1-Hydroxybenzotriazole → 5-Bromoisoquinolin-4-carboxylic amide

Participants

Reaction Steps

To a stirred solution of 5-bromoisoquinoline-4-carboxylic acid (Intermediate-17) (1 equiv, 2.0 mmol) in dry THF (10.0 ml) were added, DIPEA (3 equiv), HOBT (1.5 equiv), EDC.HCl (1.5 equiv) at RT and the mixture was stirred for 10 min. To this, corresponding amine (1.2 equiv) was added and the reaction mixture was stirred overnight. After completion (TLC), it was concentrated under reduced pressure and the crude product was purified by flash column chromatography to furnish the corresponding amide derivative (60-80%).

Provenance & Evidence