Suppr超能文献

[ F]PARPi 的一锅法放射性合成。

A one-pot radiosynthesis of [ F]PARPi.

机构信息

Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, New York, USA.

Department of Radiology, Weill Cornell Medical College, New York, New York, USA.

出版信息

J Labelled Comp Radiopharm. 2020 Jul;63(9):419-425. doi: 10.1002/jlcr.3847. Epub 2020 Jun 16.

Abstract

In this paper, we disclose a new strategy for the radiosynthesis of [ F]PARPi from the corresponding, boc-protected, nitro-precursor. Using a two-step procedure, [ F]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.

摘要

在本文中,我们披露了一种从相应的 Boc 保护的硝基前体来放射性合成 [ F]PARPi 的新策略。采用两步法,[ F]PARPi 的放射性化学收率最高可达 9.6%。该反应通过高效的一锅两步法进行,简化了以前需要采用复杂的多步、多釜策略的方法。

相似文献

1
A one-pot radiosynthesis of [ F]PARPi.
J Labelled Comp Radiopharm. 2020 Jul;63(9):419-425. doi: 10.1002/jlcr.3847. Epub 2020 Jun 16.
2
Practical microscale one-pot radiosynthesis of F-labeled probes.
J Labelled Comp Radiopharm. 2018 Jun 15;61(7):540-549. doi: 10.1002/jlcr.3618. Epub 2018 Apr 17.
3
Radiosynthesis of [18)F]trifluoroalkyl groups: scope and limitations.
Biomed Res Int. 2014;2014:380124. doi: 10.1155/2014/380124. Epub 2014 Jul 10.
4
Radiosynthesis of novel N- F-labeled F-FHex-α-l-Glu and F-FHex-β-Glu.
J Labelled Comp Radiopharm. 2020 May 15;63(5):222-230. doi: 10.1002/jlcr.3834. Epub 2020 Mar 30.
5
Manual and automated Cu-mediated radiosynthesis of the PARP inhibitor [F]olaparib.
Nat Protoc. 2020 Apr;15(4):1525-1541. doi: 10.1038/s41596-020-0295-7. Epub 2020 Feb 28.
6
Fully automated synthesis of [(18)F]T807, a PET tau tracer for Alzheimer's disease.
Bioorg Med Chem Lett. 2015 Aug 1;25(15):2953-7. doi: 10.1016/j.bmcl.2015.05.035. Epub 2015 May 21.
7
Facile and rapid one-step radiosynthesis of [(18)F]BAY94-9172 with a new precursor.
Nucl Med Biol. 2011 Jan;38(1):121-7. doi: 10.1016/j.nucmedbio.2010.06.009. Epub 2010 Aug 16.
8
Fluorine-18 radiochemistry, labeling strategies and synthetic routes.
Bioconjug Chem. 2015 Jan 21;26(1):1-18. doi: 10.1021/bc500475e. Epub 2014 Dec 12.
9
Synthesis of F-radiolabeled organophosphine fluorides for thiol-chemoselective peptide conjugation.
J Labelled Comp Radiopharm. 2020 Dec;63(14):597-607. doi: 10.1002/jlcr.3882. Epub 2020 Oct 12.

引用本文的文献

1
Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging.
EJNMMI Radiopharm Chem. 2025 Jul 3;10(1):37. doi: 10.1186/s41181-025-00364-5.
2
[I]CC1: A PARP-Targeting, Auger Electron-Emitting Radiopharmaceutical for Radionuclide Therapy of Cancer.
J Nucl Med. 2023 Dec 1;64(12):1965-1971. doi: 10.2967/jnumed.123.265429.
4
Fully Automated, High-Dose Radiosynthesis of [F]PARPi.
Pharmaceuticals (Basel). 2022 Jul 14;15(7):865. doi: 10.3390/ph15070865.
5
DNA Repair Enzyme Poly(ADP-Ribose) Polymerase 1/2 (PARP1/2)-Targeted Nuclear Imaging and Radiotherapy.
Cancers (Basel). 2022 Feb 23;14(5):1129. doi: 10.3390/cancers14051129.
6
Two experts and a newbie: [F]PARPi vs [F]FTT vs [F]FPyPARP-a comparison of PARP imaging agents.
Eur J Nucl Med Mol Imaging. 2022 Feb;49(3):834-846. doi: 10.1007/s00259-021-05436-7. Epub 2021 Sep 6.
7
Advancements in PARP1 Targeted Nuclear Imaging and Theranostic Probes.
J Clin Med. 2020 Jul 6;9(7):2130. doi: 10.3390/jcm9072130.

本文引用的文献

1
Safety and Feasibility of PARP1/2 Imaging with F-PARPi in Patients with Head and Neck Cancer.
Clin Cancer Res. 2020 Jul 1;26(13):3110-3116. doi: 10.1158/1078-0432.CCR-19-3484. Epub 2020 Apr 3.
2
Poly(ADP-Ribose)Polymerase (PARP) Inhibitors and Radiation Therapy.
Front Pharmacol. 2020 Mar 3;11:170. doi: 10.3389/fphar.2020.00170. eCollection 2020.
4
Manual and automated Cu-mediated radiosynthesis of the PARP inhibitor [F]olaparib.
Nat Protoc. 2020 Apr;15(4):1525-1541. doi: 10.1038/s41596-020-0295-7. Epub 2020 Feb 28.
5
Targeted Brain Tumor Radiotherapy Using an Auger Emitter.
Clin Cancer Res. 2020 Jun 15;26(12):2871-2881. doi: 10.1158/1078-0432.CCR-19-2440. Epub 2020 Feb 17.
7
PET Imaging of PARP Expression Using F-Olaparib.
J Nucl Med. 2019 Apr;60(4):504-510. doi: 10.2967/jnumed.118.213223. Epub 2018 Nov 2.
8
An F-Labeled Poly(ADP-ribose) Polymerase Positron Emission Tomography Imaging Agent.
J Med Chem. 2018 May 10;61(9):4103-4114. doi: 10.1021/acs.jmedchem.8b00138. Epub 2018 Apr 19.
9
PARP-1-Targeted Radiotherapy in Mouse Models of Glioblastoma.
J Nucl Med. 2018 Aug;59(8):1225-1233. doi: 10.2967/jnumed.117.205054. Epub 2018 Mar 23.
10
A PET imaging agent for evaluating PARP-1 expression in ovarian cancer.
J Clin Invest. 2018 May 1;128(5):2116-2126. doi: 10.1172/JCI97992. Epub 2018 Apr 16.

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验