Methanol--water (1/1) → 5-Bromo-2-hydroxy-6-(3-methylpiperidin-1-yl)-benzo[de]isoquinoline-1,3-dione

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-benzyloxy-5-bromo-6-(3-methyl-piperidin-1-yl)-benzo[de]isoquinoline-1,3-dione (0.24 g, 0.50 mmol, from Example U1) in TFA (8.0 mL) at 0° C. was added a 1.0 M solution of boron tris(trifluoroacetate) in TFA (5 mL). The reaction was stirred at 0° C. for 2 hours, then poured into a solution of water/methanol (1:1), and extracted with chloroform. The organic layer was dried over MgSO4, filtered, and the solvent removed under vacuum to give 0.19 g of the title compound as the TFA salt, mp >250° C.

Provenance & Evidence