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Development of a safe and scalable route towards a tau PET tracer precursor
Authors:Bjoern Bartels  Philipp Cueni  Dieter Muri  Matthias Koerner
Institution:Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland
Abstract:A scalable 5-step synthesis of the diazacarbazole derivative 1 used as tau PET tracer precursor is reported. Key features of this synthesis include a Buchwald-Hartwig amination, a Pd catalyzed C/>H activation and a <em>Suzuki-Miyaura</em> cross-coupling.</td>
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Keywords:calcd  calculated  h  hour(s)  IPC  in-process control  min  minutes  NFT  neurofibrillary tangle  NSB  non-specific binding  NT  neutropil thread  r  t    ambient (room) temperature  Diazacarbazole  Direct arylation  PET tracer  Tau
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