Organic letters, 2009-05, Vol.11 (9), p.1999-2002
2009
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Details
- Autor(en) / Beteiligte
- Titel
- Enantioselective Synthesis of Janus Kinase Inhibitor INCB018424 via an Organocatalytic Aza-Michael Reaction
- Ist Teil von
- Organic letters, 2009-05, Vol.11 (9), p.1999-2002
- Ort / Verlag
- United States: American Chemical Society
- Erscheinungsjahr
- 2009
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1523-7060eISSN: 1523-7052DOI: 10.1021/ol900350kTitel-ID: cdi_proquest_miscellaneous_67154407
- Format
- –
- Schlagworte
- Benzoates - chemistry, Catalysis, Janus Kinases - antagonists & inhibitors, Molecular Structure, Protein Kinase Inhibitors - chemical synthesis, Protein Kinase Inhibitors - chemistry, Protein Kinase Inhibitors - pharmacology, Pyrazoles - chemical synthesis, Pyrazoles - chemistry, Pyrazoles - pharmacology, Stereoisomerism