3'-tosylcytidine compounds and process for production thereof

C - Chemistry – Metallurgy – 07 – H

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260/229.4

C07H 19/06 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2012095

Novel compounds of Formula I, or pharmaceutically acceptable salts thereof, are provided: Image (I) wherein Y is selected from p-toluenesulfonyl and -SO2CF3 and R2 is selected from the group comprising hydrogen, trityl, methoxytrityl, dimethoxytrityl, acetyl, a C2-C6 alkylacyl group, a C6-C9 arylacyl group, allyl, 2,2,2- trichloroethyl, phosphates and salts thereof, tosyl and mesyl. A process for the production of cytidine compounds, including the compounds of Formula I, is provided and comprises reacting a 2',3'-O- dialkylstannylene cytidine-type compound with an amine in the presence of a sulfonyl compound. Compounds of Formula I can be used to inhibit RNA synthesis.

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