反应详情

N-(5-{7-Methoxy-6-[3-(4-methyl-piperazin-1-yl)-propoxy]-quinazolin-4-ylamino}-benzothiazol-2-yl)-benzamide was prepared by heating a mixture of N-(5-aminobenzothiazol-2-yl)benzamide (IM 5, 35 mg, 0.13 mmol), 4-chloro-7-methoxy-6-[3-(4-methylpiperazin-1-yl)propoxy]quinazoline (IM 8, 46 mg, 0.13 mmol) and 4 M HCl in dioxane (0.09 mL, 0.39 mmol) in n-butanol (3 mL) to 110° C. for 5 h. The HCl salt of the product precipitated. It was separated by filtration and washed twice with CH2Cl2. No ether purification was necessary (65 mg, 0.1 mmol, 93%). LC:/ESI-MS: m/z=620 [M+H]+; m/z=618 [M−H]−; Rt=2.43 min.

1. temperatureby heating
2. customThe HCl salt of the product precipitated
3. customIt was separated by filtration
4. washwashed twice with CH2Cl2
5. customNo ether purification