- Hydrogenation of 2-fluoro-9-(2,3,5-tri-o-benzyl-beta-D-arabinofuranosyl)adenine
-
A process for the preparation of 2-fluoro-9-beta-D-arabinofuranosyl purine (VII) by a reaction of palladium chloride and hydrochloric acid with 2-fluoro-9-(2,3,5-tribenzyl-beta-D-arabinofuranosyl)adenine (VI) at elevated pressures in a solvent for (VI) is described. The reaction is rapid, economical and efficient.
- -
-
-
- Process for the preparation of 2-amino (2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl)adenine
-
A process for the preparation of 2-amino-9-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl) adenine (V) is described. The process uses a protected 2,6-di(tri-alkylsilylamino)-9-trialkylsilylpurine (II) which is reacted with protected chlorosugar 2,3,5-tri-O-benzyl-1-chloro-D-arabinofuranose (III) and then the protection groups are removed from the 2 and 6 positions. The process provides a 9-beta-D-arabinofuranosyl-2-fluoroadenine (VII) which is an antileukenine drug.
- -
-
-
- Process for the preparation of 2-amino-9-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl) adenine and novel intermediates
-
A process for the preparation of 2,6-diamino-9-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl)purine (V) by reacting 2,6-di(alkoxyacetamido)purine (II) with 2,3,5-tri-O-benzyl-1-chloro-alpha-D-arabinofuranose (III) to produce 2,6-di(alkoxyacetamido)-9-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl)purine (IV) and then deprotecting the 2,6-positions to produce the 2,6-diamine (V) is described. The process provides purine (V) in high yield. Purine (V) is an intermediate in the preparation of 9-beta-D-arabinofuranosyl-2-fluoroadenine which is a cytotoxic agent.
- -
-
-
- Anticancer and antiviral activity of 9-β-D-arabinofuranosyl-2-fluoroadenine
-
A method of utilizing 9-β-D-arabinofuranosyl-2-fluoroadenine, known as 2-F-AraA (NSC 118218), in the treatment of murine leukemia and as an antiviral agent for DNA viruses, such as DNA viruses Herpes Simplex Virus Type I and Vaccinia virus grown in H.Ep-2 cells in culture. An operable dosage for utilization of 2-F-AraA is a treatment span of 1-10 days with the dosage 2-8 times per day at 8-400 mg/kg/dose. It has been further found that a single dosage on days 1, 5, and 9 based on a 10-day treatment schedule gave satisfactory results.
- -
-
-
- Amino purine derivatives
-
Compounds of the formula STR1 where R1 is amino or lower alkylamino, R2 is amine or hydrogen and pharmaceutically acceptable salts thereof, provided that when R1 is amino, R2 is amino. The compounds are useful as immune suppressants and as antivirals.
- -
-
-
- Purine sugar derivatives
-
This invention relates to purine sugar derivatives which are useful as suppressors of the immune response and as antiviral agents, and to methods of preparation thereof.
- -
-
-