Markable compounds for easy synthesis of 3'-[ 18 F]...

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

Reexamination Certificate

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C536S028400, C536S028500

Reexamination Certificate

active

07145000

ABSTRACT:
What is described are compoundswherein R represents Br, I or R1—SO3, where R1is an unsubstituted or substituted C1–C5-alkyl group, or an unsubstituted or substituted phenyl group;X is O or NR″, where R″ is a usual protective group for N; andR′ represents hydrogen, a halogen, such as F, Cl, and Br, a substituted or unsubstituted C1–C7-alkyl group, such as methyl and ethyl, a substituted or unsubstituted C2–C7-alkenyl group, or a substituted or unsubstituted C2–C7-alkynyl group.

REFERENCES:
Minamoto et al., “Synthesis and Alkali-Hydrolysis Reactions of some 2,3′-(Substituted imino)pyrimidine Nucleosides Lacking a 2′-Hydroxyl Group”, J. Org. Chem., vol. 54, pp. 4543-4549, 1989.
Doerr et al., “The Introduction of a 2,3′-Imino Bridge into Pyrimidine Nucleosides”, Journal of the American Chemical Society, 89;7, pp. 1760-61, 1967.
Doerr et al., “Synthesis of 2,3′-Imino-1-(2-deoxy-β-D-threo-pentofuranosyl)thymine and related derivatives”, Journal of Organic Chemistry, vol. 33, No. 4, pp. 1592-1599, 1968.
Minamoti et al., “Synthesis and Alkali-Hydrolysis Reactions of Some 2,3′-(Substituted imino) pyrimidine Nucleosides Lacking a 2′-Hydroxyl Group,” Journal of Organic Chemistry, vol. 54, No. 19, pp. 4543-4549, 1989.
Grierson et al., “Radiosynthsis of 3′-Deoxy-3′-[18F]fluorothymidine: [18F]FLT for Imaging of Cellular Proliferation In Vivo,” Nuclear Medicine & Biology, vol. 27, pp. 143-156, 2000.
Machulla et al., “Simplified labeling approach for synthesizing 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT),” Journal of Radioanalytical and Nuclear Chemistry, Fol. 243, No. 3, pp. 843-846, 2000.
Wodarski et al., “Synthesis of 3′-Deoxy-3′-[18F]Fluoro-Thymidine with 2,3′-Anhydro-5′-0-(4,4′-Dimethoxytrityl)-Thymidine,” Journal of Labelled Compounds and Radiopharmaceuticals, vol. 43, pp. 1211-1218, 2000.

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