1,4-Dioxane hydrochloride → Cyclopropanesulfonic acid [14-amino-18-(isoquinolin-1-yloxy)-2,15-dioxo-3,16-diaza-tricyclo[14.3.0.04,6]nonadec-7-ene-4-carbonyl)-amide bis hydrochloride

Participants

Reaction Steps

A stirred slurry of [4-cyclopropane-sulfonylaminocarbonyl-18-(isoquinolin-1-yloxy)-2,15-dioxo-3,16-diaza-tricyclo[14.3.0.04,6]nonadec-7-en-14-yl]-carbamic acid tert-butyl ester (1.20 g, 1.7 mmol) was treated with 4N HCl/dioxane (Aldrich)(10 mL) for 4 h. The reaction mixture was concentrated in vacuo to give 1.10 g (92%) of cyclopropanesulfonic acid [14-amino-18-(isoquinolin-1-yloxy)-2,15-dioxo-3,16-diaza-tricyclo[14.3.0.04,6]nonadec-7-ene-4-carbonyl]-amide bis hydrochloride as a white solid: LC-MS (Method B, retention time: 1.39 min), MS m/z 596 (M++1–2HCl).

Provenance & Evidence