ABSTRACT
A new strategy for the synthesis of chiral α-amino phosphonates by enantioselective C-H phosphonylation of allylamine with phosphite in the presence of a chiral Brønsted acid catalyst has been developed. This protocol successfully integrates direct C-H oxidation with asymmetric phosphonylation and exhibits high enantioselectivity.
ABSTRACT
The first Cu-catalyzed cascade sp(3) C-H bond oxidative functionalization of the 2-ethylazaarenes has been developed. The two different sp(3) C-H bonds in 2-ethylazaarenes are selectively oxidized and four new types of bonds (C=O, C=N, C-C, C-O) are constructed in one operation. Starting from the simple substrates and cheap nitro source, this reaction provides an efficient approach to produce new kinds of isoxazolines.
