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 (4 g) is alkylated using (2-iodo-ethyl)-cyclopropane (5.36 g; 27.3 mmol) and K2CO3 (6.30 g; 45.6 mmol) at 55° C. for 12 h. After aqueous work-up the crude material (4.21 g) is de-acetylated in hydrochloric acid (6 N, 30 ml) at reflux. After aqueous work-up 5-amino-1-(2-cyclopropyl-ethyl)-3,3-dimethyl-6-nitro-1,3-dihydro-indol-2-one (3.75 g) is obtained and used without further purification.

1. customat 55° C.
2. customfor 12 h
3. temperatureat reflux