Synthesis of 4-(3'-[125I]iodoanilino)-6,7-dialkoxyquinazolines: Radiolabeled epidermal growth factor receptor tyrosine kinase inhibitors

被引：0
|
作者：
Lim, John K. [1 ,2 ]
Negash, Kitaw [1 ,3 ]
Hanrahan, Stephen M. [1 ]
Vanbrocklin, Henry F. [1 ]
机构：
[1] Lawrence Berkeley National Laboratory, University of California, MS 55-121, 1 Cyclotron Rd., Berkeley, CA 94720, United States
[2] Department of Radiology, University of California, San Francisco, CA 94143, United States
[3] American Cyanamide Co., Agricultural Research Division, Princeton, NJ 08543, United States
来源：
Journal of Labelled Compounds and Radiopharmaceuticals | 2000年 / 43卷 / 12期
关键词：
Amino acids - Enzyme inhibition;
D O I：
10.1002/1099-1344(20001030)43:123.0.CO;2-N
中图分类号：
学科分类号：
摘要：
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'-[125I]iodoanilino)-6,7-dimethoxyquinazoline and 4-(3'-[125I]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.
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页码：1183 / 1191
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