Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives
Patent
1995-04-10
1996-12-31
Kunz, Gary L.
Organic compounds -- part of the class 532-570 series
Organic compounds
Carbohydrates or derivatives
536 2852, 536 275, 544242, C07H 100
Patent
active
055895875
ABSTRACT:
The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors. The novel process of the present invention utilizes a cytidine derivative as the required starting material and provides the ribonucleotide reductase inhibitor in a more efficient than the reaction sequence. The process is more efficient than the process disclosed by McCarthy et al. in European Patent Application Publication No. 0 372 268 published Jun. 13, 1990, in that it requires fewer chromatographies and results in an overall yield of greater than 25% for the five steps. The present invention further provides the ribonucleotide reductase inhibitor in a four step reaction sequence and results in an overall yield of greater than 35%.
REFERENCES:
patent: 5047520 (1991-09-01), Matsuda et al.
patent: 5378693 (1995-06-01), McCarthy et al.
McCarthy, et al., J of the American Chem Society 113(19):7439-7440 (1991).
Takenuki, et al., J Med Chem. 31:1064-1066 (1988).
McCarthy, et al., Tetrahedron Letters 31(38):5449-5452 (1990).
Sabol, et al., Tetrahedron Letters 33(22):3101-3104 (1992).
Matsuda, et al., Chem. Pharm. Bull. 36(3):945-953 (1988).
Markiewicz et al. Tetrahedron Letters, vol. 29, No. 13. pp. 1561-1564, (1988).
Donaldson Richard E.
Duquid Robert
Matthews Donald P.
McCarthy James R.
McConnell James R.
Kunz Gary L.
Lentz Nelsen L.
Merrell Pharmaceuticals Inc.
Wilson James O.
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