Cobalt-catalyzed direct α-hydroxymethylation of amides with methanol as a C1 source.

Herein, we report a cobalt-catalyzed α-hydroxymethylation of amides with methanol under mild conditions. Using CoCl 2 ·6H 2 O as an inexpensive and efficient catalyst, some important bioactive β-hydroxyamides were obtained in moderate to excellent yields. The developed method features a wide substrate scope and good functional group tolerance. In addition, anticholinergic tropicamide was easily synthesized in this way.