Rudolph, Dale A.; Alcazar, Jesus; Ameriks, Michael K.; Anton, Ana Belen; Ao, Hong; Bonaventure, Pascal; Carruthers, Nicholas I.; Chrovian, Christa C.; De Angelis, Meri; Lord, Brian; Rech, Jason C.; Wang, Qi; Bhattacharya, Anindya; Andres, Jose Ignacio; Letavic, Michael A. published their research in Bioorganic & Medicinal Chemistry Letters on August 15 ,2015. The article was titled 《Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists》.Application In Synthesis of (S)-tert-Butyl 2-methyl-3-oxopiperazine-1-carboxylate The article contains the following contents:
The optimization efforts that led to a novel series of Me substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones that are potent rat and human P2X7 antagonists are described. These efforts resulted in the discovery of compounds with good drug-like properties that are capable of high P2X7 receptor occupancy in rat following oral administration, including compounds I (P2X7 IC50 = 7.7 nM) and II (P2X7 IC50 = 7.7 nM). These compounds are expected to be useful tools for characterizing the effects of P2X7 antagonism in models of depression and epilepsy, and several of the compounds prepared are candidates for effective P2X7 PET tracers. The results came from multiple reactions, including the reaction of (S)-tert-Butyl 2-methyl-3-oxopiperazine-1-carboxylate(cas: 1799971-34-8Application In Synthesis of (S)-tert-Butyl 2-methyl-3-oxopiperazine-1-carboxylate)
(S)-tert-Butyl 2-methyl-3-oxopiperazine-1-carboxylate(cas: 1799971-34-8) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Application In Synthesis of (S)-tert-Butyl 2-methyl-3-oxopiperazine-1-carboxylate
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics