3.8 Article

Preparation of two triflate precursors for O-(2-[18F] fluoroethyl)-L-tyrosine used in positron emission tomography (PET)

期刊

SCIENCE IN CHINA SERIES B-CHEMISTRY
卷 52, 期 12, 页码 2195-2199

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SCIENCE PRESS
DOI: 10.1007/s11426-009-0195-8

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positron emission tomography; triflate; L-tyrosine; [18F]FET precursor; PET imaging

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  1. Tianjin University

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Two novel triflate precursors for radiolabelling of L-tyrosine in positron emission tomography (PET) for tumor imaging, O-(2-trifluoromethanesulfonyloxyethyl)-N-(tert-butoxycarbonyl)-L-tyrosine methyl ester 9a and O-(2-trifluoromethanesulfonyloxyethyl)-N-(tert-butoxycarbonyl)-L-tyrosine tert-butyl ester 9b, are synthesized. The triflate agent, 9a or 9b, is prepared by esterification of methanol or transesterification of tert-butyl acetate with L-tyrosine, protection of the amine group with di-tert-butyl dicarbonate, alkylation with chlorohydrin, and triflation with trifluoromethanesulfonic anhydride in four steps with overall yields of 30% and 15%, respectively.

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