YU15195A - PROCEDURE FOR OBTAINING 2-BETA-D-RIBOFURANOSYLSELENAZOLE-4-CARBOXIAMIDE - Google Patents
PROCEDURE FOR OBTAINING 2-BETA-D-RIBOFURANOSYLSELENAZOLE-4-CARBOXIAMIDEInfo
- Publication number
- YU15195A YU15195A YU15195A YU15195A YU15195A YU 15195 A YU15195 A YU 15195A YU 15195 A YU15195 A YU 15195A YU 15195 A YU15195 A YU 15195A YU 15195 A YU15195 A YU 15195A
- Authority
- YU
- Yugoslavia
- Prior art keywords
- beta
- ribofuranosylselenazole
- selenazofurine
- anhydro
- synthesis
- Prior art date
Links
Landscapes
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Cilj pronalaska je dobijanje, na nov način, 2-beta-D-ribofuranozilselenazol-4-karboksiamida (selenazofurina) za koji je utvrđena značajna antitumorska aktivnost kod životinja i širok spektar antiviralne aktivnosti na ćelijskim kulturama. Postupkom prema pronalasku je opisan nov put sinteze etil 2-beta-D-ribofuranozilselenazol-4-karboksilata, intermedijera u sintezi selenazofurina, iz metil-2,5-anhidro-D-alonimidata, čime se obezbeđuje ekonomičniji postupak i znatno veći prinos finalnog proizvoda - selenazofurina. Postupak se sastoji u sintezi metil-2,5-anhidro-D-alonimidata, koji se dobija baznom metanolizom 2,3-anhidro-3,4,6-tri-O-benzoil-beta-D-alononitrila, a koji sa gasovitim vodonik selenidom daje 2,5-anhidro-D-alonselenoamid, koji se ne izoluje nego in situ reaguje sa etil-alfa-bromopiruvatom dajući etil-2-beta-D-ribofuranozilselenazol-4-karboksilat koji amonolizom prelazi u 2-beta-D-ribofuranozilselenazol-4-karboksiamid-selenazofurin.The aim of the invention is to provide, in a novel way, 2-beta-D-ribofuranosylselenazole-4-carboxamide (selenazofurine), which has been shown to have significant antitumor activity in animals and a wide range of antiviral activity on cell cultures. The process of the invention describes a novel route for the synthesis of ethyl 2-beta-D-ribofuranosylselenazole-4-carboxylate, an intermediate in the synthesis of selenazofurine from methyl-2,5-anhydro-D-alonimidate, thereby providing a more economical process and a significantly higher yield of the final product - selenazofurine. The process consists in the synthesis of methyl-2,5-anhydro-D-alonimidate, obtained by basic methanolysis of 2,3-anhydro-3,4,6-tri-O-benzoyl-beta-D-alononitrile, which is gaseous hydrogen selenide gives 2,5-anhydro-D-allonselenoamide, which is not isolated but reacted in situ with ethyl alpha-bromopyruvate to give ethyl 2-beta-D-ribofuranosylselenazole-4-carboxylate which by ammonolysis is converted to 2-beta-D -ribofuranosylselenazole-4-carboxamide-selenazofurine.
Priority Applications (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
YU15195A YU49442B (en) | 1995-03-07 | 1995-03-07 | PROCESS FOR OBTAINING 2-β-D-RIBOFURANOSYLSELENOAZOLE-4-CARBOXYLAMIDE |
US08/603,106 US5907036A (en) | 1995-02-17 | 1996-02-20 | Procedures for obtaining ribo-C-nucleosides |
AU52980/96A AU5298096A (en) | 1995-02-17 | 1996-02-20 | Procedures for obtaining ribo-c-nucleosides |
PCT/US1996/002512 WO1996026212A1 (en) | 1995-02-17 | 1996-02-20 | Procedures for obtaining ribo-c-nucleosides |
EP96909514A EP0804447A1 (en) | 1995-03-07 | 1996-02-20 | Procedures for obtaining ribo-c-nucleosides |
SK1202-97A SK120297A3 (en) | 1995-03-07 | 1996-02-20 | Procedures for obtaining ribo-c-nucleosides |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
YU15195A YU49442B (en) | 1995-03-07 | 1995-03-07 | PROCESS FOR OBTAINING 2-β-D-RIBOFURANOSYLSELENOAZOLE-4-CARBOXYLAMIDE |
Publications (2)
Publication Number | Publication Date |
---|---|
YU15195A true YU15195A (en) | 1998-07-10 |
YU49442B YU49442B (en) | 2006-03-03 |
Family
ID=25548578
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
YU15195A YU49442B (en) | 1995-02-17 | 1995-03-07 | PROCESS FOR OBTAINING 2-β-D-RIBOFURANOSYLSELENOAZOLE-4-CARBOXYLAMIDE |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP0804447A1 (en) |
SK (1) | SK120297A3 (en) |
YU (1) | YU49442B (en) |
-
1995
- 1995-03-07 YU YU15195A patent/YU49442B/en unknown
-
1996
- 1996-02-20 SK SK1202-97A patent/SK120297A3/en unknown
- 1996-02-20 EP EP96909514A patent/EP0804447A1/en not_active Withdrawn
Also Published As
Publication number | Publication date |
---|---|
YU49442B (en) | 2006-03-03 |
SK120297A3 (en) | 1998-01-14 |
EP0804447A1 (en) | 1997-11-05 |
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