A kind of compound for nano-pet imaging agent and preparation method and application thereof
A PET imaging agent and compound technology, applied in the field of nanomaterials, can solve the problems of unsatisfactory imaging effect of nano-PET imaging agent, difficult preparation of nano-PET imaging agent, low uptake rate, etc., and achieves objective guarantee and mild labeling conditions. , the effect of high uptake rate
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Embodiment 1
[0039] Example 1: Synthesis of FB-CBT-KCRRVR
[0040] In this embodiment, the preparation method of FB-CBT-KCRRVR is as follows:
[0041] Dissolve 0.018mmol of the precursor substance CBT-KCRRVR in 5mL of phosphate buffer, then add 0.11mmol of SFB in 5mL of acetone solution, adjust the pH to 7.2, and react at 50°C for 8 hours to obtain the product.
[0042] The solution obtained by the above reaction was separated by HPLC, and the mixed solvent of acetonitrile and water added with 0.1V% trifluoroacetic acid was used as mobile phase, and gradient elution was carried out by a C18 chromatographic column (5 μm, 10mm×250mm). Increase from 30% to 70% within 30 minutes, keep the flow rate of the eluent at 3mL / min, collect the product, freeze-dry to obtain 0.012mmol of the product, and the product yield is 67%.
[0043] The product obtained above is confirmed by nuclear magnetic resonance and mass spectrometry, and the result is: 1 HNMR(d 4 -CD 3 OD,300MHz):8.63(s,1H),8.10(d,J=9.0...
Embodiment 2
[0045] Example 2: Synthesis of FB-CBT-KCRRVR
[0046] In this embodiment, the preparation method of FB-CBT-KCRRVR is as follows:
[0047] Dissolve 0.005 mmol of the precursor substance CBT-KCRRVR in 5 mL of water, then add 0.08 mmol of SFB in 5 mL of dimethylformamide solution, and adjust the pH of the reaction solution to 8.0 using 0.01 M sodium carbonate buffer. React at 40°C for 5 hours to obtain.
[0048] The product was separated by HPLC using the same method as in Example 1 to obtain 0.0037 mmol of the product, and the product yield was 74%.
Embodiment 3
[0049] Example 3: Synthesis of FB-CBT-KCRRVR
[0050] In this embodiment, the preparation method of FB-CBT-KCRRVR is as follows:
[0051] Dissolve 0.0005 mmol of the precursor substance CBT-KCRRVR in 5 mL of water, then add 0.01 mmol of SFB in 5 mL of acetonitrile solution, and react at 10° C. for 24 hours to obtain the product.
[0052] Adopt the method HPLC separation product identical with embodiment 1, obtain product 0.00026mmol,
[0053] The product yield was 52%.
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