Invention Grant
US08933252B2 Method for rapid fluoromethylation and method for preparation of PET tracer using the same
有权
快速氟甲基化方法及使用该方法制备PET示踪剂
- Patent Title: Method for rapid fluoromethylation and method for preparation of PET tracer using the same
- Patent Title (中): 快速氟甲基化方法及使用该方法制备PET示踪剂
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Application No.: US13513565Application Date: 2010-12-03
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Publication No.: US08933252B2Publication Date: 2015-01-13
- Inventor: Masaaki Suzuki , Hisashi Doi , Miki Goto
- Applicant: Masaaki Suzuki , Hisashi Doi , Miki Goto
- Applicant Address: JP Wako-Shi
- Assignee: Riken
- Current Assignee: Riken
- Current Assignee Address: JP Wako-Shi
- Agency: Birch, Stewart, Kolasch & Birch, LLP
- Priority: JP2009-277028 20091204
- International Application: PCT/JP2010/071632 WO 20101203
- International Announcement: WO2011/068181 WO 20110609
- Main IPC: C07C67/343
- IPC: C07C67/343 ; C07D311/30 ; A61K51/04 ; C07B59/00

Abstract:
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.
Public/Granted literature
- US20120289716A1 METHOD FOR HIGH-SPEED FLUOROMETHYLATION AND PROCESS FOR PREPARATION OF PET TRACER USING SAME Public/Granted day:2012-11-15
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