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Synthesis of [2-14C]thymidine: A potential route for [2-11C]thymidine

✍ Scribed by T. Vander Borght; Dr. S. Pauwels; L. Lambotte; C. De Saeger; C. Beckers

Publisher: John Wiley and Sons
Year: 1990
Tongue: French
Weight: 201 KB
Volume: 28
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580280711

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✦ Synopsis

Abstract

We report a three‐step synthesis of thymidine, starting from trace amounts of urea, that allows rapid introduction of radioactivity in C2‐position of the pyrimidine ring. Thymine was produced within 5 min with a 60% yield by cyclocondensation of urea and diethyl β‐methylmalate in fuming sulfuric acid (15% SO~3~). Thymidine was further synthesized by the enzymatic transfer of deoxyribose onto thymine with a 90% yield achieved within 10 min. Using [^14^C]urea as precursor, the present method allowed the synthesis of radiochemically pure [2‐^14^C]thymidine in 35 min with a cumulative yield of 40%.

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