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Synthesis method for morpholine derivative

A technology of morpholine ethylamine and compounds, which is applied in the field of synthesis of morpholine derivatives, i.e. N--2-morpholine ethylamine, can solve problems such as difficult synthesis and achieve the effect of an efficient synthesis method

Inactive Publication Date: 2018-03-09
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 N-(4-fluorobenzyl)-2-morpholine ethylamine is relatively difficult at present

Method used

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  • Synthesis method for morpholine derivative
  • Synthesis method for morpholine derivative
  • Synthesis method for morpholine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] (1) Synthesis of (2-chloro-N-acetamido)-4-fluorobenzylamine

[0014] Add 12g of 4-fluorobenzylamine into 120ml of dichloromethane, cool down to 0°C, add chloroacetyl chloride dropwise, stir for 3 hours, add water for extraction, separate, dry, concentrate, and the residue is separated on a column to obtain 14g ( 2-Chloro-N-acetamido)-4-fluorobenzylamine.

[0015] (2) Synthesis of (2-morpholine-N-acetamido)-4-fluorobenzylamine

[0016] 14g (2-chloro-N-acetamido)-4-fluorobenzylamine was added to 110ml of N,N-dimethylformamide, 6g of potassium carbonate and 8g of morpholine were added, heated to reflux overnight, and cooled to Room temperature, concentrated, then added 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 17g (2-morpholine-N-acetamido)-4- Fluoridine.

[0017] (3) Synthesis of N-(4-fluorobenzyl)-2-morpholine ethylamine

[0018] Ad...

Embodiment 2

[0020] (1) Synthesis of (2-chloro-N-acetamido)-4-fluorobenzylamine

[0021] 10g of 4-fluorobenzylamine was added to 120ml of tetrahydrofuran, cooled to 5°C, chloroacetyl chloride was added dropwise, stirred for 4 hours, water was added for extraction, separated, dried and concentrated, and the residue was separated on a column to obtain 11g (2- Chloro-N-acetamido)-4-fluorobenzylamine.

[0022] (2) Synthesis of (2-morpholine-N-acetamido)-4-fluorobenzylamine

[0023] Add 11g (2-chloro-N-acetamido)-4-fluorobenzylamine to 100ml toluene, add 5.7g triethylamine and 6.3g morpholine, heat to reflux overnight, cool to room temperature, concentrate, and then Add water and ethyl acetate, extract and separate the liquid, collect the organic phase, separate the liquid, dry, concentrate, and separate the residue on a silica gel column to obtain 12.9 g of (2-morpholine-N-acetamido)-4-fluorobenzylamine .

[0024] (3) Synthesis of N-(4-fluorobenzyl)-2-morpholine ethylamine

[0025] Add 12....

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Abstract

The invention belongs to the field of organic synthesis, and particularly relates to a synthesis method for a morpholine derivative, namely, N-(4-fluorobenzyl)-2-morpholineethanamine. A target productis obtained through acylating, performing nucleophilic substitution and reducing by taking 4-fluorobenzylamine as a starting raw material; the compound can enrich organic synthetic molecular blocks.

Description

technical field [0001] The invention belongs to the field of organic synthesis, and particularly relates to a synthesis method of a morpholine derivative, namely N-(4-fluorobenzyl)-2-morpholine ethylamine. technical background [0002] Compound N-(4-fluorobenzyl)-2-morpholine ethylamine, the structural formula is: [0003] [0004] The present compound N-(4-fluorobenzyl)-2-morpholine ethylamine and related derivatives are widely used in medicinal chemistry and organic synthesis. Currently, the synthesis of N-(4-fluorobenzyl)-2-morpholine ethylamine is relatively 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 method for synthesizing N-(4-fluorobenzyl)-2-morpholine ethylamine, which uses 4-fluorobenzylamine as a starting material, undergoes acylation, nucleophilicity, reduction, an...

Claims

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Application Information

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IPC IPC(8): C07D295/13
CPCC07D295/13
Inventor 不公告发明人
Owner 湖南华腾制药有限公司