Ethanol → N-Cyclopropyl-3-fluoro-5-(2-{[1-(hydroxymethyl)cyclopropyl]methyl}-1-oxo-4-{[(3R)-piperidin-3-ylmethyl]sulfanyl}-1,2-dihydroisoquinolin-6-yl)-4-methylbenzamide

Participants

Reaction Steps

A solution of tert-Butyl (3R)-3-{[(2-{[1-({[tert-butyl(dimethyl)silyl]oxy}methyl)-cyclopropyl]methyl}-6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-1-oxo-1,2-dihydroisoquinolin-4-yl)sulfanyl]methyl}piperidine-1-carboxylate (Example 63e, 110 mg) in 4N HCl in dioxane (1 mL) and ethanol (3 mL) was stirred for 20 h before being concentrated in vacuo. The residue was dissolved in methanol (2 mL) and loaded onto a 10 g SCX cartridge. The impurities were washed through with methanol (50 mL) and discarded. The product was eluted with 1N methanolic ammonia (50 mL) and evaporated in vacuo to afford the title product (63 mg) as a white solid.

Provenance & Evidence