The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: (S)-tert-Butyl 2-methyl-3-oxopiperazine-1-carboxylate( cas:1799971-34-8 ) is researched.Name: (S)-tert-Butyl 2-methyl-3-oxopiperazine-1-carboxylate.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 the article 《Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists》 about this compound( cas:1799971-34-8 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: dihydrotriazolopyrazinylmethanone preparation purinoceptor antagonist antidepressant anticonvulsant; 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones; CNS; Depression; P2X7. Let’s learn more about this compound (cas:1799971-34-8).
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.
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