Chiral proton catalysis of secondary nitroalkane additions to azomethine: Synthesis of a potent GlyT1 inhibitor
The first enantioselective synthesis of a potent GlyT1 inhibitor is described. A 3-nitroazetidine donor is used in an enantioselective aza-Henry reaction catalyzed by a bis(amidine)-triflic acid salt organocatalyst, delivering the key intermediate with 92% ee. This adduct is reductively denitrated and converted to the target through a short sequence, thereby allowing assignment of the absolute configuration of the more potent enantiomer.
Davis, Tyler A.,Danneman, Michael W.,Johnston, Jeffrey N.
p. 5578 - 5580
(2012/07/17)
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