@article{bbd417ffa75f4802880df1564b9ff310,
title = "Methodology for the synthesis and specific activity determination of 16α-[77Br]-Bromoestradiol-17 β and 16α-[77Br]-11 β-methoxyestradiol-17 β, Two estrogen receptor-binding radiopharmaceuticals",
abstract = "16α-[77Br]-Bromoestradiol-17β (3a) has been synthesized from estrone enol diacetate (1) by bromination with Na 77Br and hydrogen peroxide-acetic acid, followed by reduction with lithium aluminum hydride to give a mixture of 16α-[77Br]-bromoestradiol-17β (3a) and 16α-[77Br]-bromoestradiol-17α (3a) from which the desired epimer (3a) can be obtained in 50% overall radiochemical yield (from Na77Br) by HPLC. Analogous procedures can be used in the preparation of 16α-[77Br]-bromo-11β-methoxyestradiol-17β. (4a) The effective specific activities of these radiopharmaceuticals, determined by binding to the uterine estrogen receptor, are 900-1500 Ci/mmol. Both have high affinity and good binding selectivity for the estrogen receptor and are useful as imaging agents for mammary tumors.",
author = "Senderoff, {Stephen G.} and McElvany, {Karen D.} and Carlson, {Kathyrn E.} and Heiman, {Daniel F.} and Katzenellenbogen, {John A.} and Welch, {Michael J.}",
note = "Funding Information: Acknowledgemenrs-Support of this research was obtained from grants from the National Institutes of Health (HHS 5ROl CA 25836 to J. A. K.). the Department of Energy (DE-AC02-81EV10650 to M. J. W.). and the National Science Foundation (NSF CHE 79-16100. University of Illinois NSF Regional Instrumentation Facility). We are very grateful to Dr J. S. BARAN (Searle Laboratories) for a gift of SC 16093. The assistance of S. W. LANDVATTER in the preparation of l6%-[“Br]-bromo-I l/I-methoxyestradiol-I 78 is gratefully acknowledged. We extend our appreciation to Drs J. W. BARNES,G . E. BENTLEY, P. M. GRANT and H. A. O{\textquoteright}BKIEN, Jr of Los Alamos National Laboratory for their assistance in providing spallation-produced bromine-77 for use in these experiments.",
year = "1982",
month = jul,
doi = "10.1016/0020-708X(82)90010-2",
language = "English (US)",
volume = "33",
pages = "545--551",
journal = "Applied Radiation and Isotopes",
issn = "0969-8043",
publisher = "Elsevier Limited",
number = "7",
}