反应详情

温度

85 °C

A suspension of 4-(6-methoxy-4-thiazol-2-yl-phthalazin-1-yl)-butyric acid methyl ester (1.2 g, 3.5 mmoles), prepared as described in example 115, in NH3/THF (10 ml) was added with THF (15 ml), then placed in autoclave at 85° C. After 1 night the mixture was dried, taken up in CH3OH (30 ml) and saturated with NH3 at 0° C., then heated at 85° C. for 44 hours. The mixture was cooled and dried to give a residue which was chromatographed (eluent: CH2Cl2/CH3OH 95:5 to 90:10). The solid was triturated in CH2Cl2 to give 840 mg of the title compound (yield: 73.1%)

1. customprepared
2. customplaced in autoclave at 85° C
3. customAfter 1 night the mixture was dried
4. customtaken up in CH3OH (30 ml) and saturated with NH3 at 0° C.
5. temperatureThe mixture was cooled
6. customdried
7. customto give a residue which
8. customwas chromatographed (eluent: CH2Cl2/CH3OH 95:5 to 90:10)
9. customThe solid was triturated in CH2Cl2