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

页码：419 / 425

页数：7

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