Methanesulfonic Acid → Taprizosin mesylate

Participants

Reaction Steps

A suspension of Form E 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1,2,3,4-tetrahydro-2-isoquinolyl)-5-(2-pyridyl)quinazoline (1.0 g, 1.97 mmol) in acetone/water (12/7 by volume, 9.5 ml) was heated to reflux. Methanesulfonic acid (0.19 g, 1.99 mmol) was added in one portion. The addition vessel was washed with water (1 ml) and the resulting solution left to cool to room temperature overnight. The solid from the resulting suspension was collected by filtration and dried overnight in vacuo at 45° C. to afford the title compound (1.14 g) as a white solid.

Provenance & Evidence