公开(公告)号：US20170224851A1

公开(公告)日：2017-08-10

申请号：US15323046

申请日：2015-07-02

Applicant: The Regents of the University of California

Inventor： Maxim Sergeev ,  Federica Morgia ,  Robert Michael Van Dam ,  Mark Lazari

IPC: A61K51/04 ,  C07B59/00 ,  C07C17/361 ,  C07H19/052 ,  C07D207/16 ,  B01J21/06 ,  C07C67/333 ,  C07C201/12 ,  C07C253/30 ,  C07D217/22 ,  C07D241/16 ,  C07D213/61 ,  C07D207/09 ,  C07D405/06

CPC classification number: A61K51/04 ,  A61K51/0446 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0491 ,  B01J21/063 ,  C07B59/00 ,  C07B59/001 ,  C07B59/002 ,  C07B59/005 ,  C07B2200/05 ,  C07C17/361 ,  C07C67/307 ,  C07C67/333 ,  C07C201/12 ,  C07C253/30 ,  C07C2601/14 ,  C07D207/09 ,  C07D207/16 ,  C07D213/61 ,  C07D215/18 ,  C07D217/22 ,  C07D241/16 ,  C07D405/04 ,  C07D405/06 ,  C07H19/052 ,  C07C69/76 ,  C07C205/12 ,  C07C255/50 ,  C07C25/13 ,  C07C22/08 ,  C07C25/22 ,  C07C19/08 ,  C07C23/10

Abstract: Inter alia, the first titania-catalyzed [18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.

公开(公告)号：US09895454B2

公开(公告)日：2018-02-20

申请号：US15323046

申请日：2015-07-02

Applicant: The Regents of the University of California

Inventor： Maxim Sergeev ,  Federica Morgia ,  Robert Michael Van Dam ,  Mark Lazari

IPC: A61K51/04 ,  C07B59/00 ,  C07D207/09 ,  C07C17/361 ,  C07H19/052 ,  C07D207/16 ,  C07D405/06 ,  C07C67/333 ,  C07C201/12 ,  C07C253/30 ,  C07D217/22 ,  C07D241/16 ,  C07D213/61 ,  B01J21/06

CPC classification number: A61K51/04 ,  A61K51/0446 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0491 ,  B01J21/063 ,  C07B59/00 ,  C07B59/001 ,  C07B59/002 ,  C07B59/005 ,  C07B2200/05 ,  C07C17/361 ,  C07C67/307 ,  C07C67/333 ,  C07C201/12 ,  C07C253/30 ,  C07C2601/14 ,  C07D207/09 ,  C07D207/16 ,  C07D213/61 ,  C07D215/18 ,  C07D217/22 ,  C07D241/16 ,  C07D405/04 ,  C07D405/06 ,  C07H19/052 ,  C07C69/76 ,  C07C205/12 ,  C07C255/50 ,  C07C25/13 ,  C07C22/08 ,  C07C25/22 ,  C07C19/08 ,  C07C23/10

Abstract: Inter alia, the first titania-catalyzed [18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.