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Preparation method of morpholine compound

A compound, the technology of morpholine ethylamine, which is applied in the field of preparation of morpholine compounds, that is, N--2-morpholine ethylamine, can solve problems such as synthesis difficulties 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-iodobenzyl)-2-morpholine ethylamine is relatively difficult at present

Method used

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  • Preparation method of morpholine compound
  • Preparation method of morpholine compound
  • Preparation method of morpholine compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0014] 12g of 4-iodobenzylamine was added to 120ml of dichloromethane, cooled to 0°C, chloroacetyl chloride was added dropwise, stirred for 3 hours, water was added for extraction, liquid separation, drying, concentration, and the residue was separated on a column to obtain 14g ( 2-Chloro-N-acetamido)-4-iodobenzylamine.

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

[0016] 14g (2-chloro-N-acetamido)-4-iodobenzylamine 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- Iodobenzylamine.

[0017] (3) Synthesis of N-(4-iodobenzyl)-2-morpholine...

Embodiment 2

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

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

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

[0023] Add 11g (2-chloro-N-acetamido)-4-iodobenzylamine into 100ml toluene, add 5.7g triethylamine and 6.3g morpholine, heat and reflux overnight, cool to room temperature, concentrate, and 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-iodobenzylamine .

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

[0025] Add 12.9g of (2-...

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Abstract

The invention belongs to the field of organic synthesis, and in particular relates to a preparation method of a morpholine compound, i.e., N-(4-iodobenzyl)-2-morpholino ethylamine. According to the preparation method, 4-iodobenzylamine is used as a raw material, and the target product is obtained by carrying out acylation, nucleophilic substitution and reduction on the raw material. The compound can enrich organic synthesis molecular blocks.

Description

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

Claims

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Application Information

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Patent Type & Authority Applications(China)
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
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