51431-58-4Relevant academic research and scientific papers
Regio- and Enantioselective Preparation of Chiral Allylic Sulfones Featuring Elusive Quaternary Stereocenters
Cai, Aijie,Kleij, Arjan W.
, p. 14944 - 14949 (2019)
We describe here the first general asymmetric synthesis of sterically encumbered α,α-disubstituted allylic sulfones via Pd-catalyzed allylic substitution. The design and application of a new and highly efficient phosphoramidite ligand (L10) proved to be crucial, and a wide variety of challenging allylic sulfones featuring quaternary stereocenters could be obtained in good yields and with good to excellent levels of regio- and enantioselectivities under attractive process conditions. The developed methodology employs easily accessible chemical feedstock including racemic allylic precursors and sodium sulfinates. The utility of the method is further demonstrated by the synthesis of the sesquiterpene (?)-Agelasidine A.
BACE INHIBITORS
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Page/Page column 11, (2009/12/02)
The present invention provides BACE inhibitors of Formula I: methods for their use, and intermediates and methods for their preparation.
