Boron tribromide → HCID 24781011, compound

Participants

Reaction Conditions

Reaction Steps

111.2 mg (0.231 mmol) of (rac.) 6-fluoro-1-[(8-fluoro-2-methylquinazolin-5-yl)-amino]-5-methoxy-4,4,7-trimethyl-2-(trifluoromethyl)-1,2,3,4-tetrahydronaphthalen-2-ol is mixed at 0° C. with 3.2 ml of a 1 molar solution of boron tribromide in dichloromethane, and it is stirred for one and one-half hours at 0 to 5° C. At 0° C., the now carefully saturated sodium bicarbonate solution is added in drops. After 10 minutes of vigorous stirring at room temperature, the batch is extracted three times with ethyl acetate. The organic phases are dried, and the residue is chromatographed on a Flashmaster after the solvent is spun off. 66.4 mg (61.5%) of the desired compound is isolated.

Provenance & Evidence