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

作　　者：LIU ChunYan1,2 & JIANG ShenDe1 1 School of Pharmaceutical Science and Technology,Tianjin University,Tianjin 300072,China 2 Department of Pharmacy,North China Coal Medical College,Tangshan 063000,China 

出　　处：《Science China Chemistry》2009年第12期2195-2199,共5页中国科学（化学英文版）

基　　金：Supported by Tianjin University

摘　　要：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.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.

关 键 词：POSITRON emission tomography TRIFLATE L-TYROSINE [18F]FET PRECURSOR PET imaging 

分 类 号：O623.6[理学—有机化学]