New Strategy for the Preparation of Clickable Peptides and Labeling with 1-(Azidomethyl)-4-[18F]-fluorobenzene for PET
New Strategy for the Preparation of Clickable Peptides and Labeling with 1-(Azidomethyl)-4-[18F]-fluorobenzene for PET
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DOI：
10.1021/bc800544p
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发表时间：
2009-04-01
影响因子：
4.7
通讯作者：
Luxen, Andre
中科院分区：
文献类型：
--
作者：
Thonon, David;Kech, Cecile;Luxen, Andre
炔-叠氮化物Cu（I）-催化的Huisgen环加成，点击型反应用于用氟-18标记肽。已经开发了用于制备可点击肽的新型固相合成方法，并且还允许直接制备参考化合物。一个互补的叠氮标记剂（1-（叠氮甲基）-4-[F-18]-氟苯）已在75分钟内以34%的放射化学产率（衰变校正）在四个步骤中产生。[F-18]氟叠氮化物与模型炔神经肽的缀合物在不到15分钟内产生所需的F-18-放射性标记的肽，产率为90%，具有优异的放射化学纯度。
The alkyne-azide Cu(I)-catalyzed Huisgen cycloaddition, a click type reaction was used to label a peptide with fluorine-18. A novel solid phase synthesis approach for the preparation of clickable peptides has been developed and has also permitted the straightforward preparation of reference compounds. A complementary azide labeling agent (1-(azidomethyl)-4-[F-18]-fluorobenzene) has been produced in a four step procedure in 75 min with a 34% radiochemical yield (decay corrected). Conjugation of [F-18]fluoroazide with a model alkyne-neuropeptide produced the desired F-18-radiolabeled peptide in less than 15 min with a yield of 90% and excellent radiochemical purity.