Title: Conversion of uracil derivatives to cytosine derivatives
Application Number: 86103615 Application Date: 1986.06.01
Publication Number: 1005484 Publication Date: 1986.12.03
Approval Pub. Date: 1991.12.25 Granted Pub. Date: 1991.12.25
International Classifi-cation: C07H19/06
Applicant(s) Name: Takeda Chemical Industries, Ltd. Address:
Inventor(s) Name: Kiyoharu Matsumoto;Masaaki Tsurushima;Mitsuru Kawa
Attorney & Agent: CAO HENGXING
Abstract:
    A process is disclosed for producing a 4-O-sulfonyluracil derivative of the formula [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 [wherein R1 and R2 are as defined above] with an organic sulfonylating agent of the formula R3SO2X [wherein R3SO2 is an organic sulfonyl and X is halogen] in the presence of potassium carbonate. The obtained 4-O-sulfonyluracil is further subjected to amination. The processes are industrially adavantageous and produce cytosine derivatives such as cytidine in high yield.
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