Morpholine → 4-(4-Methoxybenzyloxy)-7-morpholin-4-ylquinazoline

Participants

Reaction Steps

Under a nitrogen atmosphere, 2.82 g (12.5 mmol) of tris(dibenzylideneacetone)dipalladium-(0) and 5.41 g (15.1 mmol) of 2-(dicyclohexylphosphino)biphenyl were dissolved in 1.5 l of toluene, and 269.0 ml (3.1 mol) of morpholine and 213.0 g (0.62 mol) of 7-bromo-4-(4-methoxybenzyloxy)quinazoline [dissolved in 2 l of toluene] were added successively. 73.0 g (0.8 mol) of sodium tert-butoxide were subsequently added in portions, and the mixture was stirred. Conventional work-up gave 178 g of 4-(4-methoxybenzyloxy)-7-morpholin-4-ylquinazoline; HPLC/MS (M+H)+=350 as oil [crude product; was reacted further directly].

Provenance & Evidence