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在柱水解法自动化合成2-^(18)F-2-脱氧-D-葡萄糖 被引量:1

Automated synthesis of 2-[^(18)F]-fluoro-2-deoxy-D-glucose by on-column hydrolysis
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摘要 目的:研究在柱水解法自动化合成2-18F-2-脱氧-D-葡萄糖(2-[18F]-fluoro-2-deoxy-D-glu-cose,18F-FDG)。方法:采用在柱水解法和TRACERlabFXF-N自动化合成仪,以三氟甘露糖为前体,经亲核氟化、氢氧化钠在柱水解两步反应及SEP-PAK小柱分离纯化制备18F-FDG注射液。结果:18F-FDG总合成时间小于20min,未校正放化产率大于60%,放化纯度大于99%。结论:在柱水解法合成18F-FDG注射液,操作简便,是很实用的18F-FDG生产方法。合成的18F-FDG注射液可用于临床PET显像研究。 Objective To study automated synthesis of 2- [^18 F ] -fluoro-2 -deoxy-D-glucose (^18 F-FDG) via on-column hydrolysis. Methods Automated synthesis of ^18 F-FDG was performed by the on-column hydrolysis procedure in TRACERIab FXF-N synthesizer, ^18F-FDG injection was obtained via nucleophilic fluorination of 1, 3, 4, 6-tetra-O-acetyl-2-O-trifluoromethanesulfony-β-D-mannopyranose as the precursor molecule with ^18F-fluoride, hydrolysis of the ^18F-labeled intermediate on SEP-PAK C18 cartridges with 2 mol/L NaOH solution, and purification and neutralization with SEP-PAK cartridges. Results The uncorrected radiochemical yield of ^18F-FDG was more than 60% within the total synthesis time shorter than 20 min. The radiochemical purity of ^18F-FDG was above 99%. Conclusion On-column hydrolysis is simple and practical for the automated synthesis of ^18F-FDG. ^18F-FDG injection produced by this procedure can be used in clinical PET imaging.
出处 《中南大学学报(医学版)》 CAS CSCD 北大核心 2009年第11期1151-1156,共6页 Journal of Central South University :Medical Science
关键词 2-18F-2-脱氧-D-葡萄糖 在柱水解法 自动化合成 2-[^18F]-fluoro-2-deoxy-D-glucose on-column hydrolysis fully automated synthesis
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参考文献10

  • 1李军,李广义,高铎.新型^(18)F-脱氧葡萄糖注射液的制备与质量控制[J].华西药学杂志,2004,19(1):8-10. 被引量:9
  • 2Lemaire C, Damhaut P H, Lauricella B, et al. Fast [^18F ] FDG synthesis by alkaline hydrolysis on a low polarity solid phase support [ J ]. J Label Compd Radiopharm, 2002, 45(4) : 435-447.
  • 3张锦明,田嘉禾,周丹,陈英茂.快速自动化合成2-^(18)F-β-D-脱氧葡萄糖[J].中华核医学杂志,2003,23(1):52-54. 被引量:18
  • 4唐刚华,唐小兰,王明芳,郭晓君.高产率自动化合成2-^(18)F-2-脱氧-D-葡萄糖[J].核技术,2006,29(7):531-536. 被引量:11
  • 5Fuchtner F, Steinbach J, Mading P, et al. Basic hydrolysis of 2 - [ ^18 F ] fluoro-1, 3 , 4,6-tetra-O-acetyl-D-glueose in the preparation of 2- [ ^18 F ] -fluoro-2 - deoxy-D-glucose [ J ] . Appl Radiat Isot, 1996, 47(1) : 61-66.
  • 6Hamacher K, Coenen H H, Stocklin G. Efficient stereospecific synthesis of no-carrier-added 2- [^18F ] -fluoro-2-deoxy-D-glucose using aminopolyether supported nucleophilic substitution[ J]. J Nucl Med, 1986, 27 ( 1 ) : 235- 238.
  • 7Chaly T, Dahl J R. Thin layer chromatographic detection of kryptofix 2.2.2 in the routine synthesis of [ ^18F ] 2-fluoro- 2-deoxy-D-glucose[J]. Nucl Med Biol, 1989, 16(4): 385-387.
  • 8Fowler J S, ldo T. Initial and subsequent approach for the synthesis of ^18FDG[J]. Sere Nucl Med, 2002, 32(1) : 6-12.
  • 9Kim H W, Jeong J M, Lee Y S, et al. Rapid synthesis of [^18F ] FDG without an evaporation step using an ionic liquid [J]. Appl Radiat Isot, 2004, 61 (3) :1241-1246.
  • 10Kim D W, Ahn D S, Oh Y H, et al. A new class of SN2 reactions catalyzed by protic solvents: facile fluorination for isotopic labeling of diagnostic molecules [ J ]. J Am Chem Soc, 2006, 128(4) :16394-16397.

二级参考文献18

  • 1中华人民共和国国家药典委员会.中国药典[S]二部[M].北京:化学工业出版社,2000.附录XC75.
  • 2United Stated Pharmacopoeial Convention,Inc.USP 24[S].2000.733
  • 3Lemaire C,Damhaut P H,Lauricella B,et al.J Label Compd Radiopharm,2002,45(4):435-447
  • 4Fuchtner F,Steinbach J,Mading P,et al.Appl Radiat Isot,1996,47(1):61-66
  • 5Hamacher K,Coenen H H,Stocklin G.J Nucl Med,1986,27(1):235-238
  • 6Chaly T,Dahl J R.Nucl Med Biol,1989,16(4):385-387
  • 7Fowler J S,Ido T.Sem Nucl Med,2002,32(1):6-12
  • 8Hamacher K;Coenen HH;Stocklin G.Efficient stereospecific synthesis of no-carrier-added 2-18F-fluoro-2-deoxy-D-glucose using aminopolyether supported nucleophilic substitution,1986.
  • 9Padgett HC;Schmidt DG;Luxen A.Computer-controlled radiochemical synthesis:a chemistry process control unit for automated production of radiochemicals[J],1989.
  • 10USP ⅩⅩⅡ.

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