1.
Bioorg Med Chem
; 26(4): 970-976, 2018 02 15.
Article
in English
| MEDLINE
| ID: mdl-29074348
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.
Subject(s)
Carbazoles/chemistry , tau Proteins/metabolism , Alzheimer Disease/diagnosis , Alzheimer Disease/metabolism , Amination , Carbazoles/chemical synthesis , Carbazoles/metabolism , Catalysis , Humans , Palladium/chemistry , Positron-Emission Tomography , tau Proteins/chemistry
2.
J Org Chem
; 80(2): 1249-57, 2015 Jan 16.
Article
in English
| MEDLINE
| ID: mdl-25495477
ABSTRACT
A new method for the straightforward synthesis of 2-amino-[1,2,4]triazolo[1,5-a]pyridines and derivatives is presented. The target products are synthesized in high yields from guanidylpyridines and analogues via copper-catalyzed N-N coupling. The present methodology shows a wide scope, tolerating not only different substituents on the pyridine ring but also different heterocylic rings such as pyrazines, pyrimidines, and pyridazines.
