Alauddin M M, Conti P S, Mazza S M, Hamzeh F M, Lever J R
PET Imaging Science Center, Department of Radiology, University of Southern California, Los Angeles 90033, USA.
Nucl Med Biol. 1996 Aug;23(6):787-92. doi: 10.1016/0969-8051(96)00075-3.
A no-carrier-added synthesis of 9-[(3-[18F]-fluoro-1-hydroxy-2-propoxy)methyl]-guanine ([18F]-FHPG) is reported. The 9-[(1,3-dihydroxy-2-propoxy)methyl)guanine (DHPG) was converted to 9-[N2,O-bis(methoxytrityl)-3-(tosyl)-2-propoxy-methyl]guanine by treatment with methoxytrityl chloride followed by tosylation. The tosylate was reacted with [18F]-KF in the presence of kryptofix 2.2.2. to produce the 3-fluoro-N2-O-bis-(methoxytrityl) derivative. Removal of the methoxytrityl protecting groups by acid hydrolysis produced [18F]-FHPG. The labeled product was purified by HPLC on a reverse-phase C18 column, and eluted in 9 min with a mobile phase of 5% acetonitrile in water. The radiochemical yield was 7-17%, with an average of 10% in 10 runs (corrected for decay to EOB). The radiochemical purity was > 99%, and specific activities with an average of 526 mCi/mumol were obtained. The synthesis time was 70-80 min, including HPLC purification and determination of radiochemical purity and specific activity.
报道了一种无载体添加合成9-[(3-[¹⁸F]-氟-1-羟基-2-丙氧基)甲基]鸟嘌呤([¹⁸F]-FHPG)的方法。9-[(1,3-二羟基-2-丙氧基)甲基]鸟嘌呤(DHPG)先用甲氧基三苯甲基氯处理，然后进行甲苯磺酰化，转化为9-[N₂,O-双(甲氧基三苯甲基)-3-(甲苯磺酰基)-2-丙氧基甲基]鸟嘌呤。甲苯磺酸酯在穴醚2.2.2存在下与[¹⁸F]-KF反应，生成3-氟-N₂,O-双(甲氧基三苯甲基)衍生物。通过酸水解去除甲氧基三苯甲基保护基，得到[¹⁸F]-FHPG。标记产物在反相C18柱上通过高效液相色谱法纯化，用5%乙腈水溶液作为流动相，9分钟内洗脱。放射化学产率为7-17%，10次运行的平均产率为10%（校正至EOB时的衰变）。放射化学纯度>99%，平均比活度为526 mCi/μmol。合成时间为70-80分钟，包括高效液相色谱纯化以及放射化学纯度和比活度的测定。
