2-aminothiophene compound preparation method

A technology of aminothiophenes and compounds, which is applied in the field of preparation of chemical drug intermediates, can solve the problems of few preparation methods of 2-aminothiophenes, and achieve the effects of strong market competitiveness, simple reaction operation, and safe process

Inactive Publication Date: 2018-12-25
浙江工业大学上虞研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] There are few preparation methods about 2-am

Method used

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  • 2-aminothiophene compound preparation method
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  • 2-aminothiophene compound preparation method

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0019] Example 1 Preparation:

[0020] In a 200 mL airtight four-necked reaction flask, add 9.8 g of cyclohexanone, 11.3 g of ethyl cyanoacetate and 3.2 g of sulfur, add 50 mL of solvent toluene and 0.5 mL of catalyst piperidine, stir and control the temperature at 30°C, react for 60 minutes, and complete the reaction , Filtered and recrystallized to obtain 17.5 g of the target product, with a molar yield of 77.8%.

Example Embodiment

[0021] Example 2: Preparation:

[0022] In a 200 mL airtight four-necked reaction flask, add 9.8 g of cyclohexanone, 11.3 g of ethyl cyanoacetate and 3.2 g of sulfur, add 50 mL of solvent methanol and 0.5 mL of catalyst piperidine, stir and control the temperature at 30°C, react for 60 minutes, and complete the reaction , Filtered and recrystallized to obtain 21.7 g of the target product, with a molar yield of 96.4%.

Example Embodiment

[0023] Example 3: Preparation:

[0024] In a 200 mL airtight four-necked reaction flask, add 9.8 g of cyclohexanone, 11.3 g of ethyl cyanoacetate and 3.2 g of sulfur, add 50 mL of solvent methanol and 0.5 mL of catalyst morpholine, stir and control the temperature at 30°C, react for 60 minutes, and complete the reaction , Filtered and recrystallized to obtain 18.6 g of the target product with a molar yield of 93.9%.

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Abstract

The invention discloses a 2-aminothiophene compound preparation method. The method includes the step that ketone, nitrile and sulfur in a mole ratio of 1:1:1 are used as raw materials for preparing 2-aminothiophene compounds through catalytic cyclization. By adoption of ketone, nitrile and sulfur as the raw materials, the method has advantages of simple operating steps, high product yield, low cost and the like, and a high industrial value is achieved.

Description

technical field [0001] The invention belongs to the technical field of preparation methods of chemical drug intermediates, and in particular relates to a preparation method of 2-aminothiophene compounds. Background technique [0002] 2-aminothiophene compound, the structure is as shown in formula (I), is a kind of important chemical drug intermediate, is used for synthesizing tacrine analogue, and tacrine is the medicine for treating Alzheimer's dementia, tacrine Lin can inhibit AChE in the brain, increase ACh content in the brain; promote the release of AChE in the brain; increase the N-R density of the cerebral cortex and hippocampus; promote the utilization of glucose in the brain tissue, and improve the learning and memory. [0003] [0004] There are few preparation methods about 2-aminothiophene compounds disclosed at home and abroad. Contents of the invention [0005] The invention provides a preparation method of 2-aminothiophene compounds, which uses o-aminoth...

Claims

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Application Information

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IPC IPC(8): C07D333/68C07D333/66C07D333/38
CPCC07D333/38C07D333/66C07D333/68
Inventor 方标许萌柯军梁王哲
Owner 浙江工业大学上虞研究院有限公司
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