Phosphorus tribromide → 4-[4-(2-Bromoethyl)piperidin-1-yl]-6,7-dimethoxyquinazoline

Participants

Reaction Steps

Phosphorus tribromide (9.7 g) was added at room temperature to a stirred solution of 1-(6,7-dimethoxyquinazolin-4-yl)-4-(2-hydroxyethyl)piperidine (7.5 g) in ethanol free chloroform (200 cm3) and triethylamine (5.0 cm3). After stirring for 16 hours the volatile material was removed in vacuo and the residue was taken into aqueous sodium carbonate solution and extracted with chloroform (3×50 cm3). The dried (MgSO4) extracts were evaporated and the residue was chromatographed on "Florisil" (Trade Mark, Hopkin and Williams) eluting with chloroform to afford 1-(6,7-dimethoxyquinazoline-4-yl)-4-(2-bromoethyl) piperidine 1/4 H2O as a white solid, m.p. 191° (5.6 g).

Provenance & Evidence