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Ring opening of epoxides with [18F]FeF species to produce [18F]fluorohydrin PET imaging agents.

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.

SUBMITTER: Verhoog S

PROVIDER: S-EPMC6542722 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature

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Ring opening of epoxides with [<sup>18</sup>F]FeF species to produce [<sup>18</sup>F]fluorohydrin PET imaging agents.

Verhoog Stefan S Brooks Allen F AF Winton Wade P WP Viglianti Benjamin L BL Sanford Melanie S MS Scott Peter J H PJH

Chemical communications (Cambridge, England) 20190501 45

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. ...[more]

PMID: 31062010

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