Receptor-like molecular targeted developing agent and preparation method therefor
A molecular targeting and imaging agent technology, applied in the field of medical imaging, can solve problems such as insufficient spatial resolution, inaccurate diagnosis results, and poor imaging effects, and achieve excellent biological properties, good chemical stability, and biodistribution properties , The effect of the simple and easy preparation method
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Embodiment 1
[0042] (1) Synthesis of p-vinylbenzylamine
[0043] Potassium phthalimide and equivalent 4-chloromethyl styrene are dissolved in an appropriate amount of DMF, and the temperature is controlled to 40-60°C for 10-30h. 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 liquid separation, and collect the organic phase. The aqueous phase was washed with dichloromethane, and the organic phases were combined. The combined organic phases were first washed with NaOH solution, and then washed with water, and the organic phases were collected. After drying, the solids were removed by suction filtration. Diformimide (VBP).
[0044] In the three-neck flask, add VBP and an appropriate amount of ethanol, and reflux under stirring until all of them are dissolved. Add hydrazine hydrate to dissolve...
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, gradually add solid NaOH until DOTA is completely dissolved, and the solution is clear. Add 0.5-5mmol EDC and 0.5-5mmol NHS, adjust the pH value with NaOH solution to reach alkalinity, and react overnight with magnetic stirring at room temperature to obtain activated DOTA.
[0074] Mix 0.5-2mL 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 finished, the reaction liquid is transferred to a dialysis belt with a molecular weight cut-off of 5000-10000, and is dialyzed with pure water for 3-5 days. After the dialysis, centrifugation was performed, and the supernatant was freeze-dried to obtain a yellow solid product, namely P(VL...
Embodiment 3
[0090] Steps (1) to (4) are the same as in Example 1
[0091] (5) Preparation of activated DTPA
[0092] Mix diethylenetriaminepentaacetic acid (DTPA) with a small amount of water, and gradually add solid NaOH 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 value with NaOH solution to reach alkali At room temperature, the reaction was carried out overnight with magnetic stirring to obtain activated DTPA.
[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, gradually add solid NaOH until DOTA is completely dissolved, and the solution is clear. Add 0.5-5mmol EDC and 0.5-5mmol NHS, adjust the pH value with NaOH solution to reach alkalinity, and react overnight with magnetic stirring at room temperature to obtain activated DOTA.
[0095] (7) Preparation ...
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