Enantioselective Synthesis of 2-Aryl-4-piperidones
R. B. C. Jagt, J. G. de Vries, B. L. Feringa*, A. J. Minnaard
University of Groningen, The Netherlands
21 September 2005 (online)
A highly enantioselective synthesis of 2-aryl-4-piperidones is reported using a rhodium/phospharamidite-catalyzed conjugate addition of arylboroxines to 2,3-dihydro-4-pyridones. The enantioselectivity remains very high for both electron-rich and electron-deficient arylboroxines, although the yields are diminished with electron-poor arylboroxines.