A concise and efficient route for the synthesis of highly substituted imidazopyrroloquinoline derivatives by simply refluxing a reaction mixture different types isatins heterocyclic ketene aminals (HKAs) acetic acid was developed. This method is suitable combinatorial parallel syntheses in drug discovery; consequently, library rapidly constructed using present protocol.

A novel Rh(III)-catalyzed cascade alkenyl C-H activation/[3 + 2] annulation/pinacol rearrangement reaction of enaminones with iodonium ylides has been developed. This methodology provides a new and straightforward synthetic strategy to afford highly functionalized 2-spirocyclo-pyrrol-3-ones in satisfactory yield from readily available starting materials under mild conditions. Moreover, gram-scale reactions further derivatization experiments are implemented demonstrate the potential utility...

A cascade oxidative annulation reaction of heterocyclic ketene aminals (HKAs) with internal alkynes catalyzed by [Cp*RhCl2]2 and oxidized Cu(OAc)2·H2O was developed to efficiently synthesize highly functionalized benzo[de]chromene derivatives in good excellent yields. The proceeded the sequential cleavage C(sp2)-H/O-H C(sp2)-H/C(sp2)-H bonds. These multicomponent reactions were regioselective. In addition, all products exhibited intense fluorescence emission solid state, they demonstrated...

An unprecedented selective chromone annulation reaction controlled by solvent for the divergent synthesis of two types 2,3-disubstituted skeletons has been developed. A variety 2-chromonyl-3-hydrazono-chromones and 2-alkoxy-3-hydrazono-chromones were constructed efficiently from readily available

A one-step methodology for the synthesis of multisubstituted quinoline-4-carboxamides was developed by simply refluxing a mixture isatins 1 and various kinds 1,1-enediamines 2–4 in reaction catalyzed NH2SO3H. As result, series quinolone-4-carboxamides were produced through novel cascade mechanism. This involved formation quinoline ring accompanied an amide bond one step. Accordingly, this protocol is suitable combinatorial parallel syntheses quinolone-4-carboxamide drugs or natural products.

An efficient one-pot, three-component synthesis of highly substituted bicyclic pyridines containing a ring-junction nitrogen, starting from simple and readily available materials, is described. Cyclocondensation heterocyclic ketene aminals (HKAs), triethoxymethane, active methylene compounds by refluxing under solvent-free catalyst-free conditions, provided in excellent yields.

The first site-selective methodology for the construction of fused [1,2-<italic>a</italic>]indolone derivatives<italic>via</italic>an unexpected anti-Nenitzescu strategy has been developed.

Abstract The C( sp 2 )−H phosphorothiolation involving cyclization process through a transition‐metal‐free strategy is reported. It provides an attractive approach for the construction valuable S ‐3‐chromon phosphorothioates from o ‐hydroxyarylenaminones and P(O)SH compounds in presence of 1.0 equiv. iodine at 60 °C. This novel protocol shows readily available chemicals, broad substrate scope, mild reaction conditions. magnified image

Pyroptosis represents a mode of programmed necrotic cell death (PCD), mediated by members gasdermin family (GSDMs), such as GSDME. It is emerging promising approach for combating cancer. Notably, GSDME the key modulator switch between apoptosis and pyroptosis in cells. However, often downregulated many malignancies, including lung adenocarcinoma. To identify novel inducers non-small cancer (NSCLC) dissect underlying mechanism. was examined live imaging, PI/Hoechst/Annexin V staining, LDH...

The substitution-cyclization reaction of heterocyclic ketene aminals with polyhalo isophthalonitrile in the presence t-BuOK to form 1,3-diazaheterocycle fused [1,2-b]isoquinolin-1(2H)-imines, followed by hydrolysis 1 N HCl, provides a concise and efficient route for synthesis highly functional [1,2-b]isoquinolin-1(2H)-ones.

Abstract A simple, straightforward and versatile multicomponent protocol for the synthesis of indanone‐fused spirooxindole derivatives has been developed. The strategy involves one‐pot three‐component reaction heterocyclic ketene aminals, 1 H ‐indene‐1,3(2 )‐dione dicarbonyl compounds isatins or acenaphthenequinone in an ethanol/water medium catalysed by p ‐TSA at reflux. Mild conditions, operational simplicity, wide substrate scope overall excellent yields make this method highly efficient...

Aromatic sulfonyl halides are readily accessible from many sources. With newly synthesized N-arylphenothiazine catalysts, organocatalyzed photoredox polymerization has been developed with arylsulfonyl initiators using white or purple LEDs light This method allows the preparation of poly(meth)acrylates and poly(meth)acrylamides possessing a broad scope (hetero)aryl chain ends without metal-contamination concern. Investigations such as MALDI-TOF analysis, extension, "ON/OFF" control...

A three-component catalyst-free protocol for the regioselective synthesis of dual highly functionalized fused pyrroles has been developed from a cascade [3 + 2] cyclization heterocyclic ketene aminals (HKAs) 1 with arylglyoxal monohydrates 2 and cyclohexane-1,3-diones 3 in water–ethanol media. The kinetically controlled products 4 could be synthesized within h but would irreversibly transform to thermodynamically 5 over an additional h. At same time, transformative 5a 4a by controlling...

A direct Csp3-H bond oxidative thioesterification of methyl ketones with aromatic thiols/disulfides promoted by TBAI/K2S2O8 has been developed. The reaction provides successfully a simple and efficient method for the synthesis functionalized α-ketothioesters thiols. This practical methodology exhibits readily available starting materials, large-scale applicability, synthetic application, broad functional group tolerance. possible mechanism transformation is proposed.

An efficient and concise one-pot procedure was developed based on a cascade reaction of 3-formylchromones 1 different types 1,1-enediamines (EDAMs) 2 with alcohols or amines 3 by site-selective synthesis 5H-chromeno[4,3-b]pyridines in an environmentally friendly solvent. This protocol is especially suitable for the rapid parallel 5H-chromeno[4,3-b]pyridine compounds. It also has some advantages, such as convenience operation, short times, use green solvent, ease purification washing crude...

A novel protocol for the preparation of functionalized 9-azabicyclo[3.3.1]nonane (ABCN) derivatives from 3-formylchromones, enaminones, and heterocyclic ketene aminals (HKAs) through an unprecedented cascade reaction has been developed by simply refluxing mixture substrates 1–3. As a result, series ABCNs were produced very complex reaction. This can be used in synthesis that are suitable combinatorial parallel syntheses ABCN natural-like products one-pot

A novel protocol was developed for the construction of highly functionalized 2-(diarylphosphoryl)-1,2-dihydropyridine derivatives (DAPDHPs) from 3-formylchromones (1), heterocyclic ketene aminals (HKAs, 2), and phosphine oxides (R2P(O)H, 3) via a novel, one-pot cascade reaction. Optimization reaction conditions determined that refluxing mixture 3-formylchromones, HKAs, various R2P(O)H in propylene carbonate (PC) presence triethylamine as base facilitated highest yields DAPDHP products. This...

This method involves a cascade reaction utilizing 1 and enamines 2 as substrates, which occurred by refluxing mixture of the starting materials in toluene with catalyst Fe(OTf) 3 .

The inclusion complexation behavior, characterization, and binding ability of nimbin with β-cyclodextrin (β-CD) its derivatives were investigated in both solution the solid state by means XRD, DSC, 1H 2D NMR, UV−vis spectroscopy. results showed that water solubility thermal stability obviously increased complex cyclodextrins. This satisfactory high nimbin/CD complexes will be potentially useful for their application as herbal medicines or healthcare products.

A concise and eco-friendly route for the synthesis of highly functionalized bicyclic pyridinium derivatives (3) via a one-pot reaction chromone-3-carboxaldehydes (1) N-benzyl nitro ketene aminals (NBNKAs) (2) under reflux in ethanol media has been developed. The targeted compound was efficiently obtained by filtration without further post-treatment. In two step reaction, C—C C═N bonds were constructed, while at same time one C—O bond cleaved. This protocol represents valuable to obtain...

A novel approach has been constructed for the synthesis of two types 2-amino-4-coumarinyl-5-arylpyrroles (ACAPs, 5 and 6) through a cascade reaction metal-free catalyzed aerobic oxidation arylglyoxal monohydrates 1, 1,1-enediamines (EDAMs) 2 3, 4-hydroxy-2H-chromen-2-ones 4 via multicomponent reactions to produce target compounds with good excellent yields. Specifically, hydroxyl-substituted 2-amino-4-coumarinyl-5-arylpyrroles, that is, 2-amino-4-coumarinyl-5-aryl-6-hydroxylpyrroles (ACAHPs)...