A one-pot radiosynthesis of [18F]PARPi

被引：8
作者：
Wilson, Thomas C. [1 ]
Pillarsetty, Nagavarakishore [1 ,2 ]
Reiner, Thomas [1 ,2 ,3 ]
机构：
[1] Mem Sloan Kettering Canc Ctr, Dept Radiol, 1275 York Ave, New York, NY 10021 USA
[2] Weill Cornell Med Coll, Dept Radiol, New York, NY USA
[3] Mem Sloan Kettering Canc Ctr, Chem Biol Program, 1275 York Ave, New York, NY 10021 USA
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2020年 / 63卷 / 09期
基金：
美国国家卫生研究院;
关键词：
F-18]PARPi; fluorine-18; Olaparib; PARP inhibitor; PET chemistry; radiochemistry; ADP-RIBOSE POLYMERASE-1; IN-VIVO; PARP1; EXPRESSION; POLY(ADP-RIBOSE); PET;
D O I：
10.1002/jlcr.3847
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
In this paper, we disclose a new strategy for the radiosynthesis of [F-18]PARPi from the corresponding, boc-protected, nitro-precursor. Using a two-step procedure, [F-18]PARPi could be isolated in radiochemical yields up to 9.6%. The reaction proceeds via an efficient one-pot, two-step process, allowing for simplification over previous methods that require complex multi-step, multi-pot strategies to be implemented.
引用
收藏
页码：419 / 425
页数：7
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