2-(4-(2-(3-((Benzyloxycarbonylamino)methyl)-4-(ethylsulfonyl)phenylamino)-2-oxoethoxy)-3,5-dimethylphenyl)-2-(1-(bis(tert-butoxycarbonyl)amino)isoquinolin-6-ylamino)acetic acid → 2-(4-(2-(3-(Aminomethyl)-4-(ethylsulfonyl)phenylamino)-2-oxoethoxy)-3,5-dimethylphenyl)-2-(1-(bis(tert-butoxycarbonyl)amino)isoquinolin-6-ylamino)acetic acid

Participants

Reaction Steps

To a solution of 79D (190 mg, 0.205 mmol) in 5 mL methanol, was added 10% Pd—C (30 mg). The reaction was evacuated and flushed with H2 (3×), then stirred under an atmosphere of H2 for 1 h. The reaction was filtered and concentrated to afford 151 mg (93%) of 79E as an orange solid. MS (ESI) m/z 926.5 (M+H)+.

Provenance & Evidence