Conversion of uracil derivatives to cytosine derivatives

Details Conversion of uracil derivatives to cytosine derivatives Conversion of uracil derivatives to cytosine derivatives

C - Chemistry, Metallurgy

07

H

260/229.2

C07H 19/067 (2006.01) C07H 19/06 (2006.01)

Patent

CA 1268174

24205-676 Abstract of the Disclosure A process is disclosed for producing a 4-0-sulfonyi- uracil derivative of the formula Image [wherein R1 is hydrogen, halogen, alkyl and alkoxy, R2 is glycosyl having protected hydroxyls; and -SO2R3 is an organic sulfonyl] which comprises reacting an uracil derivative of the formula Image [wherein R1 and R2 are the same above] with an organic sulfonylating agent of the formula R3 SO2X [wherein R3SO2 is an organic sulfonyl and X is halogen] in the presence of potassium carbonate. The obtained 4-0-sulfonyluracil is further subjected to amination. The processes are industrially advantageous and produce cytosine derivatives such as cytidine in high yield. The 4-0-sulfonyluracil derivative is useful as an intermediate for production of drugs such as cytidine diphosphate choline whose generic name is Citicoline.

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