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Synthesis of 4‐(3′‐[ 125 I]iodoanilino)‐6,7‐dialkoxyquinazolines: radiolabeled epidermal growth factor receptor tyrosine kinase inhibitors
Author(s) -
Lim John K.,
Negash Kitaw,
Hanrahan Stephen M.,
VanBrocklin Henry F.
Publication year - 2000
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/1099-1344(20001030)43:12<1183::aid-jlcr405>3.0.co;2-n
Subject(s) - chemistry , tyrosine kinase , yield (engineering) , epidermal growth factor receptor , tyrosine , platelet derived growth factor receptor , receptor tyrosine kinase , tyrosine kinase inhibitor , epidermal growth factor , kinase , receptor , stereochemistry , biochemistry , growth factor , medicine , cancer , materials science , metallurgy
The preparation of two radioiodinated analogs of the epidermal growth factor receptor tyrosine kinase (EGFrTK) inhibitor PD153035 (4‐(3′‐bromoanilino)‐6,7‐dimethoxyquinazoline) are reported herein. The two analogs. 4‐(3′‐[ 125 I]iodoanilino)‐6,7‐dimethoxyquinazoline and 4‐(3′‐[ 125 I]iodoanilino)‐6,7‐diethoxyquinazoline, were synthesized via iododestannylation of the corresponding 4‐(3′‐trimethylstannylanilino)‐6,7‐dialkoxyquinazolines to form the desired I‐125 labeled products in good yield, high radiochemical purity (>99%) and high specific activity. Copyright © 2000 John Wiley & Sons, Ltd.