反应详情

Analogously to general procedure (I) N-(3,3-dimethyl-6-nitro-2-oxo-2,3-dihydro-1H-indol-5-yl)-acetamide (0.3 g; 1.14 mmol) is alkylated using 2-bromomethyl-5-fluoro-pyridine (0.22 g; 0.46 mmol) and K2CO3 (0.4 g; 0.23 mmol) at 35° C. for 18 h. After aqueous work-up and purification by RP chromatography the pure material (87 mg) is de-acetylated in MeOH (6 ml) using DBU (16 μl) at reflux. After aqueous work-up 5-amino-1-(5-fluoro-pyridin-2-ylmethyl)-3,3-dimethyl-6-nitro-1,3-dihydro-indol-2-one (75.0 mg) is obtained and used without further purification.

1. customat 35° C.
2. customfor 18 h
3. customAfter aqueous work-up and purification by RP chromatography the pure material (87 mg)
4. temperatureat reflux