Labelled derivatives of digoxin and digitoxin

Details Labelled derivatives of digoxin and digitoxin Labelled derivatives of digoxin and digitoxin

C - Chemistry, Metallurgy

07

J

150/11, 260/8

C07J 19/00 (2006.01) C07J 41/00 (2006.01)

Patent

CA 1070670

ABSTRACT Radio-iodine derivatives of tyrosine-Me-ester conjugates of digoxin and digitoxin are provided having the formula Image V wherein one or two groups Z are = NO(CHR)n.CO.R1, any remaining group Z being = O; X is -OH or -H R is H or C1 to C4 alkyl; n is 1, 2, or 3; R1 is either -OH or -NH.CHY.(CH2)m Q; Y is -H or -COOR2; m is 0, 1, 2, 3, 4 or 5; R2 is H, CH3 or C2H5; Q is unlabelled or labelled and has one of the following structural formulae:- Image or Image or Image and the symbol * indicates the probable positions at which the compound may be labelled with one or more radioactive iodine atoms. Novel intermediates in the preparation of the radio-iodine derivative are described. The derivatives are useful for the radioimmuno- assay of digoxin and digitoxin.

229511

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