Synthesis of 3-acylated 1-aminoisoquinolin-4-ols via construction of a fully substituted pyridine moiety.

Described herein is an annulative functionalization approach to synthesize the 3-acylated 1-aminoisoquinolin-4-ol skeleton from a base-catalyzed reaction of 2-formylbenzonitrile with α-azidoketone under mild conditions, enabling the facile assembly of a fully functionalized aminopyridinol moiety via a domino procedure involving an aldol reaction, imine formation, tautomerization, and cycloisomerization.