Citation:
LIU Chunyan, JIANG Shende. Synthesis of Precursors for O-(2-[18F]fluoroethyl)-L-tyrosine Used in Positron Emission Tomography[J]. Chinese Journal of Applied Chemistry,
;2011, 28(8): 892-896.
doi:
10.3724/SP.J.1095.2011.00686
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Five precursors,N-(tert-butoxycarbonyl)-O-(2-mosyloxyethyl/nosyloxyethyl)-L-tyrosine methyl ester(9a,11a) and N-(tert-butoxycarbonyl)-O-(2-mosyloxyethyl/tosyloxyethyl/nosyloxyethyl)-L-tyrosine tert-butyl ester(9b,10b,11b),were designed and synthesized for O-(2-[18F]fluoroethyl)-L-tyrosine([18F]FET) used in positron emission tomography(PET) for tumor imaging.These compounds were prepared by the esterification of methanol or transesterification of tert-butyl acetate with L-tyrosine,protection of the amine group with di-tert-butyl dicarbonate,and then nucleophilic substitution with glycol sulfonate in three steps with overall yields varied from 30% to 67%.
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