Development of a safe and scalable route towards a tau PET tracer precursor. Issue 4 (15th February 2018)

• Record Type: Journal Article
• Authors: Bartels, Bjoern; Cueni, Philipp; Muri, Dieter; Koerner, Matthias
• Is Part Of: Bioorganic & medicinal chemistry. Volume 26:Issue 4(2018)
• Page Start: 970
• Page End: 976
• Publication Date: 2018-02-15
• Subjects: 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; Buchwald-Hartwig amination -- CH activation -- Diazacarbazole -- Direct arylation -- PET tracer -- Suzuki-Miyaura cross-coupling -- Stille coupling -- Tau; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2017.10.007
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: A scalable 5-step synthesis of the diazacarbazole derivative1 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.