Process for producing n4-acyl-5'-deoxy-5-fluorocytidine...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/073 (2006.01) C07H 19/06 (2006.01)

Patent

CA 2110335

A novel process for producing N'-acyl-5'-deoxy-5- fluorocytidine derivatives using the novel 5'-deoxy-5- fluoro-N4, 2'-0,3'-0-triacylcytidine derivatives are provided. 5-Deoxy-1,2,3-tri-0-acyl-.beta.-D-ribofuranoside is reacted with 5-fluorocytosine to produce 5'-deoxy-2',3'-di-0-acyl-5- fluorocytidine, followed by acylation. The acyl radicals of the obtained 5'-deoxy-5-fluoro-N4,2'-0,3'-0-triacylcytidine derivatives are selectively de-D-acylated to obtain N4-acyl- 5'-deoxy-5-fluorocytidine derivatives. From fluorocytosine, N4-acyl-5'-deoxy-5-fluorocytidine derivatives can be ob- tained through very few steps in high yield.

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