Novel Method for Selective Debenzylation Under Maintenance of Fluoro Atom Substituted on β-Amino Acids

(整期优先)网络出版时间:2011-02-12
/ 1
tert-Butyl(R)-3-amino-3-(3-fluorophenyl)propanoate(5)waspreparedwithconventionaldebenzylationmethod.However,thetert-butyl(R)-3-[(S)-1-phenylethyl-amino]-3-(3-fluorophenyl)propanoate(6)andtert-butyl(R)-3-amino-3-phenylpropanoate(7)weregeneratedasthebyproductsunderthegeneralcatalytichydrogenationPd(OH)2/C-H2conditions.Soaseriesofexperimentswasperformedtooptimizethereactionconditionssothatproduct5couldbeobtainedwithhighpurityandyield.Finallyaneffectivecatalyticsystem,Pd/C-HCOOH-CH3OH,wasdiscovered.