(R)-3-(2-(2-(hydroxymethyl)pyrrolidin-1-yl)ethyl)-5-methylisoquinolin-1(2H)-one → (R)-3-[2-(2-hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one monomesylate

Participants

Reaction Conditions

Reaction Steps

To a solution (4 mL) of a free form (500 mg) of (R)-3-[2-(2-hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one in ethanol was added dropwise 2M methanesulfonic acid ethanol solution (1 mL) with stirring on an oil bath at 50° C. The bath was removed, ethyl acetate (8 mL) and seed crystals were added and the mixture was stirred to allow precipitation of crystals. After stirring under ice-cooling, the crystals were collected through filtration, washed with ethyl acetate/ethanol (2:1) and dried under reduced pressure at 50° C. for 18 hr to give the title compound (507 mg).

Provenance & Evidence