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Synthesis of Some Nitrosourea Analogues of 5-Aminomethyl-2'-Deoxyuridine Author: George Tsu-rong Shiau(Department of Chemistry College of Sciences )

Abstract：

This paper reports the synthesis of some nitrosourea analogues of 5-amino-methyl-2'-deoxyuridine as potential anticancer agents.
Nitrosourea derivatives sudh as BCNU and CCNU have been in clinical trials for many years. However, many studies to modify nitrosourea agents have been undergoing mainly due to their side effects.
Newly synthesized 3'-nitrosourea analogues of thymidine have shown greater inhibitory activity against some cancer cells than BCNU. On the other hand, 5-aminomethyl-2'-doxyuridine is more soluble in water than 3-nitrosourea thymidine analogues. These facts, thus, prompted the preparation of the title compounds from commercially available thymidine through 5-aminomethy1-2'-deoxyuridine intermediate and then to the nitrosourea analogues, in hope, to imporve the therapeutic index of nitrosourea agents. The total yield from thymidine through 6 steps of reaction is about 4%. The study on the structure of nitrosourea analogues by NMR is also reported.

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