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Abstract
A chiral phosphoric acid-catalyzed efficient, operationally simple, general method for straightforward syntheses of axially chiral arylpyrazole employing 3-aryl-5-aminopyrazoles reacting with azonaphthalenes was firstly reported. A wide variety of axially chiral heterobiaryl diamines in generally good yields with excellent enantioselectivities were obtained under mild conditions. In addition, a scale-up experiment and postmodification of the chiral product further highlighted the synthetic utility.
Supplementary materials
Title
Chiral Phosphoric Acid-Catalyzed Asymmetric Synthesis of Axially Chiral Arylpyrazole
Description
A chiral phosphoric acid-catalyzed efficient, operationally simple, general method for straightforward syntheses of axially chiral arylpyrazole employing 3-aryl-5-aminopyrazoles reacting with azonaphthalenes was firstly reported. A wide variety of axially chiral heterobiaryl diamines in generally good yields with excellent enantioselectivities were obtained under mild conditions. In addition, a scale-up experiment and postmodification of the chiral product further highlighted the synthetic utility.
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