5368-28-5Relevant articles and documents
An Efficient Two-Step Preparation of α-, β-, γ- or δ-Amino Acids from 2-Pyrazinones, 2-Hydroxypyrimidines or 2-Pyridones Respectively
Zacharie, Boulos,Abbott, Shaun D.,Baigent, Christopher B.,Doyle, Christopher,Yalagala, Ravi Shekar
, p. 6486 - 6493 (2018/11/23)
A practical and efficient two-step procedure is reported for the preparation of a variety of α-, β-, γ- and δ-amino acids from 2-pyridone, 2-pyrazinone or 2-hydroxypyrimidine and derivatives. The procedure is amenable to scale-up and in most cases no chromatographic purification of the product is required. This approach is useful, especially in the synthesis of amino acids or deuterated amino acids that are not obtained by other methods.
Novel Phenyl-Substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 Antagonists with Robust Target Engagement in Rat Brain
Chrovian, Christa C.,Soyode-Johnson, Akinola,Ao, Hong,Bacani, Genesis M.,Carruthers, Nicholas I.,Lord, Brian,Nguyen, Leslie,Rech, Jason C.,Wang, Qi,Bhattacharya, Anindya,Letavic, Michael A.
, p. 490 - 497 (2016/05/19)
Novel 5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists were optimized to allow for good blood-brain barrier permeability and high P2X7 target engagement in the brain of rats. Compound 25 (huP2X7 IC50 = 9 nM; rat P2X7 IC50
Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process
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Page/Page column 13, (2008/06/13)
Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The compounds are characterized by the formulae: wherein: n is an integer of 1 to 6; X, Y, Z1 and Z2 can be the same or different and are hydrogen, halo, haloalkyl, alkyl, aryl, (C1-C6) alkoxy, N-alkyl,(C2-C6) acyloxy, N-alkylene, —SH, —SR, wherein R is from the same group as R1 and R2 and can be the same or different than R1 and R2, amino, nitro, cyano, hydroxy, C(═O) OR6, —C(═O) NR5R4, NR3R2, or S(αO)k R1 wherein k is 1 or 2, and R1 to R6 are independently hydrogen or (C1-C6) alkyl; R1, and R2 can be the same or different and are hydrogen, (C1-C6) alkyl, hydroxyalkyl or mercaptoalkyl, —C(═O) OR1, cyano, (C1-C6) alkenyl, (C2-C6) alkynyl, or 1,2,4-oxadiazol-5-yl optionally substituted at the 3-position by Z4 wherein any (C1-C6) alky, (C1-C6) alkanoyl, (C2-C6) alkenyl or (C2-C6) alkynyl can optionally be substituted by 1, 2 or 3 Z; R7 can be hydrogen, O or phenyl R8 can be hydrogen, phenyl, halophenyl, nitrophenyl, pyridyl, piperonyl or sulfoxonitrophenyl Z4 is (C1-C6) alkyl or phenyl, optionally substituted by 1, 2 or 3 Z1 W is O or S T is amino or C1-C6 aminoalkyl A is N or C T is C1-C6 alklyl or sulfonyl and V is alkyl (C0-C6), alkenyl, alkynyl, haloaryl, alkyl phenol, alkyl halophenyl, and R1 or R2 as indicated above and φ is phenyl, naphthyl, thienyl or pyridinyl.