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

被引：6

作者：

Liu ChunYan ^{[1
,2
]}

Jiang ShenDe ^{[1
]}

机构：

[1] Tianjin Univ, Sch Pharmaceut Sci & Technol, Tianjin 300072, Peoples R China

[2] N China Coal Med Coll, Dept Pharm, Tangshan 063000, Peoples R China

来源：

SCIENCE IN CHINA SERIES B-CHEMISTRY | 2009年 / 52卷 / 12期

关键词：

positron emission tomography; triflate; L-tyrosine; 18F]FET precursor; PET imaging; F-18-LABELED AMINO-ACID; MAGNETIC-RESONANCE; TUMOR; TRACER; CANCER;

D O I：

10.1007/s11426-009-0195-8

中图分类号：

O6 [化学];

学科分类号：

0703 ;

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.

引用

页码：2195 / 2199

页数：5

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