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

Autor:	Luc Lambotte, T. Vander Borght, Stanislas Pauwels, Christian Beckers, C. De Saeger
Rok vydání:	1990
Předmět:	Pyrimidine Organic Chemistry Sulfuric acid Biochemistry Analytical Chemistry Thymine chemistry.chemical_compound chemistry Deoxyribose Yield (chemistry) Drug Discovery Urea Radiology Nuclear Medicine and imaging Carbon-14 Thymidine Spectroscopy Nuclear chemistry
Zdroj:	Journal of Labelled Compounds and Radiopharmaceuticals. 28:819-822
ISSN:	0362-4803
DOI:	10.1002/jlcr.2580280711
Popis:	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%.
Databáze:	OpenAIRE
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