Abstract A difluoro-derivative of the anti-cancer drug chlorambucil has been made in 7 stages from 4-nitrophenylacetic acid. The acid chloride and ethyl malonate/butyl lithium afforded ethyl 4-(4′-nitrophenyl)-3-oxobutanoate, of which the 3-oxo-function was converted to CF 2 by sulphur tetrafluoride/hydrogen fluoride at room temperature. The nitro- group was reduced to amino, which was alkylated to bis (hydroxy-ethyl) amino using ...
