Chen C,
Pflüger PM,
Chen P,
Liu G.
* Shanghai Institute of Organic Chemistry, P. R. of China and Wilhelms-Universität Münster, Germany
Palladium(II)-Catalyzed Enantioselective Aminotrifluoromethoxylation of Unactivated Alkenes using CsOCF
3 as a Trifluoromethoxide Source.
Angew. Chem. Int. Ed. 2019;
58: 2392-2396
Key words
palladium catalysis - oxidative amination - piperidines
Significance
The authors reported an asymmetric palladium(II)-catalyzed aminotrifluoromethoxylation of unactivated alkenes leading to a variety of enantioenriched piperidines in good yields.
Comment
Remarkably, the method was used to prepare a derivative of pridinol, an antiparkinsonian and anticholineric drug, in three steps and 62% overall yield. The mild reaction conditions and the use of CsOCF3 salt make the method practical.
