摘要
报道了一种无酸条件下合成二芳基碘鎓盐的方法。以4-碘-L-苯丙氨酸为原料,经酯化、氨基保护、无酸组合试剂氮-氟试剂/乙酰基三甲基硅烷反应、苯基三氟硼酸钾/三甲基硅三氟乙酸发生金属转移反应和在离子交换反应成功制得了目标产物4-(氮,氮-二叔丁氧羰基苯丙氨酸甲酯)苯基碘鎓六氟磷酸盐。该碘鎓盐与氟-18标记的氟离子反应可制备氟18-氟代苯丙氨酸,是一种潜在的正电子发射断层显像显像剂。
A metal- free synthesis of [2- [（ di- tert- butoxycarbonyl）- amino]- 3- methoxy- 3- o- xopropyl- phenyl]-（ phenyl） iodonium hexafluorophosphate from the corresponding iodoarene was reported. Trimethylsilyl acetate（ TMSOAc） was used to tame the reactive I（ III） intermediate formed from oxidation of 2- amino- 3-（ 4- iodophenyl）propanoic acid by N- F reagents. The corresponding diacetoxyiodoarene could be obtained without damaging the acid-sensitive Boc protecting groups. The I（ III） intermediate could be converted to the corresponding diaryliodonium salts by reacting with benzenetrifluoroboric acid potassium salt and potassium hexaflourophosphate in excellent isolated yield. The iodonium salt was a useful precursor for synthesis of18F- fluorophenalanine,an18F- labled amino acid to be used as a radio tracer for positron emission tomography（ PET）. The structure of the product was confirmed by1H- NMR,13C-NMR and mass spectroscopy.
出处
《广州化工》
CAS
2015年第2期1-3,共3页
GuangZhou Chemical Industry
基金
国家青年科学基金项目(No:21202018)
