Synthesis of new carbon-11 labeled cyclofenil derivatives for PET imaging of breast cancer estrogen receptors.

作者信息

Gao Mingzhang, Wang Min, Mock Bruce H, Miller Kathy D, Sledge George W, Hutchins Gary D, Zheng Qi-Huang

机构信息

Department of Radiology, Indiana University School of Medicine, 1345 West 16th Street, L-3 Room 202, Indianapolis, IN 46202, USA.

出版信息

Appl Radiat Isot. 2008 Apr;66(4):523-9. doi: 10.1016/j.apradiso.2007.11.006. Epub 2007 Nov 19.

DOI:10.1016/j.apradiso.2007.11.006

PMID:18155914

Abstract

Carbon-11 labeled cyclofenil derivatives, [(11)C]methyl-2-{4-[bis(4-hydroxyphenyl)methylene]cyclohexyl}acetate ([(11)C]16a), [(11)C]methyl-4-[bis(4-hydroxyphenyl)methylene]cyclohexanecarboxylate ([(11)C]16b), [(11)C]methyl-2-{3-[bis(4-hydroxyphenyl)methylene]cyclohexyl}acetate ([(11)C]18a), and [(11)C]methyl-3-[bis(4-hydroxyphenyl)methylene]cyclohexanecarboxylate ([(11)C]18b), have been synthesized as new potential PET agents for imaging breast cancer estrogen receptors. The target tracers were prepared by O-[(11)C]methylation of their corresponding precursors using [(11)C]CH(3)OTf and isolated by a simplified SPE purification procedure in 35-50% radiochemical yields decay corrected to EOB, 15-20 min overall synthesis time, and 74-111 GBq/micromol specific activity at EOS.

摘要

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