Moon Byung Seok, Park Jun Hyung, Lee Hong Jin, Kim Ji Sun, Kil Hee Sup, Lee Byoung Se, Chi Dae Yoon, Lee Byung Chul, Kim Yu Kyeong, Kim Sang Eun
Department of Nuclear Medicine, Seoul National University Bundang Hospital, Seoul National University College of Medicine, Seongnam 463-707, Republic of Korea.
Appl Radiat Isot. 2010 Dec;68(12):2279-84. doi: 10.1016/j.apradiso.2010.06.016. Epub 2010 Jun 22.
To minimize the base concentration of a phase-transfer catalyst, [(18)F]fluoride was extracted from (18)O-enriched water trapped on an activated ion exchange cartridge (Chromafix PS-HCO(3)) using different concentrations of tetrabutylammonium bicarbonate (TBAHCO(3)) or Kryptofix 2.2.2./K(2)CO(3) in organic solvents such as CH(3)CN/H(2)O or MeOH/H(2)O. The optimal labeling condition for [(18)F]fallypride with automated synthesis was that 2 mg of tosyl-fallypride in acetonitrile (1 mL) was heated at 100 degrees C for 10 min using 40% TBAHCO(3) (10 microL). [(18)F]Fallypride was obtained with a high radiochemical yield of approximately 68+/-1.6% (decay-corrected, n=42) with a total synthesis time of 51+/-1.2 min, including HPLC purification and solid-phase purification for the final formulation.
为了使相转移催化剂的碱浓度最小化，使用不同浓度的碳酸氢四丁铵（TBAHCO₃）或冠醚2.2.2./碳酸钾（K₂CO₃）在诸如乙腈/水（CH₃CN/H₂O）或甲醇/水（MeOH/H₂O）的有机溶剂中，从捕集在活化离子交换柱（Chromafix PS-HCO₃）上的富¹⁸O水中萃取[¹⁸F]氟化物。使用自动化合成制备[¹⁸F]法螺哌隆的最佳标记条件是，将2mg对甲苯磺酰法螺哌隆溶于乙腈（1mL）中，加入40% TBAHCO₃（10μL），在100℃加热10分钟。[¹⁸F]法螺哌隆的放射化学产率较高，约为68±1.6%（衰变校正，n = 42），总合成时间为51±1.2分钟，包括HPLC纯化和最终制剂的固相纯化。
