Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor

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A novel methodology for the synthesis of 3,3-difluoropiperidines has been developed. The target compounds are prepared in three steps using a robust protocol and simple starting materials. The incorporation of the fluorine is achieved by using the cheap and easily available ethyl 2-bromo-2,2-difluoroacetate as building block. Using this methodology, a new potent in vitro phosphodiesterase 2A (PDE2A) inhibitor containing the functionalized fluorinated piperidine scaffold has been prepared.
Original languageEnglish
JournalSYNLETT: Accounts and Rapid Communications in Chemical Synthesis
Volume27
Issue number20
Pages (from-to)2803-2806
Number of pages4
ISSN0936-5214
DOIs
Publication statusPublished - Dec 2016

    Research areas

  • fluorine, piperidine, ethyl 2-bromo-2,2-difluoroacetate, reductive amination, phosphodiesterase

ID: 172089965