Click for PET:: rapid preparation of [18F]fluoropeptides using CuI catalyzed 1,3-dipolar cycloaddition
Click for PET:: rapid preparation of [18F]fluoropeptides using CuI catalyzed 1,3-dipolar cycloaddition
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DOI：
10.1016/j.tetlet.2006.06.176
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发表时间：
2006-09-11
影响因子：
1.8
通讯作者：
Sutcliffe, Julie L.
中科院分区：
文献类型：
--
作者：
Marik, Jan;Sutcliffe, Julie L.
利用铜-I催化的1，3-偶极环加成‘点击化学’制备了F-18标记多肽。合成了三种欧米伽-[F-18]-氟炔烃，产率1为36%~81%。通过铜-I介导的1，3-偶极环加成反应，将欧米伽-[F-18]氟炔与3-叠氮丙酸修饰的多肽偶联，在10分钟内得到了所需的F-18标记产物，产率为54-99%，放化纯度为81-99%。总合成时间为轰击结束后30min。(C)2006爱思唯尔有限公司。保留所有权利。
Cu-I catalyzed 1,3-dipolar cycloaddition 'click chemistry' was used to prepare F-18-radiolabeled peptides. Three omega-[F-18]-fluoroalkynes were prepared in yields 1 ranging from 36% to 81%. Conjugation of omega-[F-18]fluoroalkynes to various peptides decorated with 3-azidopropionic acid via Cu-I mediated 1,3-dipolar cycloaddition yielded the desired F-18-labeled products in 10 min with yields of 54-99% and excellent radiochemical purity (81-99%). The total synthesis time was 30 min from the end of bombardment. (c) 2006 Elsevier Ltd. All rights reserved.