| abstract |
Described are radiolabeled epidermal growth factor receptor tyrosine kinase irreversible inhibitors of formula (I) wherein: Q1 is X-Y(=O)-Z and Q2 is H, halogen, alkoxy, hydroxyl, thiohydroxy, thioalkoxy, alkylamino and amino, or; Q2 is X-Y(=O)-Z and Q1 is H, halogen, alkoxy, hydroxyl, thiohydroxy, thioalkoxy, alkylamino and amino; X is selected from -NR1-, -O-, -NH-NR1-, -O-NR1-, -NH-CHR1-, -CHR1-NH-, -CHR1-O-, -O-CHR1-, -CHR1-CH2- and -CHR1-S-, or absent; Y is a radioactive or non-radioactive C; Z is -R2C=CHR3-, -Ca"C=R3, or -R2C=C=CHR3; Ra is hydrogen, or alkyl; A, B, C and D are independently H, a non-radioactive derivatising group or radioactive Br, I or F; Provided the compound comprises at least one radioactive atom. Further described is: a method of synthesizing a radiolabeled compound of formula (I); a pharmaceutical composition with as active ingredient a radiolabeled compound and a pharmaceutical carrier, for use in a medicinal radioimaging method for monitoring the level of epidermal growth factor receptor within the body of a patient, and as radiopharmaceuticals for radiotherapy. |