96727-98-9Relevant articles and documents
Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists
Savall, Brad M.,Wu, Duncan,De Angelis, Meri,Carruthers, Nicholas I.,Ao, Hong,Wang, Qi,Lord, Brian,Bhattacharya, Anindya,Letavic, Michael A.
, p. 671 - 676 (2015/06/23)
We describe the synthesis and SAR of 1,2,3-triazolopiperidines as a novel series of potent, brain penetrant P2X7 antagonists. Initial efforts yielded a series of potent human P2X7R antagonists with moderate to weak rodent potency, some CYP inhibition, poo
Use of the graebe-ullmann reaction in the synthesis of 8-methyl-γ- carboline and isomeric aromatic aza-γ-carbolines
Alekseev,Kurkin,Yurovskaya
, p. 1235 - 1250 (2013/03/13)
Two variants of the Graebe-Ullmann reaction were used to obtain 8-methyl-5H-pyrido[4,3-b]indole (8-methyl-γ-carboline) and the conditions for this reaction were optimized. The feasibility of using this method was studied for the synthesis of a series of isomeric aromatic aza-γ- carbolines from the corresponding 1-(pyridyl)-1H-1,2,3-triazolo[4,5-c]pyridines under thermal and microwave irradiation conditions.