SPECT imaging agent for FAP-alpha specific tumor diagnosis

[0055] The chemical synthesis of embodiment 1 HFAPi and HpFAPi

[0056] Method 1 for separation and purification of the target product by high performance liquid chromatography: Agilent 1260 HPLC system is equipped with YMC-Pack ODS-A C18 semi-preparative column (250×10mml.D.S-5μm, 12nm). Gradient elution for 25min with a flow rate of 3.2mL / min, wherein the mobile phase A is deionized water (containing 0.05% TFA), the mobile phase B is acetonitrile (containing 0.05% TFA), and the elution gradient is set to 85% A and 15% B, 85% A and 15% B at 5 min, 45% A and 55% B at 25 min.

[0057] Method 2 for separating and purifying the target product by high performance liquid chromatography: Agilent 1260 HPLC system is equipped with YMC-Pack ODS-A C18 semi-preparative column (250×10mml.D.S-5μm, 12nm). Gradient elution for 25min, flow rate 2.0mL / min, wherein the mobile phase A is deionized water (containing 0.05% TFA), the mobile phase B is acetonitrile (containing 0.05% TFA), and the e...

[0094] Example 2 Preparation of HFAPi and HpFAPi freeze-dried labeling kit

[0095] (1) Preparation of HFAPi kit

[0096] Weigh 1mg of HFAPi, dissolve it in 1mL of 75% ethanol aqueous solution, the concentration is 1μg / μL; then prepare a mixed solution containing 25μg (25μL) HFAPi, 2.0mg Tricine, 3.0mg TPPTS, 29.55mg succinic acid and 17.0mg sodium hydroxide 1mL, filtered through a 0.22μm filter membrane, added to a 10mL sterile vial, freeze-dried the mixture, sealed and capped to obtain 1 tube that can be used for 99m Tc-labeled lyophilized kit.

[0097] (2) Kit preparation of HpFAPi

[0098] Weigh 1 mg of HpFAPi, dissolve it in 1 mL of 75% ethanol aqueous solution, the concentration is 1 μg / μL; then prepare a mixed solution containing 25 μg (25 μL) HFAPi, 2.0 mg Tricine, 3.0 mg TPPTS, 29.55 mg succinic acid and 17.0 mg sodium hydroxide 1mL, filtered through a 0.22μm filter membrane, added to a 10mL sterile vial, freeze-dried the mixture, sealed and capped to obtain 1 tube...

[0099] Example 3 99m Tc-HFAPi and 99m Preparation and quality control of Tc-HpFAPi

[0100] The radiochemical purity (Radiochemical Purity, RCP) of the marker was determined using HPLC (equipped with Raytest Gabistar radioactive detector and Agilent-35900E digital-to-analog converter) and YMC-Pack ODS-A C18 analytical column (250×4.6mmml.D.S -5μm, 12nm), gradient elution for 20 minutes, flow rate 1mL / min, wherein the mobile phase A is deionized water (containing 0.05% TFA), and the mobile phase B is acetonitrile (containing 0.05% TFA). The elution gradient was set as 90% A and 10% B at the beginning, 60% A and 40% B at 17.5 min, and 90% A and 10% B at 20 min.

[0101] (1) 99m Preparation of Tc-HFAPi:

[0102] Add 1mL Na to the HFAPi freeze-dried kit (without opening the cap) 99m TCO 4 Solution (~740MBq), react in a water bath at 99°C for 15 minutes, take out the kit after the reaction and cool to room temperature to obtain the radiopharmaceutical 99m Tc-HFAPi, the struc...