反应详情

(1-Benzyl-1H-indazol-5-yl)-(6-iodoquinazolin-4-yl)-amine (3.58 g) in dioxane (30 ml) under N2 was treated with tributyltin cyanide (2.51 g) and catalytic quantities of 1.4-bis-(diphenylphosphino)-butane palladium (II) chloride and tetrakis (triphenylphosphine) palladium at reflux for 5 days. The mixture was absorbed onto silica and chromatographed to give the title compound (1.25 g); δH [2H6]DMSO 10.20(1H, s), 9.15(1H, s), 8.65(1H, s), 8.24(1H, s), 8.18(2H, m), 7.89(1H, s), 7.70(2H, m), 7.30(5H, m), 5.70(2H, s); m/z (M+1)+ 377.

1. temperatureat reflux for 5 days
2. customThe mixture was absorbed onto silica
3. customchromatographed