发明公开
EP2774933A1 ULIPRISTAL ACETATE PREPARATION METHOD AND INTERMEDIATE THEREOF
有权
ZWISCHENPRODUKTE DAVON的HERSTELLUNGSVERFAHRENFÜRULIPRISTALACETAT
- 专利标题: ULIPRISTAL ACETATE PREPARATION METHOD AND INTERMEDIATE THEREOF
- 专利标题(中): ZWISCHENPRODUKTE DAVON的HERSTELLUNGSVERFAHRENFÜRULIPRISTALACETAT
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申请号: EP12845071.5申请日: 2012-07-12
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公开(公告)号: EP2774933A1公开(公告)日: 2014-09-10
- 发明人: LUO, Junzhi , SUN, Yongqiang , LUO, Xun , YAN, Yimin , WANG, Zhaojun , QIAN, Mingxia , TU, Yongrui
- 申请人: Utopharm (Shanghai) Co., Ltd , Changzhou No.4 Pharmaceutical Factory Co., Ltd.
- 申请人地址: Building 3 No.237 Xitai Rd. Xu Hui District Shanghai 200232 CN
- 专利权人: Utopharm (Shanghai) Co., Ltd,Changzhou No.4 Pharmaceutical Factory Co., Ltd.
- 当前专利权人: Utopharm (Shanghai) Co., Ltd,Changzhou No.4 Pharmaceutical Factory Co., Ltd.
- 当前专利权人地址: Building 3 No.237 Xitai Rd. Xu Hui District Shanghai 200232 CN
- 代理机构: Török, Ferenc
- 优先权: CN201110339479 20111101
- 国际公布: WO2013063859 20130510
- 主分类号: C07J41/00
- IPC分类号: C07J41/00 ; C07J21/00 ; C07J75/00
摘要:
A method as well as new intermediates for preparing Ulipristal acetate (a compound I) and a method for preparing the new intermediates are provided. The intermediate in a constitutional formula IV is conductive to reacting with methyl lithium or methyl Grignard reagent, a protective group is easy to be removed after a reaction, side reactions are few, a mid-term treatment is simple, the reagents used are cheap, costs are low and the yield is high, if a compound in a constitutional formula V is obtained by the reaction of a compound in a constitutional formula III and the intermediate in the constitutional formula IV, the yield of a two-step reaction is 75%, a purity is above 98%.
wherein R is defined in the specification.
wherein R is defined in the specification.
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