Morpholine → 2,4-Bis(4-methoxybenzyloxy)-7-morpholin-4-ylquinazoline

Participants

Reaction Conditions

Reaction Steps

Under a nitrogen atmosphere, 2.26 g (2.47 mmol) of tris(dibenzylideneacetone)dipalladium-(0) and 4.42 g (12.35 mmol) of 2-(dicyclohexylphosphino)biphenyl were dissolved in 1.5 l of toluene, and 215.2 ml (2.47 mol) of morpholine and 269.0 g (0.5 mol) of 7-bromo-2,4-bis(4-methoxybenzyloxy)quinazoline [dissolved in 5 l of toluene] were added successively. 66.47 g (0.7 mol) of sodium tert-butoxide were subsequently added in portions, and the mixture was stirred at 90° C. for 12 h. Conventional work-up gave 249.0 g of 2,4-bis(4-methoxybenzyloxy)-7-morpholin-4-ylquinazoline; HPLC/MS (M+H)+=488 as oil [crude product; was reacted further directly].

Provenance & Evidence