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Benzothiazolo [3, 2,-a]-miazine derivant and uses thereof

A technology of thiazolo and its derivatives, which is applied in the field of medicine, can solve problems such as drug resistance or pharmacokinetic defects, and achieve the effect of improving memory

Inactive Publication Date: 2008-07-16
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004]Existing acetylcholinesterase inhibitors such as tacrine, stigmine, galantamine, etc., still have drug resistance or pharmacokinetic defects

Method used

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  • Benzothiazolo [3, 2,-a]-miazine derivant and uses thereof
  • Benzothiazolo [3, 2,-a]-miazine derivant and uses thereof
  • Benzothiazolo [3, 2,-a]-miazine derivant and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] General method for the preparation of 5-acetyl-6-methyl-2-thio-1,2,3,4-pyrimidines At 0°C, add 1 mmol of acetylacetone dropwise to 10 ml of 1 mmol of any aldehyde In the solution or suspension of saturated hydrochloric acid ethanol, stir while adding dropwise, the mixture is naturally warmed to room temperature, and after stirring at room temperature for 30 minutes, add 10 ml of saturated hydrochloric acid ethanol solution of 1 mmol thiourea. After stirring for 30 minutes, the mixture was refluxed for 30 minutes under nitrogen protection. After cooling to room temperature, the reaction solution was concentrated to dryness and recrystallized from ethanol to obtain the desired product.

Embodiment 2

[0057] Preparation of 5-acetyl-4-(4-hydroxyphenyl)-6-methyl-2-thio-1,2,3,4-pyrimidine

[0058] At 0°C, add 1 mmol of acetylacetone dropwise to a solution or suspension of 1 mmol of p-hydroxybenzaldehyde in 10 ml of saturated hydrochloric acid ethanol, and stir while adding dropwise. After the drop is complete, the mixture is naturally warmed to room temperature. After stirring for 30 minutes, a solution of 1 mmol of thiourea in 10 ml of saturated ethanol hydrochloric acid was added. After stirring for 30 minutes, the mixture was refluxed for 30 minutes under nitrogen protection. After cooling to room temperature, the reaction solution was concentrated to dryness and recrystallized from ethanol to obtain the desired product.

Embodiment 3

[0060] Preparation of 5-acetyl-4-(4-methoxyphenyl)-6-methyl-2-thio-1,2,3,4-pyrimidine

[0061] At 0°C, add 1 mmol of acetylacetone dropwise to a solution or suspension of 1 mmol of p-methoxybenzaldehyde in 10 ml of saturated ethanol hydrochloride, stir while adding dropwise, after the drop is complete, the mixture is naturally warmed to room temperature, and After stirring at room temperature for 30 minutes, a solution of 1 mmol of thiourea in 10 ml of saturated ethanol hydrochloric acid was added. After stirring for 30 minutes, the mixture was refluxed for 30 minutes under nitrogen protection. After cooling to room temperature, the reaction solution was concentrated to dryness and recrystallized from ethanol to obtain the desired product.

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Abstract

The invention belongs to the technical field of medicine and relates to thiazole [3, 2-a] pyrimidine derivatives and the application thereof. The general structure formula is shown on the right: Thiazole [3, 2-a] pyrimidine derivatives and additive salts of pharmaceutically applicable acids of the compounds are used as acetylcholine esterase inhibitors. R1 can be substituted arbitrarily and selectively by one or two substituent groups independently selected from C1-C6 alkyls, C1-C6 alkoxyls, amino alkoxyls arbitrarily and selectively substituted from C1-C10, substituted or unsubstituted amidine formyl alkoxyls, hydroxyl and halogens; R2 is independently selected from hydrogen, C1-C6 alkyls, phenyl substituted by arbitrarily and selectively substituted amino alkoxyls from C1-C10, phenyl substituted by substituted or unsubstituted amidine formyl alkoxyls, and phenyl substituted by hydroxyl; R3 is independently selected from methyl and ethoxyl. The derivatives are used for enhancing the memory of patients with aphrenia or Alzheimer.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to thiazolo[3,2-a]pyrimidine derivatives and applications thereof, in particular to thiazolo[3,2-a]]pyrimidine derivatives (I) and the three-dimensional Isomers and pharmaceutically acceptable salts and their use. Compounds of formula (I) are acetylcholinesterase inhibitors useful for improving memory in patients with dementia and Alzheimer's disease. Background technique: [0002] Alzheimer's disease is associated with the degeneration of cholinergic neurons in the basal forebrain, which play an important role in recognition functions, including memory. As a result of said degeneration, patients suffering from this disease exhibit marked attenuations in acetylcholine synthesis, choline acetyltransferase activity, acetylcholinesterase activity, and choline absorption. [0003] Acetylcholinesterase inhibitors are known to be effective in increasing cholinergic activity and thus may...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D513/04A61K31/519A61P25/28
Inventor 胡春郅慧刘斯婕陈兰妹张琳琳黄二芳刘晓平
Owner SHENYANG PHARMA UNIVERSITY
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