Amino sugar thiazole derivative as well as synthetic method and application thereof

A synthesis method and sugar thiazole technology, applied in the field of drug preparation, can solve the problems such as the inability to prevent the degeneration and death of central cholinergic neurons, the decrease in the efficacy of acetylcholinesterase inhibitors, the large side effects of gastrointestinal irritation, and the like. Scope of application, strong inhibitory activity, effect of reducing production cost
CN104292280AActive Publication Date: 2015-01-21HUAIHAI INST OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HUAIHAI INST OF TECH
Publication Date
2015-01-21

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Abstract

The invention discloses an amino sugar thiazole derivative as well as a synthetic method thereof. When synthesis is carried out, glucosamine hydrochloride is taken as a raw material, and benzyl ether protection is carried out on hydroxy, so that the selective reaction of amino is realized, a novel intermediate glycosyl thiourea-N-(1,3,4,6-tetra-0-benzyl-2-deoxygenation- beta-D-glucopyranose-2-group) thiocarbamide is synthesized, and glycosyl thiazole-N-(1,3,4,6-tetra-0-benzyl-beta-D-glucopyranose-2-group)-2-amido-4-substituted thiazole is synthesized by cyclizing the novel intermediate glycosyl thiourea-N-(1,3,4,6-tetra-0-benzyl-2-deoxygenation beta-D-glucopyranose-2-group) thiocarbamide with 1-bromine-2-substituted ethyl ketone. The synthetic method disclosed by the invention has the advantages of easiness and safety for operation, wide application scope, low cost of the raw material, easiness for raw material obtaining, easiness and convenience for post-processing and high yield, is a fast high-efficiency synthetic method and has a wide application prospect on the aspect of preparing an acetylcholinesterase resistant drug because the synthesized compound has high inhibiting effect on acetylcholinesterase.
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Description

technical field

[0001] The invention relates to the field of medicine preparation, in particular to an aminoglucothiazole derivative, and also relates to a preparation method and application of the aminoglucothiazole derivative. Background technique

[0002] Alzheimer's disease (AD) is a common brain neurodegenerative disease with a relatively high incidence rate, and has become one of the diseases that seriously threaten human life in modern society. Its clinical manifestations are deteriorating cognition and memory function, progressive decline in the ability of daily life, and various neuropsychiatric symptoms and behavioral disturbances. In developed countries, AD has become the fourth leading cause of death among the elderly after heart disease, cancer, and stroke. In China, the prevalence rate of the elderly over 65 years old is as high as 6.6%. For every 5 years of age increase, the prevalence rate doubles. One in three elderly people over the age of 85 has Alzheimer...

Claims

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