1-Methylpiperazine → 2-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-N-{6-[6-(methyloxy)-5-({[2-(4-methyl-1-piperazinyl)ethyl]sulfonyl}amino)-3-pyridinyl]-1H-indazol-4-yl}-1,3-thiazole-4-carboxamide

Participants

Reaction Steps

Acetonitrile (10 ml) was added to 2-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-N-[6-[5-[(ethenylsulfonyl)amino]-6-(methyloxy)-3-pyridinyl]-2-(tetrahydro-2H-pyran-2-yl)-2H-indazol-4-yl]-1,3-thiazole-4-carboxamide (250 mg) followed by 1-methylpiperazine (0.33 ml). The reaction was stirred at RT for 3 hours. The reaction was evaporated to dryness and the residue was separated between DCM and water. The DCM was passed through a hydrophobic frit then evaporated to dryness. The residue was dissolved in DMSO:methanol (1:1, v/v, 2 ml) and purified by MDAP (method E). Pure fractions were combined and evaporated to dryness. Analysis showed complete deprotection on dry-down to give title compound (116 mg).

Provenance & Evidence