Synthesis of enantioenriched azo compounds: organocatalytic Michael addition of formaldehyde N-tert-butyl hydrazone to nitroalkenes

Org Biomol Chem. 2013 Jan 14;11(2):326-35. doi: 10.1039/c2ob26963e. Epub 2012 Nov 22.

Abstract

The unprecedented diaza-ene reaction of formaldehyde N-tert-butyl hydrazone with nitroalkenes can be efficiently catalyzed by an axially chiral bis-thiourea to afford the corresponding diazenes in good to excellent yields (60-96%) and moderate enantioselectivities, up to 84 : 16 er; additional transformation of diazenes into their tautomeric hydrazones proved to be operationally simple and high-yielding, affording bifunctional compounds which represent useful intermediates for the synthesis of enantioenriched β-nitro-nitriles and derivatives thereof.