Mechanochemical Single-Carbon Insertion into (Iso)quinolines [PDF]
(Iso)quinolines are among the most common heterocycles in US Food and Drug Administration approved drugs, whereas benzoazepines are underrepresented in drug discovery libraries, primarily because of the lack of efficient preparation routes. Therefore, an
Chunxiu Jing +6 more
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Two mutually complementary synthetic approaches towards 3-substituted 3,4-disubstituted and 1-(2-pyridyl)-substituted isoquinolines [PDF]
Two mutually complementary synthetic approaches towards 3- and 3,4-disubstituted 1-(2-pyridyl) isoquinolines were studied. The aryne-based method was successfully used for the obtaining of the corresponding the 3-cyano-1-(2-pyridyl)isoquinolines in one ...
I. L. Nikonov +10 more
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Rh(III)-catalyzed chelation-assisted C–H activation/annulation of 2-arylimidazolines with cyclic diazo-1,3-dicarbonyl compounds: a novel approach to tetracyclic annulated derivatives of 2,3-dihydroimidazo[2,1-a]isoquinoline [PDF]
2-Arylimidazolines were annulated with cyclic diazo-1,3-dicarbonyl compounds under Rh(III)-catalysis for the first time. The developed general and efficient approach based on CH-activation allowed the efficient preparation of five novel types of ...
Ivan Lyutin +3 more
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Synthesis of 1H-Pyrrolo[3,2-g]isoquinoline Derivatives as Ligands Targeting Haspin Kinase [PDF]
A new series of 1H-pyrrolo[3,2-g]isoquinolines, diversely substituted at the 3-position either by a heteroaromatic scaffold or by propionate/acrylate side chains, were synthesized and evaluated as Haspin kinase inhibitors.
Killian Malosse +5 more
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Photoredox catalytic asymmetric dearomative [3 + 2] cycloaddition of isoquinolines with enones [PDF]
Asymmetric dearomative photocycloaddition has emerged as a transformative strategy for the enantioselective construction of complex three-dimensional molecular architectures from simple planar aromatic precursors. While significant progress has been made
Jingjing Huo +5 more
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Photoinduced polarity-mismatched transformations of isoquinolines into naphthalenes [PDF]
Isosteric replacement is an important strategy for lead optimization in drug-development paradigms. However, it is usually restricted to cost- and labor-intensive de novo syntheses.
Congcong Zhang +6 more
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Studies concerning bridged isoquinolines and related compounds
This report describes studies concerning bridged isoquinolines and related compounds, Four aspects have been studied, Firstly, Diels-Alder reactions between heterarynes and different dienes have been carried out to provide 5,8-bridged isoquinolines.
Angela S. Mallard (7166759)
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C-1 Substituted isoquinolines potentiate the antimycobacterial activity of rifampicin and ethambutol
IntroductionThe emergence of extensively drug-resistant strains of Mycobacterium tuberculosis threatens decades of progress in the treatment of a disease which remains one of the leading infectious causes of death worldwide.
Liam T. Martin +9 more
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A variety of thieno[3,2-f]isoquinolines were prepared by combination of Pd catalysed cross-coupling reactions with Brønsted acid mediated cycloisomerisations. The reactions tolerate various functional groups and proceed with high selectivity. In addition,
Maria Ines Mangione +11 more
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An innovative and efficient approach has been developed for the synthesis of 5,6-dihydropyrazolo[5,1-a]isoquinolines. This one-pot tandem reaction involves the reaction of C,N-cyclic azomethine imines with α,β-unsaturated ketones, using K2CO3 as the base
Young Jae Yun, Sung-Gon Kim
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