1.
Bioorg Med Chem
; 26(4): 970-976, 2018 02 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-29074348
RESUMEN
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.
Asunto(s)
Carbazoles/química , Proteínas tau/metabolismo , Enfermedad de Alzheimer/diagnóstico , Enfermedad de Alzheimer/metabolismo , Aminación , Carbazoles/síntesis química , Carbazoles/metabolismo , Catálisis , Humanos , Paladio/química , Tomografía de Emisión de Positrones , Proteínas tau/química
2.
J Org Chem
; 80(2): 1249-57, 2015 Jan 16.
Artículo
en Inglés
| MEDLINE
| ID: mdl-25495477
RESUMEN
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.
