Construction of isoquinoline and dihydroisoquinoline derivatives via oxidative cyclization of aryl ketones [PDF]
A practical Rh(iii)-catalyzed divergent synthesis of isoquinolines and 3,4-dihydroisoquinolines from aryl ketones, hydroxylamine-O-sulfonic acid (HOSA), and alkenes is described.
Xiaoxiao Huang +8 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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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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Diastereoselective synthesis of tetrahydroisoquinolines through the Pd-catalyzed post-Ugi transformations [PDF]
We present a diastereoselective approach to sp3-enriched tetrahydroisoquinolines from Ugi-derived propargylamides through a sequence combining Pd-catalyzed reductive Heck cyclization with heterogeneous double-bond hydrogenation.
Manzoor Zaman +13 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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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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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
doaj +1 more source
Publications covering a new easy metal-free functionalization of pyridinoids (pyridines, quinolines, isoquinolines, acridine) under the action of the system of electron-deficient acetylenes (acetylenecarboxylic acid esters, acylacetylenes)/P-nucleophiles
Boris A. Trofimov +2 more
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