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

Authors
Lim, JK Negash, K Hanrahan, SM VanBrocklin, HF
Citation
Jk. Lim et al., Synthesis of 4-(3 '-[I-125]iodoanilino)-6,7-dialkoxyquinazolines: Radiolabeled epidermal growth factor receptor tyrosine kinase inhibitors, J LABEL C R, 43(12), 2000, pp. 1183-1191
Citations number
24
Categorie Soggetti
Chemistry & Analysis","Inorganic & Nuclear Chemistry
Journal title
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
ISSN journal
03624803 → ACNP
Volume
43
Issue
12
Year of publication
2000
Pages
1183 - 1191
Database
ISI
SICI code
0362-4803(20001030)43:12<1183:SO4'R>2.0.ZU;2-4
Abstract
The preparation of two radioiodinated analogs of the epidermal growth facto r receptor tyrosine kinase (EGFrTK) inhibitor PD153035 (4-(3'-bromoanilino) -6,7-dimethoxyquinazoline) are reported herein. The two analogs, 4-(3'-[I-1 25]iodoanilino)-6,7-dimethoxyquinazoline and 4-(3'-[I-125]iodoanilino)-6,7- diethoxyquinazoline, were synthesized via iododestannylation of the corresp onding 4-(3'-trimethylstannylanilino)-6,7-dialkoxyquinazolines to form the desired I-125 labeled products in good yield, high radiochemical purity (>9 9%) and high specific activity.