Copper(I)-Catalyzed Cross-Coupling of 1-Bromoalkynes with N-Heterocyclic Organozinc Reagents
Nitrogen-containing heterocycles represent the majority of FDA-approved small-molecule pharmaceuticals. Herein, we describe a synthetic method to produce saturated N-heterocyclic drug scaffolds with an internal alkyne for elaboration.
Christian Frabitore +2 more
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In the category of drugs approved by the U.S. FDA, pyrrolidine is the most frequently used core of five-membered nonaromatic heterocycles containing nitrogen.
Maocheng Tang +5 more
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Catalytic Asymmetric C-N Bond Formation: Phosphine-Catalyzed Intra- and Intermolecular γ-Addition of Nitrogen Nucleophiles to Allenoates and Alkynoates [PDF]
Pin the amine on the gamma: A new method has been developed for the γ-addition of nitrogen nucleophiles to γ-substituted alkynoates or allenoates through intra- and intermolecular processes that are catalyzed by spirophosphine 1 (see scheme).
Chung, Ying Kit +5 more
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Methodology-driven efficient synthesis of cytotoxic (±)-piperarborenine B
The evolution of synthetic design toward the efficient synthesis of cyclobutane natural product (±)-piperarborenine B is demonstrated. Taking the advantages of good functional group compatibility of contractive synthesis of cyclobutanes from pyrrolidines,
Chunngai Hui, Andrey P. Antonchick
doaj +1 more source
A general protocol to afford enantioenriched linear homoprenylic amines [PDF]
The reaction of a readily obtained chiral branched homoprenylamonium salt with a range of aldehydes, including aliphatic substrates, affords the corresponding linear isomers in good yields and enantioselectivities.We thank the Spanish Ministerio de ...
Bosque, Irene +2 more
core +2 more sources
In‐situ‐Konstruktion von Imidazopyridinium‐Fluoreszenzlabels für Biokonjugationen
Durch Chromophor‐Engineering von Isochinolinaldehyden entstehen TICT‐basierte fluorogene Farbstoffe für die In Situ Markierung unterschiedlicher (Bio‐)Moleküle mit großen Stokes‐Verschiebungen, die mit der Zellbildgebung kompatibel sind. ZUSAMMENFASSUNG Einfache, effiziente Transformationen fluorogenen Charakters, die unter biokompatiblen Bedingungen ...
Dongchen Du +7 more
wiley +1 more source
Evaluating New Chemistry to Drive Molecular Discovery: Fit for Purpose? [PDF]
As our understanding of the impact of specific molecular properties on applications in discovery-based disciplines improves, the extent to which published synthetic methods meet (or do not meet) desirable criteria is ever clearer. Herein, we show how the
Atack +63 more
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Three-Component Synthesis of Polysubstituted Homoproline Analogs
Tetrasubstituted pyrrolidines representing analogs of homoproline weresynthesized by three-component condensation of aryl(heteroaryl)aldehydes, asparagineand N-methylmaleimide (NMM). Compounds with (1S*, 3R*, 3aS*, 6aR*)-configurationat the corresponding
V. Irkha, K. Kudryavtsev
doaj +1 more source
A Stepwise [4 + 3] Cycloaddition Reaction of the 1,3-Diphenyl-2-azaallyl Anion [PDF]
The 1,3-diphenyl-2-azaallyl anion (1) undergoes [3 + 2] cycloaddition reactions with the s-cis-fixed 1,3-dienes 8-11. In contrast, 1,1,2,2,3,3-hexamethyl-4,5-bis(methylene)cyclopentane (7) reacts with 1 to give the [4 + 3] cycloadduct 13 and the linear 1,
Anh +23 more
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Carbohydrate-auxiliary assisted preparation of enantiopure 1,2-oxazine derivatives and aminopolyols
An approach to enantiopure hydroxylated 2H-1,2-oxazine derivatives is presented utilizing the [3 + 3] cyclisation of lithiated alkoxyallenes and an L-erythrose-derived N-glycosyl nitrone as precursors.
Marcin Jasiński +2 more
doaj +1 more source

