p-Toluenesulfonic acid monohydrate → N2-((1H-Indazol-4-yl)methyl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine

Participants

Reaction Conditions

Reaction Steps

To a solution of 200 (215 mg, 0.5 mmol) in MeOH (5 mL) and water (1 mL) was added p-TsOH.H2O (95 mg, 0.5 mmol) and the mixture was heated in a sealed tube at 80° C. overnight. The solvent was evaporated in vacuo. The residue was purified by preparative HPLC to afford 110 mg (63%) of I-59 as white solid.

Provenance & Evidence