4-Chloroquinazoline → 4-Aminoquinazoline

Participants

Reaction Steps

4-Chloro quinazoline derivative 3a was reacted with the primary amine 2d in the presence of Hunig's base to provide the 4-amino quinazoline intermediate 3b. Ammonolysis of the ester group with 7N ammonia/methanol solution afforded carboxamide 3c. When R4 is a protecting Nosyl group, deprotection with cesium carbonate in the presence of thiophenol provides 3d.

Provenance & Evidence