Enantioselective Formal C(sp3 )-H Bond Activation in the Synthesis of Bioactive Spiropyrazolone Derivatives.
Angew Chem Int Ed Engl
; 58(1): 307-311, 2019 01 02.
Article
en En
| MEDLINE
| ID: mdl-30511449
ABSTRACT
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 synthetic utility was demonstrated by the late-stage functionalization of drugs and natural products as well as the preparation of enantioenriched [3]dendralenes. Preliminary biological investigations also identified the spiropyrazolones as a novel class of Hedgehog pathway inhibitors.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Compuestos de Espiro
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Año:
2019
Tipo del documento:
Article
País de afiliación:
Alemania