Synthesis of [2‐14C]thymidine: A potential route for [2‐11C]thymidine
- 1 July 1990
- journal article
- research article
- Published by Wiley in Journal of Labelled Compounds and Radiopharmaceuticals
- Vol. 28 (7) , 819-822
- https://doi.org/10.1002/jlcr.2580280711
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% SO3). Thymidine was further synthesized by the enzymatic transfer of deoxyribose onto thymine with a 90% yield achieved within 10 min. Using [14C]urea as precursor, the present method allowed the synthesis of radiochemically pure [2‐14C]thymidine in 35 min with a cumulative yield of 40%.Keywords
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