Preparation method and application of ethyl 2-(4-hydroxyphenyl)thiazole-4-carboxylate derivatives

A technology of ethyl carboxylate and hydroxyphenyl, which is applied in the field of preparation of ethyl 2-thiazole-4-carboxylate derivatives, can solve problems such as toxic side effects and failure to prevent the degeneration and death of central cholinergic neurons, and achieve Convenient post-processing, simple and safe synthesis method, and high yield
CN106749090BActive Publication Date: 2019-05-14伊势久(江苏连云港)生物科技有限责任公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
伊势久(江苏连云港)生物科技有限责任公司
Publication Date
2019-05-14

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Abstract

The invention discloses a preparation method and an application of ethyl 2-(4-hydroxyphenyl)thiazole-4-carboxylate derivatives. The preparation method comprises the following steps: reacting p-hydroxythiobenzamide with ethyl 3-bromopyruvate to synthesize an intermediate ethyl 2-(4-hydroxyphenyl)thiazole-4-carboxylate, respectively reacting the intermediate with 1,3-dibromopropane, 1,4-dibromobutane or 1,5-dibromopentate to synthesize ethyl 2-(4-(3-bromopropoxy)phenyl)thiazole-4-carboxylate, ethyl 2-(4-(4-bromobutoxy)phenyl)thiazole-4-carboxylate or ethyl 2-(4-((5-bromopentyl)oxy)phenyl)thiazole-4-carboxylate, and respectively reacting the ethyl 2-(4-(3-bromopropoxy)phenyl)thiazole-4-carboxylate, ethyl 2-(4-(4-bromobutoxy)phenyl)thiazole-4-carboxylate or ethyl 2-(4-((5-bromopentyl)oxy)phenyl)thiazole-4-carboxylate with an amine to generate the target products. The synthesis method has the advantages of simplicity, safety and small pollution, and the products have a strong inhibition effect on butyrylcholine esterase and / or acetylcholinesterase, and can be used for preparing anti-Alzheimer disease medicines.
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Description

technical field

[0001] The invention relates to the field of medicine preparation, in particular to a preparation method of a 2-(4-hydroxyphenyl)thiazole-4-carboxylic acid ethyl ester derivative and its function as an inhibitor of acetylcholinesterase and / or butyrylcholinesterase Application of drugs in the treatment of Alzheimer's disease. Background technique

[0002] Alzheimer's disease is a common brain neurodegenerative disease in the elderly. It has the characteristics of high morbidity and high mortality. Its mortality rate is second only to cardiovascular disease, cancer and stroke. It has become a modern One of the most threatening diseases in society. According to literature reports, there were 36 million people in the world suffering from Alzheimer's disease in 2010, and the number is expected to rise to 42.3 million in 2020 and 81.1 million in 2040.

[0003] The pathogenesis of Alzheimer's disease is still unclear. In recent years, scientists have proposed a va...

Claims

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