Compound for nanometer PET developer and its preparation method and use
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 targeting ability, etc., and achieve objective and labeling conditions. Mild, high uptake effect
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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 0.005mmol of the precursor substance CBT-KCRRVR in 5mL of water, then add 0.08mmol of SFB in 5mL of dimethylformamide solution, and adjust the pH of the reaction solution to 8.0 with 0.01M 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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