Enantioselective Formal C(sp3)−H Bond Activation in the Synthesis of Bioactive Spiropyrazolone Derivatives

Herein, we report the first enantioselective annulation of α‐arylidene pyrazolones through a formal C(sp3)−H activation under mild conditions enabled by highly variable RhIII‐Cpx catalysts. The method has a wide substrate scope and proceeds with good to excellent yields and enantioselectivities. Its...

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Veröffentlicht in:	Angewandte Chemie International Edition 2019-01, Vol.58 (1), p.307-311
Hauptverfasser:	Li, Houhua, Gontla, Rajesh, Flegel, Jana, Merten, Christian, Ziegler, Slava, Antonchick, Andrey P., Waldmann, Herbert
Format:	Artikel
Sprache:	eng
Schlagworte:	Activation asymmetric catalysis Catalysts Chemical reactions C−H activation Enantiomers Hedgehog pathway inhibitors Natural products Organic chemistry Pyrazolones rhodium spiropyrazolones Substrates
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