erlyj2006
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[ASAP] Silver-Promoted (4 + 1) Annulation of Isocyanoacetates with Alkylpyridinium Salts: Divergent Regioselective Synthesis of 1,2-Disubstituted Indolizines
Photomediated ring contraction of saturated heterocycles
Saturated heterocycles are found in numerous therapeutics and bioactive natural products and are abundant in many medicinal and agrochemical compound libraries. To access new chemical space and function, many methods for functionalization on the periphery of these structures have been developed. Comparatively fewer methods are known for restructuring their core framework. Herein, we describe a visible light–mediated ring contraction of α-acylated saturated heterocycles. This unconventional transformation is orthogonal to traditional ring contractions, challenging the paradigm for diversification of heterocycles including piperidine, morpholine, thiane, tetrahydropyran, and tetrahydroisoquinoline derivatives. The success of this Norrish type II variant rests on reactivity differences between photoreactive ketone groups in specific chemical environments. This strategy was applied to late-stage remodeling of pharmaceutical derivatives, peptides, and sugars.
Asymmetric total synthesis of (+)-xestoquinone and (+)-adociaquinones A and B
DOI: 10.1039/D0SC07089K, Edge Article
The asymmetric total synthesis of (+)-xestoquinone and (+)-adociaquinones A and B was achieved in 6–7 steps using an easily accessible meso-cyclohexadienone derivative.
The content of this RSS Feed (c) The Royal Society of Chemistry
[ASAP] Copper-Catalyzed Functionalization of Aza-Aromatic Rings with Fluoroalcohols via Direct C(sp2)–H/C(sp3)–H Coupling Reactions
A general carbonyl alkylative amination for tertiary amine synthesis
Nature, Published online: 08 April 2020; doi:10.1038/s41586-020-2213-0
A general carbonyl alkylative amination for tertiary amine synthesisOrtho C–H arylation of arenes at room temperature using visible light ruthenium C–H activation
DOI: 10.1039/D0SC01289K, Edge Article
A ruthenium-catalyzed ortho C–H arylation process is described using visible light.
The content of this RSS Feed (c) The Royal Society of Chemistry
Electrochemical oxidative aminocarbonylation of terminal alkynes
Nature Catalysis, Published online: 06 April 2020; doi:10.1038/s41929-020-0443-z
Oxidative carbonylation using CO/O2 is an attractive strategy to construct carbonyl compounds, but the explosive limit of the gas mixture hampers its application. Now, this safety issue is overcome in the aminocarbonylation of alkynes by replacing the external oxidant O2 by electrochemistry facilitating a mild and safe reaction.