反应详情

In an analogous manner to Example 10, 5-(4-(4-Benzyloxy-phenylamino)-quinazolin-6-yl)-furan-2-carbaldehyde hydrochloride (0.200 g, 0.436 mmol) was reacted with 2-aminoethylsulphonamide hydrochloride (0.200 g, 1.245 mmol) and triethylamine (10 drops). On completion of the reaction, the mixture was acidified with dilute HCl and diluted with water, to give the crude product as a precipitate collected by filtration. Treatment with triethylamine followed by purification by silica gel chromatography, eluting with 3-10% MeOH/CHCl3 gave the title compound as a yellow solid (0.085 g, 0.160 mmol, 37%); δH [2H6]DMSO 9.61 (2H, brs), 9.25 (1H, s), 8.58 (1H, s), 8.23 (1H, d), 7.77-7.88 (3H, m), 7.30-7.52 (5H, m), 7.26 (2H, s), 7.20 (1H, d), 7.08 (2H, d), 6.81 (1H, d), 5.14 (2H, s), 4.44 (2H, s), 3.34-3.60 (2H, m), 3.25-3.45 (2H,obscured by water); m/z (M+1+) 530.

1. customOn completion of the reaction
2. customto give the crude product as a precipitate
3. filtrationcollected by filtration
4. customTreatment with triethylamine followed by purification by silica gel chromatography
5. washeluting with 3-10% MeOH/CHCl3