Methylamine → N-(2,6-Diethylphenyl)-1-methyl-8-[(1-{[3-(methylamino)propyl]sulfonyl}piperidin-4-yl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide hydrochloride

Participants

Reaction Conditions

Reaction Steps

To a solution of 8-({1-[(3-chloropropyl)sulfonyl]piperidin-4-yl}amino)-N-(2,6-diethylphenyl)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (30 mg, 0.050 mmol) in tetrahydrofurane (2 mL) in a sealed tube, methylamine (40% aqueous solution) (0.5 mL) was added. The mixture was then heated at 60° C. for 20 h. Solvent evaporated to dryness and the crude solid was purified by flash chromatography on silica gel (eluant: dichloromethane/methanol: 8/2) to 23 mg of the title compound (76% yield).

Provenance & Evidence