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With N-ethyl-N,N-diisopropylamine; In isopropyl alcohol; at 90℃; for 2h;
6.7-dimethoxy-4-(3-phenylpiperidin-1-yQquinazoline: 4-chloro-6,7- dimethoxyquinazoline (15 g, 66.8 mmol) was mixed with 3-phenylpiperidine (11.8 g, 73.5 mmol) in isopropanol (300 ml_), then diisopropylethylamine (23 ml_, 133.6 mmol) was added and the mixture was heated at 900C for 2 h. After cooling to room temperature, the solvent was removed in vacuo, the residue was diluted with water and chloroform, and the mixture was made basic by adding sodium hydroxide (pH <12). The mixture was extracted with chloroform, the organic layer was washed with brine and was dried over MgSO4, was filtered, and was concentrated in vacuo. Purification by silica gel chromatography (100% chloroform to 100-1-1 chloroform/methanol/aqu. cone, ammonium hydroxide) afforded 17.5 g (75% yield) of the title compound; MS (AP/CI): 350.2 (M+H)+.
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