Ammonia → HCID 66599640, compound

Participants

Reaction Steps

To tert-butyl 2-(4-(hydroxymethyl)phenyl)-3-(isoquinolin-6-ylamino)-3-oxopropylcarbamate (E139) in THF and water and cooled to 0° C. was added HCl (1 N in Et2O). After 30 min the mixture was warmed to room temperature and the solution was stirred for 48 h. 2 M NH3 in MeOH was added. The solvents were evaporated and the mixture purified by column chromatography (SiO2, 0-5-10% (2 M NH3 in MeOH)/CH2Cl2). The compound was dissolved in DCM/MeOH and 1 N HCl in Et2O added. The solvents were evaporated to give pure 3-amino-2-(4-(hydroxymethyl)phenyl)-N-(isoquinolin-6-yl)propanamide dihydrochloride (E144).

Provenance & Evidence