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

共 36 条

[1] Dual-Modality Optical/PET Imaging of PARP1 in Glioblastoma [J].

Carlucci, Giuseppe ;

Carney, Brandon ;

Brand, Christian ;

Kossatz, Susanne ;

Irwin, Christopher P. ;

Carlin, Sean D. ;

Keliher, Edmund J. ;

Weber, Wolfgang ;

Reiner, Thomas .

MOLECULAR IMAGING AND BIOLOGY, 2015, 17 (06) :848-855

[2] Target engagement imaging of PARP inhibitors in small-cell lung cancer [J].

Carney, Brandon ;

Kossatz, Susanne ;

Lok, Benjamin H. ;

Schneeberger, Valentina ;

Gangangari, Kishore K. ;

Pillarsetty, Naga Vara Kishore ;

Weber, Wolfgang A. ;

Rudin, Charles M. ;

Poirier, John T. ;

Reiner, Thomas .

NATURE COMMUNICATIONS, 2018, 9

[3] Molecular Imaging of PARP [J].

Carney, Brandon ;

Kossatz, Susanne ;

Reiner, Thomas .

JOURNAL OF NUCLEAR MEDICINE, 2017, 58 (07) :1025-1030

[4] Non-invasive PET Imaging of PARP1 Expression in Glioblastoma Models [J].

Carney, Brandon ;

Carlucci, Giuseppe ;

Salinas, Beatriz ;

Di Gialleonardo, Valentina ;

Kossatz, Susanne ;

Vansteene, Axel ;

Longo, Valerie A. ;

Bolaender, Alexander ;

Chiosis, Gabriela ;

Keshari, Kayvan R. ;

Weber, Wolfgang A. ;

Reiner, Thomas .

MOLECULAR IMAGING AND BIOLOGY, 2016, 18 (03) :386-392

[5] 18F-labelling innovations and their potential for clinical application [J].

Coenen, Heinz H. ;

Ermert, Johannes .

CLINICAL AND TRANSLATIONAL IMAGING, 2018, 6 (03) :169-193

[6] Fluorine-18 labeled poly (ADP-ribose) polymerase1 inhibitor as a potential alternative to 2-deoxy-2-[18F]fluoro-D-glucose positron emission tomography in oral cancer imaging [J].

de Souza Franca, Paula Demetrio ;

Roberts, Sheryl ;

Kossatz, Susanne ;

Guru, Navjot ;

Mason, Christian ;

Zanoni, Daniella Karassawa ;

Abrahao, Marcio ;

Schoder, Heiko ;

Ganly, Ian ;

Patel, Snehal G. ;

Reiner, Thomas .

NUCLEAR MEDICINE AND BIOLOGY, 2020, 84-85 :80-87

[7]

Edmonds CE, 2016, AM J NUCL MED MOLEC, V6, P94

[8] Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy [J].

Farmer, H ;

McCabe, N ;

Lord, CJ ;

Tutt, ANJ ;

Johnson, DA ;

Richardson, TB ;

Santarosa, M ;

Dillon, KJ ;

Hickson, I ;

Knights, C ;

Martin, NMB ;

Jackson, SP ;

Smith, GCM ;

Ashworth, A .

NATURE, 2005, 434 (7035) :917-921

[9] Evolution of Poly(ADP-ribose) Polymerase-1 (PARP-1) Inhibitors. From Concept to Clinic [J].

Ferraris, Dana V. .

JOURNAL OF MEDICINAL CHEMISTRY, 2010, 53 (12) :4561-4584

[10] Manual and automated Cu-mediated radiosynthesis of the PARP inhibitor [18F]olaparib [J].

Guibbal, Florian ;

Isenegger, Patrick G. ;

Wilson, Thomas C. ;

Pacelli, Anna ;

Mahaut, Damien ;

Sap, Jeroen B. I. ;

Taylor, Nicholas J. ;

Verhoog, Stefan ;

Preshlock, Sean ;

Hueting, Rebekka ;

Cornelissen, Bart ;

Gouverneur, Veronique .

NATURE PROTOCOLS, 2020, 15 (04) :1525-1541

← 1 2 3 4 →