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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 shu

Synthesis of Precursors for O-(2-[¹⁸F]fluoroethyl)-L-tyrosine Used in Positron Emission Tomography

LIU Chunyan ^a,b ,
JIANG Shende ^a,,

1.
a School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072;
2.
b Department of Pharmacy, Hebei United University, Tangshan 063000

Corresponding author: JIANG Shende,
Received Date: 18 November 2010
Available Online: 25 December 2010

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%.
- positron emission tomography,
- L-tyrosine,
- O-(2-[¹⁸ F]fluoroethyl)-L-tyrosine precursor,
- positron emission tomography imaging
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Synthesis of Precursors for O-(2-[¹⁸F]fluoroethyl)-L-tyrosine Used in Positron Emission Tomography