公开(公告)号：EP1412369B1

公开(公告)日：2008-05-07

申请号：EP02768391.1

申请日：2002-08-01

申请人： Ilex Oncology, Inc.

发明人： BAUTA, William, E. ,  SCHULMEIER, Brian, E. ,  CANTRELL, William, R., Jr. ,  LOVETT, Dennis ,  PUENTE, Jose

IPC分类号： C07H19/00

CPC分类号： C07H19/16

摘要： The present invention provides for the preparation β-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-β-D-adenine nucleosides wherein a blocked 2-deoxy-β-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 β to α-anomer is at least 99:1.

公开(公告)号：EP1412369A2

公开(公告)日：2004-04-28

申请号：EP02768391.1

申请日：2002-08-01

申请人： Ilex Oncology, Inc.

发明人： BAUTA, William, E. ,  SCHULMEIER, Brian, E. ,  CANTRELL, William, R., Jr. ,  LOVETT, Dennis ,  PUENTE, Jose

IPC分类号： C07H19/00

CPC分类号： C07H19/16

摘要： The present invention provides for the preparation β-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-β-D-adenine nucleosides wherein a blocked 2-deoxy-β-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 β to α-anomer is at least 99:1.