A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-1,2,3triazolo4,5-cpyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate

• Published in: Journal of medicinal chemistry Vol. 61; no. 1; p. 207
• Main Authors: Chrovian, Christa C, Soyode-Johnson, Akinola, Peterson, Alexander A, Gelin, Christine F, Deng, Xiaohu, Dvorak, Curt A, Carruthers, Nicholas I, Lord, Brian, Fraser, Ian, Aluisio, Leah, Coe, Kevin J, Scott, Brian, Koudriakova, Tatiana, Schoetens, Freddy, Sepassi, Kia, Gallacher, David J, Bhattacharya, Anindya, Letavic, Michael A
• Format: Journal Article
• Language: English
• Published: 11.01.2018

A single pot dipolar cycloaddition reaction/Cope elimination sequence was developed to access novel 1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridine P2X7 antagonists that contain a synthetically challenging chiral center. The structure-activity relationships of the new compounds are described. T...