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Clean production method of antidepressant drug intermediate

An ammonium paratungstate, supported technology, used in the field of medicine, can solve the problems of large environmental pollution and easy deactivation of catalysts, and achieve the effects of overcoming poisoning and deactivation, improving the reaction rate and large specific surface area.

Active Publication Date: 2018-11-16
山东君瑞医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0017] The purpose of the present invention is to overcome problems such as large environmental pollution and easy deactivation of catalyst in the reduction process of 2-(2,4-dimethylphenylsulfanyl) nitrobenzene in the prior art, and provide a kind of 2-(2 , 4-dimethylphenylsulfanyl) nitrobenzene nitro reduction catalyst, the present invention has prepared a kind of ammonium paratungstate modified loaded Pd material as hydrogen transfer catalyst, used to catalyze 2-(2,4-dimethyl Preparation of antidepressant drug vortioxetine hydrobromide intermediate 2-((2,4-dimethylphenyl)thio)aniline by nitroreduction of phenylthio)nitrobenzene

Method used

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  • Clean production method of antidepressant drug intermediate

Examples

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Embodiment 1

[0045] Prepare the loaded Pd catalyst modified by ammonium paratungstate as follows:

[0046] 1) Add 0.3g of ammonium paratungstate to 100ml of purified water, raise the temperature to 60-80°C, then add 10.0g of alumina-doped silica and stir for 6-8h to obtain the first dispersion;

[0047] 2) Add 62ml of 0.1mol / L K dropwise to the first dispersion 2 PdCl 4 Aqueous solution (the loading capacity of Pd on alumina-doped silica is about 6.6%wt), after the dropwise addition, keep stirring at 60-80°C to obtain the second dispersion;

[0048] 3) Lower the temperature of the second dispersion to 10-20°C, and then dropwise add 260ml of 0.3mol / L sodium borohydride aqueous solution to carry out the reduction reaction. After the dropwise addition, the temperature is gradually raised to 50-60°C and kept for 2-3 hours to obtain the third Dispersions;

[0049] 4) Cool the third dispersion to room temperature, filter, wash with water, and collect the filter cake until there is no chloride...

Embodiment 1-A

[0051] Compared with Example 1, 0.3 g of ammonium paratungstate is not added in step 1), and the rest is completely consistent with Example 1, and the prepared catalyst is defined as Pd@Al-Si.

Embodiment 1-B

[0053] Compared with Example 1, 10.0 g of activated carbon was used instead of alumina-doped silica, and the rest were completely consistent with Example 1, and the prepared catalyst was defined as Pd@C.

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Abstract

The invention belongs to the technical field of medicines and particularly relates to a clean production method of an antidepressant drug intermediate. Aluminum oxide doped silicon dioxide is taken asa carrier, ammonium paratungstate is taken as a modifier, K2PdCl4 is taken as a Pd precursor, an ammonium paratungstate modified supported Pd catalyst is prepared through reduction with sodium borohydride and can catalyze 2-(2,4-dimethylphenyl)(2-nitrophenyl)sulfane to perform nitroreduction, and an antidepressant drug vortioxetine hydrobromide intermediate 2-[(2,4-dimethylphenyl)thio]benzenamineis prepared. The catalysis process is green and pollution-free, the catalyst does not easily cause poisoning, and the method is suitable for production amplification.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a clean production method of an antidepressant drug intermediate. Background technique [0002] Vortioxetine hydrobromide is an inhibitor of serotonin transporter and regulates the activity of its receptors, jointly developed by Lundbeck and Takeda; clinically used to treat severe depression and generalized anxiety disorder. On September 30, 2013, it was approved for marketing in the United States, with the product name Trintellix; on December 18, 2013, it was approved for listing in Europe, with the product name Trintellix; it is currently in the clinical development stage in China and has not been approved for marketing; 2014 The annual global sales reached 123 million US dollars, and the global sales in 2015 reached 281 million US dollars, which has become an increasing trend year by year. [0003] The chemical name of vortioxetine hydrobromide is 1-[2-[(2,4-dim...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C319/20C07C323/37B01J23/652B01J35/10
CPCC07C319/20B01J23/6527B01J35/61C07C323/37
Inventor 张浩亮谭月光王成光范建荣胡国民
Owner 山东君瑞医药科技有限公司
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