Hydrazine → HCID 58541884, compound

Participants

Reaction Conditions

Reaction Steps

To a vial is added 2-[5-(2-amino-pyrimidin-5-yl)-1-tert-butyl-1H-benzimidazol-2-yl]-benzoic acid methyl ester (example 16) (85 mg, 0.212 mmol) in EtOH (5 mL), follow by the addition of hydrazine (35 wt % solution in water) (1 mL). The reaction mixture is stirred at 80° C. for 5 days. The reaction mixture is concentrated in vacuo. The residue is loaded to a silica gel column. The column is eluted with 0-10% 2M NH3 in MeOH/CH2Cl2. The product fractions are collected and is concentrated to afford 2-[5-(2-amino-pyrimidin-5-yl)-1-tert-butyl-1H-benzimidazol-2-yl]-benzoic acid hydrazide (43 mg, 51%) as a off-white solid. LCMS (ESMS): m/z 402.57 (M++1)

Provenance & Evidence