6954-28-5Relevant academic research and scientific papers
Synthesis of pyrido[1,2- a ]indole malonates and amines through aryne annulation
Rogness, Donald C.,Markina, Nataliya A.,Waldo, Jesse P.,Larock, Richard C.
experimental part, p. 2743 - 2755 (2012/05/05)
Pyrido[1,2-a]indoles are known as medicinally and pharmaceutically important compounds, but there is a lack of efficient methods for their synthesis. We report a convenient and efficient route to these privileged structures starting from easily accessible 2-substituted pyridines and aryne precursors. A small library of compounds has been synthesized utilizing the developed method, affording variously substituted pyrido[1,2-a]indoles in moderate to good yields.
Studies on cerebral protective agents. I. Novel 4-arylpyrimidine derivatives with anti-anoxic and anti-lipid peroxidation activities
Kuno,Sugiyama,Katsuta,Kamitani,Takasugi
, p. 1452 - 1461 (2007/10/02)
Novel 4-arylpyrimidine derivatives were synthesized by the oxidation of 4-aryl-1,4-dihydropyrimidines, and their effects on anti-anoxic (AA) activity in mice and anti-lipid peroxidation (ALP) activity in rat brain mitochondria were investigated. Among these compounds, ethyl 6-methyl-2-phenyl-4-(4-pyridyl)-5-pyrimidinecarboxylate (4b) has AA activity (10mg/kg, i.p.) and ethyl 6-methyl-4-(3-nitrophenyl)-2-phenyl-5-pyrimidinecarboxylate (4f) has ALP activity (73% inhibition at 10-5 g/ml). The latter compound (100mg/kg, i.p.) was also effective on arachidonate-induced cerebral edema in rats with comparable potency to that of vitamin E.
ENANTIOSELECTIVE HANTZSCH DIHYDROPYRIDINE SYNTHESIS VIA METALATED CHIRAL ALKYL ACETOACETATE HYDRAZONES
Enders, Dieter,Mueller, Stephan,Demir, Ayhan S.
, p. 6437 - 6440 (2007/10/02)
An efficient, overall enantioselective variant of the Hantzsch synthesis of 4-aryl-1,4-dihydropyridines 5 (ee = 84 - 98percent), important biologically active compounds (e. g. as calcium channel blockers), is described.Key step of the new procedure is the
