Title:
PROCESS FOR ANOMERIZING NUCLEOSIDE
Document Type and Number:
Japanese Patent JP3462893
Kind Code:
B2
Abstract:
PURPOSE: To obtain a pharmaceutically useful beta-anomernucleoside in a high yield by bringing alpha-anomer enriched nucleoside in contact with a hydroxide base in an organic solvent.
CONSTITUTION: The objective nucleoside is obtained by bringing alpha-anomer enriched nucleoside of formula I {wherein R1 represents H, lower alkyl, fluoro or the like; R2 represents H, azide or the like; R3 represents H or azide; R4 represents H, azide or the like; R5 represents H, azide or the like; Z represents a nucleobase group of formula II [wherein X represents N or CR8 (wherein R8 represents H or lower alkyl); R4 represents amino, lower alkylamino or the like; R7 represents H, lower alkyl or the like]} with (preferably from 0.5 to 5 molar concentration of) a hydroxide base such as lithium hydroxide, potassium hydroxide or the like, in a solvent such as methanol, ethanol or the like.
Inventors:
Thomas Charles Briton
Michael Edward Le Tornew
Michael Edward Le Tornew
Application Number:
JP21565393A
Publication Date:
November 05, 2003
Filing Date:
August 31, 1993
Export Citation:
Assignee:
ELI LILLY AND COMPANY
International Classes:
C07H19/048; C07H19/06; C07H1/00; (IPC1-7): C07H19/06; C07H1/00
Other References:
ＨＥＴＥＲＯＣＹＣＬＥＳ，１９７７年，Ｖｏｌ．８，ｐ．４２７−４３２
Ｎｕｃｌｅｉｃ Ａｃｉｄｓ Ｒｅｓｅａｒｃｈ，１９７６年 ７月，Ｖｏｌ．３， Ｎｏ．７，ｐ．１７９１−１８１０
Ｎｕｃｌｅｉｃ Ａｃｉｄｓ Ｒｅｓｅａｒｃｈ，１９７６年 ７月，Ｖｏｌ．３， Ｎｏ．７，ｐ．１７９１−１８１０
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)
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