A receptor molecular targeting imaging agent and preparation method thereof
A molecular targeting and imaging agent technology, applied in the field of medical imaging, can solve the problems of inaccurate diagnosis results, insufficient spatial resolution, poor imaging effect, etc., achieve excellent biological properties, simple and easy preparation method, and reduce radioactivity damage effect
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Embodiment 1
[0042] (1) Synthesis of p-vinylbenzylamine
[0043] Potassium phthalimide and the equivalent amount of 4-chloromethylstyrene are dissolved in an appropriate amount of DMF, and the temperature is controlled to 40-60°C to react for 10-30 hours. After the reaction, the reaction solution was cooled to room temperature, and an appropriate amount of water was added to produce a large amount of white precipitate. Add dichloromethane to dissolve, transfer the liquid to a separatory funnel for separation, and collect the organic phase. The aqueous phase was washed with dichloromethane, and the organic phases were combined. The combined organic phase was washed with NaOH solution and then with water. The organic phase was collected. After drying, the solid was removed by suction filtration, and the solvent was removed by rotating the filtrate to obtain a white solid, namely N-(4-vinylbenzyl)-o-benzene. Diformimide (VBP).
[0044] In a three-necked flask, add VBP and an appropriate amount ...
Embodiment 2
[0071] Steps (1) to (4) are the same as in Example 1
[0072] (5) Preparation of P (VLA-co-VNI-co-VDT)
[0073] Mix 1,4,7,10-tetraazacyclododecyl-1,4,7,10-tetraacetic acid (DOTA) with a small amount of water, and gradually add NaOH solid until DOTA is completely dissolved and the solution is clear. Add 0.5-5mmol EDC and 0.5-5mmol NHS, adjust the pH to alkaline with NaOH solution, and react with magnetic stirring overnight at room temperature to obtain activated DOTA.
[0074] Mix 0.5-2 mL of P (VLA-co-VNI-co-VBA) solution with activated DOTA, control the temperature of the oil bath to 30-60°C, and react at constant temperature for 1-3 days under magnetic stirring. After the reaction is over, the reaction solution is transferred to a dialysis belt with a molecular weight cutoff of 5000-10000, and the pure water is dialyzed for 3-5 days. After the dialysis is over, centrifugal separation is performed, and the supernatant is freeze-dried to obtain a yellow solid product, namely P(VLA-...
Embodiment 3
[0090] Steps (1) to (4) are the same as in Example 1
[0091] (5) Preparation of activated DTPA
[0092] Diethylenetriaminepentaacetic acid (DTPA) is mixed with a small amount of water, and NaOH solid is gradually added until all DTPA is dissolved and the solution is clear. Add excess N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (EDC) and N-hydroxysuccinimide (NHS), adjust the pH to alkalinity with NaOH solution Activated DTPA is obtained by magnetic stirring at room temperature overnight.
[0093] (6) Preparation of activated DOTA
[0094] Mix 1,4,7,10-tetraazacyclododecyl-1,4,7,10-tetraacetic acid (DOTA) with a small amount of water, and gradually add NaOH solid until DOTA is completely dissolved and the solution is clear. Add 0.5-5mmol EDC and 0.5-5mmol NHS, adjust the pH to alkaline with NaOH solution, and react with magnetic stirring overnight at room temperature to obtain activated DOTA.
[0095] (7) Preparation of P (VLA-co-VNI-co-VDT-co-VDP)
[0096] Mix 0.5-2 ...
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