反应详情

The procedure used in stage 1 of Example 1 is followed, but starting from 2.69 g of 4-fluoro-5-(4-methylpiperazin-1-yl)benzene-1,2-diamine, which can be prepared according to J. Het. Chem. 2005, 42(1), 67-71, 2.82 ml of triethylamine and 2.43 g of 9H-fluoren-9-one-4-carboxylic acid chloride in 50 ml of dichloromethane for 20 hours at room temperature. After purification by flash chromatography on silica gel (40-63 μm), eluting with a mixture of dichloromethane and methanol (95/5 by volume), and then formation of a paste with diisopropyl ether, in this way we obtain 1 g of [2-amino-4-fluoro -5-(4-methyl piperazin-1-yl)phenyl]amide of 9-oxo-9H-fluorene-4-carboxylic acid, in the form of an orange powder, which is used as it is in the following stage, with the following characteristics:

1. customcan be prepared
2. customAfter purification by flash chromatography on silica gel (40-63 μm)
3. washeluting with a mixture of dichloromethane and methanol (95/5 by volume)