发明授权
- 专利标题: Method for the preparation of 2′-deoxy-2′,2′-difluorocytidine
- 专利标题(中): 2'-脱氧-2',2'-二氟胞苷的制备方法
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申请号: US11573869申请日: 2005-12-29
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公开(公告)号: US07799907B2公开(公告)日: 2010-09-21
- 发明人: Jaeheon Lee , Gha Seung Park , Moonsub Lee , Hyo-Jeong Bang , Jae Chul Lee , Cheol Kyong Kim , Chang-Ju Choi , Han Kyong Kim , Hoe Chul Lee , Young-Kil Chang , Gwan Sun Lee
- 申请人: Jaeheon Lee , Gha Seung Park , Moonsub Lee , Hyo-Jeong Bang , Jae Chul Lee , Cheol Kyong Kim , Chang-Ju Choi , Han Kyong Kim , Hoe Chul Lee , Young-Kil Chang , Gwan Sun Lee
- 申请人地址: KR Kyungki-do
- 专利权人: Hanmi Pharm. Co., Ltd
- 当前专利权人: Hanmi Pharm. Co., Ltd
- 当前专利权人地址: KR Kyungki-do
- 代理机构: Sughrue Mion, PLLC
- 优先权: KR10-2004-0116316 20041230; WOPCT/KR2005/001954 20050623
- 国际申请: PCT/KR2005/004633 WO 20051229
- 国际公布: WO2006/071090 WO 20060706
- 主分类号: C07H19/073
- IPC分类号: C07H19/073
摘要:
Provided is an improved method for stereoselectively preparing 2′-deoxy-2′,2′-difluorocytidine of formula (I), which includes reacting a 1-halo ribofuranose compound with a nucleobase of formula (IV) in a solvent to obtain a nucleo side of formula (II) with removal of a silyl halide ((alkyl)3SiX (X=halide)); and deprotecting the nucleoside of formula (II) to obtain 2′-deoxy-2′,2′-difluorocytidine of formula (I). 2′-Deoxy-2′,2′-difluorocytidine of formula (I) is effective for treating various cancers such as non-small cell lung (NSCLC), pancreatic, bladder, breast or ovarian cancers.
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