Methylamine → 4-{2-[2-Amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]-3-methyl-1,2,3,4-tetrahydroisoquinolin-7-yl}-N,1-dimethyl-1H-pyrrole-2-carboxamide

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Reaction Steps

4-{2-[2-Amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]-3-methyl-1,2,3,4-tetrahydroisoquinolin-7-yl}-1-methyl-1H-pyrrole-2-carboxylic acid (12.0 mg, 0.0260 mmol) and benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (0.0192 g, 0.0433 mmol) in DMF (0.5 mL) was stirred at r.t. for 3 min. and then methylamine in THF (2.0M, 0.2 mL, 0.4 mmol) was added. To this mixture, triethylamine (15.4 uL, 0.110 mmol) was slowly added and the mixture was stirred for 1 h at r.t. The mixture was purified by RP-HPLC (pH=10) to afford the desired product. LCMS (M+H)+: m/z=475.3.

Provenance & Evidence