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Title: Synthesis of 4-(3'-[125I]iodoanilino)-6,7-dialkoxyquinazolines:radiolabeled epidermal growth factor receptor tyrosine kinaseinhibitors

Journal Article · · Journal of Labelled Compounds andRadiopharmaceuticals
OSTI ID:894401

The preparation of two radioiodinated analogs of theepidermal growth factor receptor tyrosine kinase (EGFrTK) inhibitorPD153035(4-(3'-bromoanilino)-6,7-dimethoxyquinazoline) are reportedherein. The two analogs,4-(3'-[125I]iodoanilino)-6,7-dimethoxyquinazoline and4-(3'-[125I]iodoanilino)-6,7-diethoxyquinazoline, were synthesizedviaiododestannylation of the corresponding4-(3'-trimethylstannylanilino)-6,7-dialkoxyquinazolines to form thedesired I-125 labeled products in good yield and high radiochemicalpurity (>99 percent).

Research Organization:
Lawrence Berkeley National Lab. (LBNL), Berkeley, CA (United States)
Sponsoring Organization:
USDOE; US Department of Defense DAMD17-98-1-8064
DOE Contract Number:
DE-AC02-05CH11231; OTHER:US DOD:DAMD17-98-1-8064
OSTI ID:
894401
Report Number(s):
LBNL-44443; m; R&D Project: 802F01
Journal Information:
Journal of Labelled Compounds andRadiopharmaceuticals, Vol. 43, Issue 12; Related Information: Journal Publication Date: 10/30/2000
Country of Publication:
United States
Language:
English