Water → 7-Bromo-4-(4-(difluoromethyl)-5-fluoro-2-methoxyphenyl)quinazoline

Participants

Reaction Steps

A solution of PdCl2(dppf)-CH2Cl2 adduct (0.101 g, 0.123 mmol), 2-(4-(difluoromethyl)-5-fluoro-2-methoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (Intermediate SSSSS; 1.365 g, 4.52 mmol), 7-bromo-4-chloroquinazoline (Synnovator, 1.000 g, 4.11 mmol), and potassium carbonate (2.270 g, 16.43 mmol) in 12 mL dioxane was treated with 4 mL water and was allowed to stir at room temperature overnight. LC/MS showed mostly product, so the reaction mixture was diluted with DCM and filtered through a plug of Celite. The aqueous layer was removed and the organics concentrated. The crude residue was carried on to step 2 without purification. (M+H)+=384.9.

Provenance & Evidence