The highly chemo- and enantioselective hydrogenation of ()-2-substituted-4-oxo-2-alkenoic acids was established for the first time using the Rh/JosiPhos complex, affording a series of chiral -substituted--keto acids with excellent results (up to 99% yield and >99% ) and high efficiency (up to 3000 TON). In addition, the importance of this methodology was further demonstrated by a concise and gram-scale synthesis of the anti-inflammatory drug ()-flobufen.
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| http://dx.doi.org/10.1021/acs.orglett.0c01618 | DOI Listing |
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