Diisopropylethylamine → Methyl 8-methoxyisoquinoline-3-carboxylate

Participants

Reaction Steps

224 mg (1.1 mmol) of 6-methoxy-isoquinoline-3-carboxylic acid was reacted with 242 mg (1 mmol) of intermediate B (2-amino-3H-benzoimidazole-4-carboxylic acid (1H-imidazol-2-yl)-amide), 569 mg (1.5 mmol) of HBTU, 0.704 ml (4 mmol) of DIEA and 5 mL of DMF stirring at 80° C. for 2 h as describe in general procedure A to provide 212.4 mg (50%) of the title compound. 1H-NMR (400 MHz, DMSO): 9.37 (s, 1H), 8.71 (s, 1H), 8.24 (d, 1H), 7.94 (d, 1H), 7.82 (d, 1H), 7.73 (d, 1H), 7.49 (dd, 1H), 7.34 (t, 1H), 6.88 (s, 1H), 6.76 (s, 1H), 3.98 (s, 3H) ppm; LCMS: 428 (M+1)+.

Provenance & Evidence