发明授权
US08415487B2 Process for preparing (3R)-2′-(4-bromo-2-fluorobenzyl)spiro-[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-A]pyrazine]-1′,2,3′,5(2H′)-tetraone
失效
制备（3R）-2' - （4-溴-2-氟苄基）螺 - [吡咯烷-3,4'（1'H） - 吡咯并[1,2-A]吡嗪] -1' 3'，5（2H'） - 四酮
![Process for preparing (3R)-2′-(4-bromo-2-fluorobenzyl)spiro-[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-A]pyrazine]-1′,2,3′,5(2H′)-tetraone](/docs/US/2013-04-09/US08415487B2/abs.jpg.600x600.jpg)
- 专利标题： Process for preparing (3R)-2′-(4-bromo-2-fluorobenzyl)spiro-[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-A]pyrazine]-1′,2,3′,5(2H′)-tetraone
- 专利标题（中）： 制备（3R）-2' - （4-溴-2-氟苄基）螺 - [吡咯烷-3,4'（1'H） - 吡咯并[1,2-A]吡嗪] -1' 3'，5（2H'） - 四酮
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申请号： US13239731申请日： 2011-09-22
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公开(公告)号： US08415487B2公开(公告)日： 2013-04-09
- 发明人: Daisuke Tanaka , Toshiyuki Negoro
- 申请人： Daisuke Tanaka , Toshiyuki Negoro
- 申请人地址： JP Osaka
- 专利权人： Dainippon Sumitomo Pharma Co., Ltd.
- 当前专利权人： Dainippon Sumitomo Pharma Co., Ltd.
- 当前专利权人地址： JP Osaka
- 代理机构： Wenderoth, Lind & Ponack, L.L.P.
- 优先权： JP2006-187588 20060707
- 主分类号： C07D207/444
- IPC分类号： C07D207/444
![Process for preparing (3R)-2′-(4-bromo-2-fluorobenzyl)spiro-[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-A]pyrazine]-1′,2,3′,5(2H′)-tetraone](/abs-image/US/2013/04/09/US08415487B2/abs.jpg.150x150.jpg)
摘要：
The present invention is a process for preparing (3R)-2′-(4-bromo-2-fluorobenzyl)spiro-[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2H′)-tetraone, comprising, for example, the following steps: (1) reacting a compound of the formula (III) wherein R is a C1-6 alkyl group, with 2,5-dimethoxytetrahydrofuran to provide a compound of the formula (IV) wherein R is a C1-6 alkyl group; (2) reacting the compound of the formula (IV) wherein R is a C1-6 alkyl group, with trichloroacetyl chloride to provide a compound of the formula wherein R is a C1-6 group; and (3) reacting the compound provided in step (2) with 4-bromo-2-fluorobenzylamine to provide (3R)-2′-(4-bromo-2-fluorobenzyl)spiro-[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2H′)-tetraone.
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