发明申请
US20120289716A1 METHOD FOR HIGH-SPEED FLUOROMETHYLATION AND PROCESS FOR PREPARATION OF PET TRACER USING SAME
有权
用于高速氟代乙酰化的方法和使用其制备PET追踪器的方法
- 专利标题: METHOD FOR HIGH-SPEED FLUOROMETHYLATION AND PROCESS FOR PREPARATION OF PET TRACER USING SAME
- 专利标题(中): 用于高速氟代乙酰化的方法和使用其制备PET追踪器的方法
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申请号: US13513565申请日: 2010-12-03
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公开(公告)号: US20120289716A1公开(公告)日: 2012-11-15
- 发明人: Masaaki Suzuki , Hisashi Doi , Miki Goto
- 申请人: Masaaki Suzuki , Hisashi Doi , Miki Goto
- 申请人地址: JP Wako-shi ,Saitama
- 专利权人: RIKEN
- 当前专利权人: RIKEN
- 当前专利权人地址: JP Wako-shi ,Saitama
- 优先权: JP2009-277028 20091204
- 国际申请: PCT/JP2010/071632 WO 20101203
- 主分类号: C07C67/343
- IPC分类号: C07C67/343 ; C07D311/30
摘要:
Provided are: a method for rapid fluoromethylation, by which a fluoromethyl group can be easily bonded to an aromatic-ring carbon of an aromatic compound with little generation of by-products; and a process for preparation of a PET tracer using the same. The method is characterized by cross-coupling an organoboron compound in which an aromatic ring is bonded to a boron atom with FCX2Br (wherein X is ordinary hydrogen or heavy hydrogen) in a solvent obtained by adding water to an aprotic polar solvent, in the presence of a palladium complex, a phosphine ligand, and a base.
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