] The invention relates to a novel preparation method of a pharmaceutical intermediate, in particular to a preparation method of a 1-substituted piperidine derivative 2-(4-((ethylamino)methyl)piperidin-1-yl)ethanol. technical background [0002] Compound 2-(4-((ethylamino)methyl)piperidin-1-yl)ethanol, the structural formula is: [0003] [0004] The present compound 2-(4-((ethylamino)methyl)piperidin-1-yl)ethanol and related derivatives are widely used in medicinal chemistry and organic synthesis. Currently, the synthesis of 2-(4-((ethylamino)methyl)piperidin-1-yl)ethanol 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 2-(4-((ethylamino)methyl)piperidin-1-yl)ethanol, which uses piperidine-4-carboxamide as the starting material, and un...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/26
CPCC07D211/26
Inventor 不公告发明人
Owner 湖南华腾制药有限公司
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