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一种用于[F]JNJ-46356479和[F]FITM全自动放射性合成的简便方法:有机硼烷的铜介导F-氟化反应。

A concise method for fully automated radiosyntheses of [F]JNJ-46356479 and [F]FITM Cu-mediated F-fluorination of organoboranes.

作者信息

Yuan Gengyang, Shoup Timothy M, Moon Sung-Hyun, Brownell Anna-Liisa

机构信息

Gordon Center for Medical Imaging, Massachusetts General Hospital and Harvard Medical School, 3rd Avenue, Charlestown, MA 02129, USA. Email:

出版信息

RSC Adv. 2020 Jul 2;10(42):25223-25227. doi: 10.1039/d0ra04943c.

Abstract

A modified alcohol-enhanced F-fluorodeboronation has been developed for the radiosyntheses of [F]JNJ-46356479 and [F]FITM. Unlike the [F]KF/K approach, this method tolerates the presence of sensitive heterocycles in Bpin precursors and allowing a one-step F-fluorodeboronation on the fully automated TRACERlab™ FX platform.

摘要

一种改进的酒精增强型F-氟脱硼反应已被开发用于[F]JNJ-46356479和[F]FITM的放射性合成。与[F]KF/K方法不同,该方法能够容忍Bpin前体中敏感杂环的存在,并允许在全自动TRACERlab™ FX平台上进行一步F-氟脱硼反应。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f2c0/9055233/d7b83e0aa250/d0ra04943c-f1.jpg

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