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US 5,399,682 AGranted
Process for preparing 2,3'-O-cyclocytidine
AssigneeACIC (Canada) Inc.
InventorsKhashayar Karimian, Bruno K. Radatus
Life of this patent
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Abstract
A process for preparing 2,3'-O-cyclocytidine wherein 3'-deoxy-3'-organosulfonyl cytidine is refluxed in the absence of base. 2,3'-cyclocytidine is an intermediate in the preparation of 1-(B-D-xylo-pentofuranose) cytosine, an inhibitor of DNA synthesis.
Claims10
A process for producing a compound of Formula IV:
- ##STR22## which comprises the step of refluxing in a polar solvent in the absence of base a compound of Formula II:
- ##STR23## wherein R.sup.6 is selected from the group comprising a trifluoromethyl group, a C.sub.1 -C.sub.6 alkyl group and a C.sub.6 -C.sub.9 aryl group, and R.sup.1 is selected from the group comprising hydrogen, trityl, methoxytrityl, dimethoxytrityl, acetyl, a C.sub.2 -C.sub.6 alkylacyl group, a C.sub.6 -C.sub.9 arylacyl group, allyl, 2,2,2-trichloroethyl, phosphates and salts thereof, tosyl and mesyl, resulting in intramolecular cyclization thereof to produce a compound of Formula IV.
A process for producing a compound of Formula V:
- ##STR24## which comprises the step of refluxing in a polar solvent in the absence of base a compound of Formula VI:
- ##STR25## wherein Ts is a tosyl group, resulting in intramolecular cyclization thereof, followed by reaction with hydrogen chloride, to produce the compound of Formula V.
Dependencies are inferred from the claim text.