The present invention provides for the preparation beta-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-beta-D-adenine nucleosides wherein a blocked 2-deoxy-beta-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 beta to alpha-anomer is at least 99:1.
申请公布号
WO03011877(A2)
申请公布日期
2003.02.13
申请号
WO2002US24392
申请日期
2002.08.01
申请人
ILEX ONCOLOGY INC.;BAUTA, WILLIAM, E.;SCHULMEIER, BRIAN, E.;CANTRELL, WILLIAM, R., JR.;LOVETT, DENNIS;PUENTE, JOSE
发明人
BAUTA, WILLIAM, E.;SCHULMEIER, BRIAN, E.;CANTRELL, WILLIAM, R., JR.;LOVETT, DENNIS;PUENTE, JOSE