SELECTIVE ALKYLATION OF PYRIMIDYL DIANIONS .3. NO-CARRIER-ADDED SYNTHESIS OF [C-11-METHYL]-THYMIDINE

被引：10

作者：

ALAUDDIN, MM

RAVERT, HT

MUSACHIO, JL

MATHEWS, WB

DANNALS, RF

CONTI, PS

机构：

[1] UNIV SO CALIF, SCH MED, CTR PET IMAGING SCI, DEPT RADIOL, LOS ANGELES, CA 90033 USA

[2] JOHNS HOPKINS MED INST, DIV NUCL MED & RADIAT HLTH SCI, BALTIMORE, MD 21205 USA

来源：

NUCLEAR MEDICINE AND BIOLOGY | 1995年 / 22卷 / 06期

关键词：

D O I：

10.1016/0969-8051(95)00027-U

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

A no-carrier-added, high specific activity synthesis of [C-11-methyl]-thymidine is reported. Reaction of 3', 5'-O-bis-(tetrahydropyranyl)-5-bromo-2'-deoxyuridine with n-butyllithium produced a dianion which was alkylated with [C-11]-methyl iodide, and on subsequent hydrolysis, yielded [C-11-methyl]-thymidine. The labeled compound was isolated from the by-product 2'-deoxyuridine by HPLC on a reverse phase C-18 semipreparative column with mean radiochemical yield of 18.8% (decay corrected) in 30-35 min and radiochemical purity >99%. This no-carrier-added synthesis can be used to produce [C-11-methyl]-thymidine with mean specific activity over 1000 mCi/mu mol for positron emission tomography (PET) studies.

引用

页码：791 / 794

页数：4

共 23 条

[1] SELECTIVE ALKYLATION OF PYRIMIDYL DIANIONS .2. SYNTHESIS, CHARACTERIZATION, AND COMPARATIVE REACTIVITY OF 3',5'-O-BIS-TETRAHYDROPYRANYL, TRIMETHYLSILYL AND TERT-BUTYLDIMETHYLSILYL DERIVATIVES OF 5-BROMO-2'-DEOXYURIDINE [J].