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

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

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.
OriginalsprogEngelsk
TidsskriftSYNLETT: Accounts and Rapid Communications in Chemical Synthesis
Vol/bind27
Udgave nummer20
Sider (fra-til)2803-2806
Antal sider4
ISSN0936-5214
DOI
StatusUdgivet - dec. 2016

ID: 172089965