HCID 86636995, compound → HCID 58000543, compound

Participants

Reaction Steps

[(2R)-3-{2-[2-Chloro-5-fluoro-6-(tetrahydro-2H-pyran-4-ylamino)-4-pyrimidinyl]hydrazino}-2-(cyclopentylmethyl)-3-oxopropyl][(phenylmethyl)oxy]formamide (0.321 g, 0.58 mmol), Pd(OH)2 (0.064 g) and MeOH (10 mL) were combined and treated as described in General Procedure E, Part D, for 4 hours. The reaction was not complete, and therefore the contents were filtered to remove the catalyst, and the filtrate was concentrated in vacuo. The resulting residue was redissolved in MeOH (10 mL), Pd(OH)2 (0.080 g) was, and the contents were again stirred under hydrogenation conditions as described in General Procedure E, Part D, for 2.5 hours. The contents were then filtered to remove the catalyst, and the filtrate was concentrated in vacuo. The resulting crude product was purified by RP-HPLC to provide [(2R)-3-{2-[2-chloro-5-fluoro-6-(tetrahydro-2H-pyran-4-ylamino)-4-pyrimidinyl]hydrazino}-2-(cyclopentylmethyl)-3-oxopropyl]hydroxyformamide as an off-white solid (0.024 g, 9%). LCMS: (M+H)+=459.5.

Provenance & Evidence