A monoamine oxidase inhibitor

A monoamine oxidase and inhibitor technology, applied in the field of monoamine oxidase A inhibitor and its synthesis, can solve the problems of high price, high toxicity, unstable properties of ruthenium tetroxide, etc., and achieve simple operation process, simple follow-up treatment, good monoamine oxidase A inhibition active effect
CN110642766BActive Publication Date: 2021-05-11ZHEJIANG UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG UNIV OF TECH
Publication Date
2021-05-11

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Abstract

The invention discloses a monoamine oxidase A inhibitor, which is obtained by using cheap ruthenium carbon as a catalyst to catalyze the synthesis of thioether at room temperature, specifically: using the compound represented by formula (III) as the reaction raw material, Ru / C as catalyst, NaIO 4 is an oxidant, water is a solvent, and the reaction is carried out at room temperature. After the reaction is completed, the reaction liquid is post-treated to obtain the sulfone compound shown in formula (IV). The method of the invention uses water as a solvent, oxidizes cheap ruthenium carbon with sodium periodate to generate ruthenium tetroxide, and further oxidizes the sulfide compound to synthesize the target product, and the preparation method is more efficient, quick, environmentally friendly and mild. The prepared monoamine oxidase A inhibitor has good monoamine oxidase A inhibitory activity, can be used to prepare a drug for inhibiting the activity of monoamine oxidase A, and has broad application prospects in drug development, in order to provide a more effective way for the treatment of related diseases.
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Description

[0001] (1) Technical field

[0002] The invention relates to a monoamine oxidase A inhibitor and its synthesis method and application.

[0003] (2) Background technology

[0004] Sulfone compounds are very important intermediates in organic synthesis, which are widely used in medicinal chemistry, materials science, and have a wide range of biological activities. For example, bicalutamide (structure a) is an antiandrogen drug, which is suitable for the treatment of advanced prostate cancer; raropiran (structure b) is a commonly used cardiovascular drug for the treatment of lipodystrophy; Cyclooxygenase (structure c) is a selective inhibitor of cyclooxygenase, which can be used to treat arthritis pain relief, has good patient tolerance, and also has the ability to prevent colorectal cancer, esophageal cancer, treat head and neck cancer, breast cancer, Potential clinical value and therapeutic effect of bladder cancer and cervical cancer; Dapsone (structure d) has a certain antiba...

Claims

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