Hydrochloric Acid → 1000210-63-8

Participants

Reaction Steps

Slurry 4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol (16.57 g, 50.45 mmol) in methanol (500 mL). Separately, prepare a solution of HCl in methanol by adding acetyl chloride (12.60 mL, 177.05 mmol) to methanol (165 mL). Add the solution of HCl in methanol dropwise at room temperature over 30 min to the slurry of 4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol in methanol. Stir for 30 min, then add ethyl acetate (600 mL) dropwise over 1 hour. Stir for 30 min, then filter the solids and wash with ethyl acetate (2×100 mL). Dry solids in vacuo at 50° C., then further dry in vacuo at room temperature with slow administration of nitrogen to afford the title compound (18.3 g, 90%). Mass spectrum (LCMS) m/z=329.0 (M+H+).

Provenance & Evidence