Process for preparing 2-deoxynucleosides

Details Process for preparing 2-deoxynucleosides Process for preparing 2-deoxynucleosides

C - Chemistry, Metallurgy

07

H

260/229

C07H 19/04 (2006.01) C07H 19/06 (2006.01) C07H 19/12 (2006.01)

Patent

CA 1301166

Abstract of the Disclosure PROCESS FOR PREPARING 2-DEOXYNUCLEOSIDES An O-, S-, or N-silyl- or O-, S-, or N-alkyl- pyrimidine is reacted with a protected 1-halo-, 1-alkoxy-, or 1-acyloxy-2- deoxy sugar in the presence of cuprous iodide and a halohydrocarbon solvent to prepare a nucleo- side having an improved beta-anomer/alpha-anomer ratio. In a preferred embodiment of the invention, 2,4-bis(tri- methylsilyloxy)-5-methylpyrimidine or 2,4-bis(trimethyl- silyloxy)-5-ethylpyrimidine is reacted with 2-deoxy-3,5- di-O-p-toluyl-D-erythro-ribofuranosyl chloride in the presence of cuprous iodide and chloroform.

571792

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