Process for the preparation of...

Details Process for the preparation of... Process for the preparation of...

2005-03-08

2005-03-08

Wilson, James O. (Department: 1623)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

C536S028530, C536S028400

Reexamination Certificate

active

06864366

ABSTRACT:
Process of preparing (E)-5-(2-bromovynyl)-2′-deoxyuridine (Brivudine) characterized in that halogen-free solvent selected form esters or cyclic ethers are used in the bromination step of 5-ethyl-2′-deoxyuridine diacylate. The use of solvents is advantageous in respect of toxicity, discharge costs and environment protection.

REFERENCES:
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patent: 2 125 399 (1984-03-01), None
Wyatt P.G. et al.: “A Short High Yielding Synthesis of the Potent ANIT-VZV Carbocyclic Nucleoside Analogue Carba-BVDU”, Nucleosides & Nucleotides, vol. 14, 1995, pp. 2039-2049, XP002203038, the whole document; in particular: p. 2042, second paragraph.
Westwood, N.B. et al.: “Synthesis and Biological Properties of a New Series of 5-Substituted-Pyrimidine-1-Nucleoside Analogues” Thetrahedron, vol. 54, 1998, pp. 13391-13404, XP002203039, the whole document, in particular p. 13395, scheme 3, step (c).
Ashwell M et al.: “The Synthesis and Antiviral Properties of (E)-5-(2-Bromovinyl)-2′-Deoxyuridine-Related Compounds” Terahedron, vol. 43, no. 20, 1987, pp. 4601-4608, XP002203040, the whole document.

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