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Development of a safe and scalable route towards a tau PET tracer precursor
Bjoern Bartels1, Philipp Cueni1, Dieter Muri1
1Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland.
Bioorganic & Medicinal Chemistry
|October 28, 2017
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 CH activation and a Suzuki-Miyaura cross-coupling.
Keywords:
Buchwald-Hartwig aminationCH activationDiazacarbazoleDirect arylationPET tracerStille couplingSuzuki-Miyaura cross-couplingTau
