((2R)-2-(Cyclopentylmethyl)-3-{2-[5-fluoro-6-(4-methyl-1-piperazinyl)-2-(methylthio)-4-pyrimidinyl]hydrazino}-3-oxopropyl)(tetrahydro-2H-pyran-2-yloxy)formamide → HCID 58000621, compound

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Reaction Steps

((2R)-2-(Cyclopentylmethyl)-3-{2-[5-fluoro-6-(4-methyl-1-piperazinyl)-2-(methylthio)-4-pyrimidinyl]hydrazino}-3-oxopropyl)(tetrahydro-2H-pyran-2-yloxy)formamide (2.5 g, 22.58 mmol) was dissolved in acetic acid/water (4:1, 1 L) and stirred at RT for 3 days. The reaction mixture was concentrated to dryness and co-evaporated with toluene (20 mL) followed by methanol (50 mL)/triethylamine (20 mL). The residue was dissolved in methanol (120 mL) and triethylamine (20 mL) and purified by Gilson HPLC (10-95% acetonitrile/water, 8 min gradient time) to provide ((2R)-2-(cyclopentylmethyl)-3-{2-[5-fluoro-6-(4-methyl-1-piperazinyl)-2-(methylthio)-4-pyrimidinyl]hydrazino}-3-oxopropyl)hydroxyformamide as a reddish foamy solid (6.90 g, 65.1%). LCMS: (M+H)+: 470.2.

Provenance & Evidence