Inventors:
William Bauta - San Antonio TX, US
Brian Burke - Lafayette IN, US
Brian Schulmeier - San Antonio TX, US
William Cantrell - San Antonio TX, US
Dennis Lovett - San Antonio TX, US
Jose Puente - San Antonio TX, US
International Classification:
C07H019/16
Abstract:
The present invention provides for the preparation -adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and solvent. The present invention also provides for the stereoselective preparation of 2-deoxy--D-adenine nucleosides wherein a blocked 2-deoxy--D-arabinofuranosyl halide is coupled with the salt of an adenine derivative. The forgoing aspects of the present invention are utilized in the preparation of a clofarabine composition wherein the ratio of to -anomer is at least 99:1.