Enantioselective organocatalytic Hantzsch synthesis of polyhydroquinolines.
Evans, Christopher G;Gestwicki, Jason E;
Organic letters2009Vol. 11pp. 2957-9
292
evans2009enantioselectiveorganic
Abstract
The four-component Hantzsch reaction provides access to pharmaceutically important dihydropyridines. To expand the utility of this method, we have developed a route under organocatalytic conditions with good yields and excellent ee's. Through catalyst screening, we found that a BINOL-phosphoric acid allowed enantioselective synthesis of six-membered heterocycles with a variety of substitution patterns.