Journal of fluorine chemistry

3, 3-Difluorochlorambucil

CW Buss, PL Coe, JC Tatlow

Index: Buss,C.W.; Coe,P.L.; Tatlow,J.C. Journal of Fluorine Chemistry, 1986 , vol. 34, p. 83

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Citation Number: 7

Abstract

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 ...

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