Acetic Acid → HCID 58000601, compound

Participants

Reaction Steps

A solution of [(2R)-3-(2-{2-chloro-5-fluoro-6-[3-methyl-3-(1-pyrrolidinyl)-1-azetidinyl]-4-pyrimidinyl}hydrazino)-2-(cyclopentylmethyl)-3-oxopropyl](tetrahydro-2H-pyran-2-yloxy)formamide (145 mg) in 4:1 AcOH:water (20 mL) was stirred at room temperature overnight. LCMS indicated ˜45% completion of the deprotection. Another portion of the mixed solvents (4:1 AcOH:water, 20 mL) was added, and stirring continued overnight. The solvents were then removed in vacuo, and the resulting crude product was purified by RP-HPLC to provide [(2R)-3-(2-{2-chloro-5-fluoro-6-[3-methyl-3-(1-pyrrolidinyl)-1-azetidinyl]-4-pyrimidinyl}hydrazino)-2-(cyclopentylmethyl)-3-oxopropyl]hydroxyformamide (45 mg, 36%). LCMS: (M+H)+: 498.2.

Provenance & Evidence