Boron tribromide → HCID 86600870, compound

Participants

Reaction Conditions

Reaction Steps

59.7 mg (0.128 mmol) of (rac.) 5-{[6-fluoro-2-hydroxy-5-methoxy-4,4,7-trimethyl-2-(trifluoromethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]amino}-isoquinolin-1-(2H)-one is mixed at 0° C. with 1.3 ml of a 1 molar solution of boron tribromide in dichloromethane, and it is stirred for one hour at 0 to 5° C. At −10° C., saturated sodium bicarbonate solution is now carefully added in drops. After 10 minutes of vigorous stirring at room temperature, the batch is extracted three times with methyl-tert-butyl ether. The organic phases are dried, and the residue is chromatographed on a Flashmaster after the solvent is spun off. 46.5 mg (80.3%) of the desired compound is isolated.

Provenance & Evidence