A new ring for your indole: An unprecedented copper-catalyzed enantioselective Friedel–Crafts alkylation/N-hemiacetalization cascade reaction with indoles and β,γ-unsaturated α-ketoesters is reported. This mild strategy provides access to various synthetically biologically important 2,3-dihydro-1H-pyrrolo[1,2-a]indoles in a highly manner. As service our authors readers, this journal supporting information supplied by the authors. Such materials are peer reviewed may be re-organized online...

Batting the ylides: A simple procedure carried out under mild conditions allows direct and efficient synthesis of structurally diverse indoles. This approach involves a cascade reaction sulfur ylides N-(ortho-chloromethyl)aryl amides (see scheme). Detailed facts importance to specialist readers are published as "Supporting Information". Such documents peer-reviewed, but not copy-edited or typeset. They made available submitted by authors. Please note: The publisher is responsible for content...

Simply complex: Diverse and structurally complex chroman derivatives with a quaternary stereocenter have been obtained through the titled reaction of thiols nitroolefin enoates using bifunctional catalyst 1. The features simple experimental procedures, high yield, enantiomeric excess, excellent diastereoselectivity. Detailed facts importance to specialist readers are published as ”Supporting Information”. Such documents peer-reviewed, but not copy-edited or typeset. They made available...

An unprecedented Zn(OTf)2-catalyzed asymmetric Michael addition/cyclization cascade of 3-nitro-2H-chromenes with 3-isothiocyanato oxindoles has been disclosed. This transformation provides an efficient access to various synthetically important polycyclic spirooxindoles in a highly stereoselective manner under mild conditions (72–99% yields, up >95:5 d.r. and >99% ee). The reaction leads the formation three consecutive stereocenters, including 1,3-nonadjacent tetrasubstituted carbon single...

Get asymmetric! Asymmetric [4+1] annulation of sulfur ylides and N-(ortho-chloromethyl)aryl amides allowed the formation desired cycloadduct with moderate to high yields enantioselectivities (see scheme). The described strategy, taking advantage chiral ylides, represents a direct procedure access 2-substituted indolines.

Abstract A highly efficient and enantioselective intramolecular crossed Rauhut–Currier (RC) reaction of nitroolefins with tethered enonates has been developed through cooperative nucleophilic activation a hydrogen‐bonding catalytic strategy (≤98 % ee 98 yield). The features simple experimental procedures is completely chemoselective atom‐economic in character. potential synthetic applications have demonstrated by the conversion RC products into biologically pharmaceutically valuable...

Abstract A visible‐light‐induced cascade radical cyclization of aroyl chlorides with 2‐(allyloxy)‐benzaldehyde derivatives has been developed. The method takes advantages unactivated C=C bonds as the acyl acceptors and offers a mild green approach for synthesis 1,4‐diketones bearing biologically important chroman‐4‐one skeletons moderate to good yields.

The first example of a catalytic asymmetric formal [4+1] annulation reaction between sulfur ylides and in situ generated ortho ‐quinone methides ( o ‐QMs) is reported this work. A C 2‐symmetric chiral urea was identified to be the best H‐bonding catalyst, affording wide range 2,3‐dihydrobenzofurans high yields moderate enantioselectivities [70–98 % yields, up 89:11 e.r. (enantiomeric ratio)].

Abstract The gold‐catalyzed synthesis of methylidene 2,3‐cyclobutane‐indoles is documented through a combined experimental/computational investigation. Besides optimizing the racemic tricyclic indole compounds, enantioselective variant presented to its full extent. In particular, scope reaction encompasses both aryloxyallenes and allenamides as electrophilic partners providing high yields excellent stereochemical controls in desired cycloadducts. computational (DFT) investigation has fully...

Abstract A [4+2]‐cycloaddition of para ‐quinone methides with hexahydro‐1,3,5‐triazines is reported. The reaction occurs under very mild conditions (catalyst‐, ligand‐, and base‐free), exhibits a broad substrate scope excellent functional group tolerance, affords series biologically important 1,3‐benzoxazine derivatives in good to yields. Moreover, the successful late‐stage functionalization pharmaceutically relevant compounds further renders approach valuable. magnified image

Abstract This review summarizes the very recent advances in organocatalytic asymmetric cycloaddition reactions involving ortho ‐quinone methides ( o‐ QMs), a family of versatile species that have proven useful broad range to afford diverse chiral molecules. In past years, different kinds organocatalysts been developed into privileged class catalytic systems synthesis. A number remarkable achievements made by many groups around world. Due length limitation, this only those works published...

A highly enantioselective organocatalytic intermolecular conjugate addition of oximes to β-nitroacrylates has been developed. The functionalized adducts obtained are valuable precursors for asymmetric synthesis, as demonstrated by the synthesis β2,2-amino acids and oxazolidin-2-ones.

A formal [4 + 1]/[3 2] cycloaddition sequence of sulfur ylides and alkene-tethered nitroolefins has been developed. The use (R)-binol-derived chiral sulfide leads to an asymmetric process that allows the construction oxa- aza-angular triquinanes in good excellent diastereo- enantioselectivities.

Abstract A visible light‐induced, aerobic oxyamidation reaction of indoles, using air as the sole oxidant, has been developed. This process serves a photocatalytic strategy to generate efficiently tetrahydro‐5 H ‐indolo[2,3‐ b ]quinolinols, which may have interesting biological and pharmacological activities owing their privileged indoline structure.

An asymmetric synthesis of epoxyoxindoles from isatins has been developed by employing chiral sulfur ylides generated in situ camphor-derived sulfonium salts. This reaction allows an efficient access to enantioenriched spiro-epoxyoxindoles under mild conditions, featuring high yields and excellent enantio- diastereoselectivities.

Abstract Photocatalysis enables the cascade reactions of indoles and CBr 4 in MeOH through a C(sp 2 )H functionalization/methanolysis sequence. The title reaction provides an efficient access to indole 2‐ 3‐carboxylates single operation (no preinstallation protecting as well directing groups was required) with good yields under mild conditions.

Ein einfacher Prozess unter milden Bedingungen ermöglicht die direkte und effiziente Synthese von strukturell diversen Indolen. Der Ansatz umfasst eine Kaskadenreaktion Schwefelyliden N-(ortho-Chlormethyl)arylamiden (siehe Schema).

Ein neuer Ring für Indol: Eine neuartige Cu-katalysierte enantioselektive Kaskade aus Friedel-Crafts-Alkylierung und N-Halbacetalisierung setzt Indole mit β,γ-ungesättigten α-Ketoestern um. Diese milde Strategie eröffnet einen enantioselektiven Zugang zu präparativ biologisch wichtigen 2,3-Dihydro-1H-pyrrolo[1,2-a]indolen.

How pain emerges from cortical activities remains an unresolved question in neuroscience. A first step toward addressing this consists identifying brain that occur preferentially response to painful stimuli comparison non-painful stimuli. key confound has affected important many previous studies is the intensity of generating and sensations. Here, we compared activity during iso-intense tactile sensations sampled by functional MRI 51 healthy participants. Specifically, perceived was recorded...

Nociceptive and tactile information is processed in the somatosensory system via reciprocal (i.e., feedforward feedback) projections between thalamus, primary (S1) secondary (S2) cortices. The exact hierarchy of nociceptive processing within this 'thalamus-S1-S2' network whether differs two submodalities remains unclear. In particular, questions related to ascending descending pathways have not been addressed. For pathways, or parallel 'thalamus-S1' 'thalamus-S2') serial 'thalamus-S1-S2')...

The special electronic configuration of phosphorus atoms endows organophosphorus reagents with unique chemical properties, which enable them to be used catalyze various organic reactions, such as the Wittig reaction, Staudinger Appel reaction and Mitsunobu reaction. However, catalytic process will accompanied by generation large amounts phosphine oxide waste, resulting in reduction atom utilization it is difficult separate product. Therefore, essential explore a greener more sustainable...