Composition for diagnosing amyloid-related disease
A technology of amyloid and correlation, applied in preparations for in vivo experiments, in vivo radioactive preparations, organic chemistry, etc., can solve problems such as uninvolved diseases
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Embodiment 1
[0114] experimental method
[0115] Reagents and Instruments
[0116] Amyloid β protein (human, 1-42) [TFA type] was purchased from Peptide Institute, Inc., and special grade reagents were used as other reagents. Measured using Varian Gemini 300 and tetramethylsilane as internal standard 1 H-NMR.
[0117] (1) Synthesis of chalcone derivatives containing aromatic heterocycles
[0118] Synthesis of (E)-3-(4-(dimethylamino)phenyl)-1-(5-iodothiophen-2-yl)prop-2-en-1-one (1)
[0119] 256 mg (1 mmol) of 5-acetyl-2-iodothiophene and 149 mg (1 mmol) of 4-dimethylaminobenzaldehyde were dissolved in ethanol (20 mL), and 10% aqueous potassium hydroxide solution (30 mL) was added to the mixture under ice-cooling middle. React at room temperature for 6 h, then add 30 mL of purified water, and filter the precipitated crystals by suction. The crystals were washed with 50% aqueous ethanol and dried to obtain target compound 1. Yield 238mg (62.1% yield). 1 H NMR (300MHz, CDCl 3 )δ...
Embodiment 2
[0137] experimental method
[0138] Reagents and Instruments
[0139] As radioactive iodine-125 ( 125 I) Iodine-125 (3.7 GBq / mL) manufactured by MP Biomedicals, Inc. was used. At a flow rate of 1.0 mL / min, Cosmosil 5C manufactured by Nacalai Tesque Inc. was used 18 -AR-II column (4.6×150 mm) and ultrapure water: acetonitrile = 3:7 as eluent, reversed-phase HPLC. Using Varian Gemini 300 with tetramethylsilane as internal standard, measure 1 HNMR. Mass spectrometry was performed using a JEOL IMS-DX300. Using 12PLC plate 20 x 20cm manufactured by MERCK - Silica Gel 60F 254 , 2 mm for preparative TLC. Amyloid β protein (human, 1-42) was purchased from Peptide Institute, Inc., and special grade reagents were used as other reagents.
[0140] (1) Synthesis of chalcone derivatives
[0141] Synthesis of 4-bromo-4'-nitrochalcone (1)
[0142] 4-Nitroacetophenone (1.67g, 10.1mmol) and 4-bromobenzaldehyde (1.86g, 10.0mmol) were dissolved in ethanol (10mL), and 10% potassium h...
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