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Synthesis method of image agent used for diagnosis of progeria dementia

A synthetic method, a technology for Alzheimer's disease, applied in chemical instruments and methods, drug combinations, preparation of organic compounds, etc., can solve problems such as limited effects and restrictions on the role of PET in Alzheimer's disease

Inactive Publication Date: 2008-02-27
北京天任瑞创科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] However, due to the influence of the structure and performance of the substance itself, the combination of the imaging agent and PET has limited effects in the diagnosis and treatment of Alzheimer's disease and other related fields, which restricts the role of PET in the diagnosis, pathogenic mechanism, and therapeutic drugs of Alzheimer's disease. , finding new and more sensitive probe molecules has been one of the focuses in this field

Method used

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  • Synthesis method of image agent used for diagnosis of progeria dementia
  • Synthesis method of image agent used for diagnosis of progeria dementia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: the synthesis of 6-hydroxyl-2-naphthylethanone (compound 2)

[0026] A solution dissolved in 80 mL of concentrated hydrochloric acid and 15 drops (about 0.75 mL) of triethylamine was heated to boiling. Add 1.00 g of 6-methoxy-2-naphthylethanone in CH 2 Cl 2 solution. After the reaction solution turned dark green, it was filtered through mineral wool to remove the black tar-like substance, washed with hot water, and solids precipitated after the solution cooled. The solid obtained by suction filtration was dissolved in 20 mL of ethyl acetate, washed with saturated sodium carbonate solution until neutral, and allowed to stand for liquid separation. The aqueous phase was extracted three times with 15 mL of ethyl acetate, the organic phases were combined, dried over anhydrous magnesium sulfate, and the solvent was evaporated to obtain 0.7311 g of a crude product with a yield of 78%.

Embodiment 2

[0027] Example 2: Synthesis of 2-acetyl-6-naphthyl-4'-methylbenzenesulfonate (compound 3a)

[0028]Will be dissolved with 35ml tetrahydrofuran, 0.35g (1.88mmol) 6-hydroxy-2-naphthyl ethyl ketone, 0.55g (2.88mmol) p-toluenesulfonyl chloride, 0.09g sodium hydroxide, 0.09g sodium bisulfite and 10 The three-necked flask dripped with triethylamine was heated to reflux, and the reaction was monitored by TLC (the developer was a mixture of acetone, dichloromethane and n-heptane, with a volume ratio of 3:6:3). After the reaction was completed, the resulting reaction mixture was dissolved in 30 ml of ethyl acetate, dried over anhydrous magnesium sulfate, filtered off insoluble matter, and the filtrate was volatilized and crystallized to obtain 0.45 g of crude product with a yield of 70.3%. The crude product was recrystallized from ethyl acetate, and the melting point of the pure product was 119-120°C.

Embodiment 3

[0029] Example 3: Synthesis of 2-acetyl-6-naphthyl acetate (compound 3b)

[0030] A solution containing 15ml of acetic anhydride, 0.60g (3.22mmol) of 6-hydroxy-2-naphthylethanone and 2 drops of triethylamine was heated to reflux for 2h. Filter out the insoluble matter, add 3 times of water to the filtrate, then add 2-3 drops of dilute HCl solution, stir, put in the refrigerator to freeze, and filter out the solid. The crude product was recrystallized from ethanol to obtain 0.60 g of needle crystals with a yield of 81.6%. The melting point is 85-86°C.

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Abstract

The invention discloses a synthesizing method of image agent to diagnoze early senile dementia, which is synthesized by right-row technical path.

Description

technical field [0001] The present invention relates to a method for synthesizing imaging reagents for diagnosing Alzheimer's disease. Background technique [0002] Alzheimer's disease (mainly manifested as Alzheimer's disease, referred to as AD) is a neurological disease with slow cognitive degeneration. The cerebral cortex of patients with this disease gradually shrinks, nerve cells continue to die, neurofibrillary tangles appear, and senile plaques are formed. The clinical onset of the patient is mostly hidden, and gradually develops memory loss, cognitive decline, emotional and behavioral abnormalities, aggressiveness, and gradually loses work and living abilities. [0003] Currently, the common diagnostic techniques for AD include various dementia detection scales and neuroimaging techniques. [0004] The dementia scale is a primary tool for checking dementia, but its ability to comprehensively assess the level of cognitive function is limited. So far, no dementia sca...

Claims

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Application Information

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IPC IPC(8): C07C255/30C07C253/00A61K51/04A61K101/02A61P25/28
Inventor 李加荣咸建良
Owner 北京天任瑞创科技发展有限公司
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