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Preparation method of 2-fluoro-5-(trifluoromethyl) pyridine

A technology of trifluoromethyl and pyridine, which is applied in the field of preparation of 2-fluoro-5-pyridine, can solve the problems of low product purity, inability to realize large-scale preparation process, cumbersome preparation process, etc.

Pending Publication Date: 2021-02-05
南京麦瑞米生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] 2-Fluoro-5-(trifluoromethyl)pyridine, molecular formula C6H3F4N, as an important chemical intermediate, is widely used in fields such as medicine and agriculture, conventional 2-fluoro-5-(trifluoromethyl)pyridine The preparation process cannot be scaled up, and the preparation process is cumbersome and the product purity is low

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] A preparation method of 2-fluoro-5-(trifluoromethyl)pyridine, comprising the following steps:

[0015] S1: take 5-(trifluoromethyl)pyridine and a brominating agent, and react to obtain 2-bromo-5-(trifluoromethyl)pyridine;

[0016] S2: Take the 2-bromo-5-(trifluoromethyl)pyridine prepared in step S1, add hydrogen fluoride, and react to obtain crude 2-fluoro-5-(trifluoromethyl)pyridine;

[0017] S3: Take the crude 2-fluoro-5-(trifluoromethyl)pyridine prepared in step S2, cool and stand still to obtain 2-fluoro-5-(trifluoromethyl)pyridine.

[0018] In step S1, the reaction temperature is 80°C.

[0019] In step S2, the reaction temperature is 30°C.

[0020] In step S3, the cooling temperature is 5°C.

Embodiment 2

[0022] A preparation method of 2-fluoro-5-(trifluoromethyl)pyridine, comprising the following steps:

[0023] S1: take 5-(trifluoromethyl)pyridine and a brominating agent, and react to obtain 2-bromo-5-(trifluoromethyl)pyridine;

[0024] S2: Take the 2-bromo-5-(trifluoromethyl)pyridine prepared in step S1, add hydrogen fluoride, and react to obtain crude 2-fluoro-5-(trifluoromethyl)pyridine;

[0025] S3: Take the crude 2-fluoro-5-(trifluoromethyl)pyridine prepared in step S2, cool and stand still to obtain 2-fluoro-5-(trifluoromethyl)pyridine.

[0026] In step S1, the reaction temperature is 160°C.

[0027] In step S2, the reaction temperature is 50°C.

[0028] In step S3, the cooling temperature is 20°C.

Embodiment 3

[0030] A preparation method of 2-fluoro-5-(trifluoromethyl)pyridine, comprising the following steps:

[0031] S1: take 5-(trifluoromethyl)pyridine and a brominating agent, and react to obtain 2-bromo-5-(trifluoromethyl)pyridine;

[0032] S2: Take the 2-bromo-5-(trifluoromethyl)pyridine prepared in step S1, add hydrogen fluoride, and react to obtain crude 2-fluoro-5-(trifluoromethyl)pyridine;

[0033] S3: Take the crude 2-fluoro-5-(trifluoromethyl)pyridine prepared in step S2, cool and stand still to obtain 2-fluoro-5-(trifluoromethyl)pyridine.

[0034] In step S1, the reaction temperature is 100°C.

[0035] In step S2, the reaction temperature is 40°C.

[0036] In step S3, the cooling temperature is 10°C.

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Abstract

The invention discloses a preparation method of 2-fluoro-5-(trifluoromethyl) pyridine. The method comprises the following steps: S1, taking 5-(trifluoromethyl) pyridine and a brominating agent, and reacting to obtain 2-bromine-5-(trifluoromethyl) pyridine; S2, adding hydrogen fluoride into the 2-bromo-5 (trifluoromethyl) pyridine prepared in the step S1, and reacting to obtain a 2-fluoro-5-(trifluoromethyl) pyridine crude product; and S3, taking the crude product of the 2-fluoro-5-(trifluoromethyl) pyridine prepared in the step S2, and carrying out cooling, and standing to obtain the 2-fluoro-5- (trifluoromethyl) pyridine. The 2-fluorine-5-(trifluoromethyl) pyridine prepared by the method is simple in process and high in purity.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a preparation method of 2-fluoro-5-(trifluoromethyl)pyridine. Background technique [0002] 2-Fluoro-5-(trifluoromethyl)pyridine, molecular formula C6H3F4N, as an important chemical intermediate, is widely used in fields such as medicine and agriculture, conventional 2-fluoro-5-(trifluoromethyl)pyridine The preparation process cannot be scaled up, and the preparation process is cumbersome and the product purity is low. Contents of the invention [0003] The object of the present invention is to provide a preparation method of 2-fluoro-5-(trifluoromethyl)pyridine, so as to realize the rapid preparation of 2-fluoro-5-(trifluoromethyl)pyridine with high purity and stable performance. [0004] Realize the technical scheme of the present invention through the following aspects: [0005] A preparation method of 2-fluoro-5-(trifluoromethyl)pyridine, comprising the foll...

Claims

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Application Information

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IPC IPC(8): C07D213/61
CPCC07D213/61
Inventor 廖明
Owner 南京麦瑞米生物技术有限公司
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