1 research outputs found
Highly Enantioselective Synthesis of Dihydroquinazolinones Catalyzed by SPINOL-Phosphoric Acids
The asymmetric condensation/amine
addition cascade sequence of
2-aminobenzamides and aldehydes catalyzed by chiral spirocyclic SPINOL-phosphoric
acids was realized. SPINOL-phosphoric acid <b>1j</b> was found
to be a general, highly enantioselective organocatalyst for such cascade
reactions at room temperature, affording 2,3-dihydroquinazolinones
in excellent yields (up to 99%) with good to excellent ee’s
(up to 98%). The best level of stereocontrol was obtained for aromatic
aldehydes with an ortho substituent