Journal
ORGANIC LETTERS
Volume 11, Issue 9, Pages 1999-2002Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol900350k
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An enantioselective synthesis of INCB018424 via organocatalytic asymmetric aza-Michael addition of pyrazoles (16 or 20) to (E)-3-cyclopentylacrylaldehyde (23) using diarylprolinol silyl ether as the catalyst was developed. Michael adducts (R)-24 and (R)-27 were isolated in good yield and high ee and were readily converted to INCB018424.
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