Direct Asymmetric Amination of α-Branched Cyclic Ketones Catalyzed by a Chiral Phosphoric Acid

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Direct asymmetric amination of α-branched cyclic ketones catalyzed by a chiral phosphoric acid.

Here we report the direct asymmetric amination of α-substituted cyclic ketones catalyzed by a chiral phosphoric acid, yielding products with a N-containing quaternary stereocenter in high yields and excellent enantioselectivities. Kinetic resolution of the starting ketone was also found to occur on some of the substrates under milder conditions, providing enantioenriched α-branched ketones, ano...

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Asymmetric addition of α-branched cyclic ketones to allenamides catalyzed by a chiral phosphoric acid† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c5sc04202j Click here for additional data file.

We describe the asymmetric addition of unactivated α-branched cyclic ketones to allenamides catalyzed by a chiral phosphoric acid, generating an all-carbon quaternary stereocenter with broad substrate scope and high enantioselectivity. The products are easily transformed into their corresponding 1,5- and 1,4-ketoaldehyde derivatives, which are both important building blocks in organic synthesis.

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ژورنال

عنوان ژورنال: Journal of the American Chemical Society

سال: 2015

ISSN: 0002-7863,1520-5126

DOI: 10.1021/jacs.5b00229