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[F]FeF 物种开环环氧化物以生成 [F]氟代醇 PET 成像剂。

Ring opening of epoxides with [F]FeF species to produce [F]fluorohydrin PET imaging agents.

机构信息

Division of Nuclear Medicine, Department of Radiology, The University of Michigan Medical School, Ann Arbor, Michigan 48109, USA.

出版信息

Chem Commun (Camb). 2019 May 30;55(45):6361-6364. doi: 10.1039/c9cc02779c.

DOI:10.1039/c9cc02779c
PMID:31062010
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6542722/
Abstract

A simple technique for the preparation of [18F]HF has been developed and applied to the generation of an [18F]FeF species for opening sterically hindered epoxides. This method has been successfully employed to prepare four drug-like molecules, including 5-[18F]fluoro-6-hydroxy-cholesterol, a potential adrenal/endocrine PET imaging agent. This easily automated one-pot procedure produces sterically hindered fluorohydrin PET imaging agents in good yields and high molar activities.

摘要

已经开发出一种用于制备[18F]HF 的简单技术,并将其应用于生成用于打开空间位阻环氧化物的[18F]FeF 物种。该方法已成功用于制备四种类似药物的分子,包括 5-[18F]氟-6-羟基胆固醇,一种潜在的肾上腺/内分泌 PET 成像剂。这种易于自动化的一锅法以高收率和高摩尔活度制备空间位阻氟醇 PET 成像剂。

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