Selective defluorinative functionalization of trifluoromethyl group (-CF3) is an attractive synthetic route to the pharmaceutically privileged fluorine-containing moiety. Herein, we report a strategy based on photoexcited copper catalysis activate C-F bond di- or trifluoromethylated arenes for divergent radical C-N coupling with carbazoles and aromatic amines. The use different ligands can tune reaction products diversity. A range substituted, structurally diverse α,α-difluoromethylamines be...

A highly efficient, catalyst-free synthesis of polysubstituted pyrroles by means a novel four-component domino reaction an arylglyoxal monohydrate, aniline, dialkyl but-2-ynedioate, and malononitrile is reported. This transformation proceeded via 6,6a-dihydrofuro[2,3-b]pyrrole as the key intermediate.

An efficient domino approach for the synthesis of novel pyrrolo[2,3,4-kl]acridin-1-one derivatives has been established. This reaction represents first facile conversion an isatin to a via C–N bond cleavage without need multistep process.

Herein, N-nucleophilic tandem oxidation–N-arylation–oxidation reaction and C-nucleophilic bromination of substituted anilines have been developed using chiral phosphoric acid catalysis, enabling access to axially diarylamines. The key feature this strategy is that the "NO2···H–N" hydrogen bond was successfully introduced into acyclic diaryl secondary amines, which contain two potential contiguous atropisomeric C–N axes, stabilize one planar axial conformations. This methodology provided a...

A catalyst-controlled diastereodivergence is described for the enantioselective conjugate addition of o-hydroxyphenyl-substituted p-QMs with 5H-thiazol-4-ones. The reactions were enabled by two chiral complementary, nonenantiomeric catalysts to furnish a series adducts possessing vicinal sulfur-functionalized quaternary and tertiary stereocenters in high yields excellent asymmetric induction. Moreover, o-QMs generated situ from o-hydroxybenzyl alcohols also compatible.

Comprehensive Summary Phthalides serve as core structures pervasive in a wide array of natural products and drug molecules, which display diverse biological activities. We report herein highly efficient dynamic kinetic resolution 3‐hydroxyphthalides by chiral isothioureas (ITUs) catalyzed asymmetric acylation, facilitating the effective synthesis variety phthalidyl esters with good yields enantioselectivities. Notably, this reaction features mild conditions, expansive substrate scope well...

A microwave-assisted regioselective synthesis of 3-functionalized indole derivatives via a three-component domino reaction anilines, arylglyoxal monohydrates, and cyclic 1,3-dicarbonyl compounds is described. The main advantages this protocol are short times, practical simplicity, its metal-free nature, the availability starting materials, green solvents, high regioselectivity.

Abstract The squaramide catalyzed enantioselective Michael addition of rhodanines to 2‐arylidene‐ N ‐tosylbenzofuran‐3(2 H )‐imines has been established, which enables the formation benzofurans bearing both rhodanine and sulfur‐containing tetrasubstituted stereocenter structural motif in good high yields with excellent enantio‐ diastereoselectivities. magnified image

The silica gel-catalyzed synthesis of 5-amino-2-aryl-3H-chromeno[4,3,2-de][1,6]naphthyridine-4-carbonitriles and 5-amino-2-aryl-3H-quinolino[4,3,2-de][1,6]naphthyridine-4-carbonitriles were simply achieved upon the one-pot cascade reaction malononitrile with substituted 2-hydroxyacetophenone (or 2-aminoacetophenone) aromatic aldehyde in aqueous media. mechanistic investigation results based on electrospray ionization mass spectrometry (ESI-MS) indicated that displayed a dual role during this...

A series of novel polyfunctionalized pyrido[2,3-b]indoles were synthesized by three- or four-component domino reactions under microwave irradiation. This protocol has the advantages readily available starting materials, short reaction times, high yields, easy workup, and chemo- regioselectivities.

The diastereoselective and enantioselective direct vinylogous Michael addition of γ-substituted β,γ-unsaturated γ-lactones to 2-arylidene-<italic>N</italic>-tosylbenzofuran-3(2<italic>H</italic>)-imines has been achieved with the aid a quinine-derived squaramide.

A facile and efficient one-pot procedure for the preparation of functionalized benzo[b][1,8]naphthyridine derivatives by three-component reaction 2-chloroquinoline-3-carbaldehyde, 1,3-dicarbonyl compounds, enaminones catalyzed l-proline is described. This new protocol has advantages environmental friendliness, good yields, convenient operation.

Abstract Herein, visible‐light‐induced metal‐free three‐component amidoheteroarylation of alkenes with quinoxalin‐2(1 H )‐ones and N‐sulfonylaminopyridinium salts is developed. This protocol involves a radical relay process in which the N‐centered radicals undergo chemoselective addition to form an alkyl that selectively combines heteroarenes, leading formation C−C C−N bonds one step under mild reaction conditions. The involved high efficiency selectivity, wide substrate scope, excellent...

Abstract N2-Methyl- or aryl-substituted 2-amino-4-aryl-5,6,7,8-tetrahydroquinoline-3-carbonitriles were synthesized via a four-component, one-pot reaction of aromatic aldehyde, cyclohexanone, malononitrile, and amines in basic ionic liquid [bmim]OH with good to excellent yields. During this transformation, at least 11 bonds cleaved 7 new constructed.

A series of new octahydrobenzo[b]indeno[1,2,3-de][1,8] naphthyridine and decahydropyrido[2,3,4-gh]phenanthridine derivatives were synthesized via a four-component domino reaction under microwave irradiation. This one-pot transformation, which involved multiple steps did not require the use catalyst, constructed four C–C bonds, two C–N three rings, with efficient all reactants.

A series of 3'-aminospiro[indoline-3,1'-pyrazolo[1,2-b]phthalazine]-2,5',10'-trione derivatives have been synthesized by a one-pot three-component reaction isatin, malononitrile or ethyl cyanoacetate and phthalhydrazide catalyzed piperidine under ultrasound irradiation. For comparison the reactions were carried out both conventional ultrasonic conditions. In general, improvement in rates yields observed when sonication compared with classical

Substantial interstudy heterogeneity exists in defining acute kidney injury (AKI) and baseline serum creatinine (SCr). This study assessed AKI incidence its association with pediatric intensive care unit (PICU) mortality under different SCr definitions to determine the preferable approach for diagnosing AKI.In this multicenter prospective observational cohort study, was defined staged according Kidney Disease: Improving Global Outcome (KDIGO), modified KDIGO, reference change value optimized...

A series of novel dispirooxindoles have been synthesized through three-component 1,3-dipolar cycloaddition azomethine ylides generated in situ by the decarboxylative condensation isatin and an α-amino acid with dipolarophile 5-benzylidene-1,3-dimethylpyrimidine-2,4,6-trione. This method has advantages mild reaction conditions, high atom economy, excellent yields, regio- stereo-selectivity.

An efficient one-pot synthesis of 1,6-diamino-2-oxo-1,2,3,4-tetrahydro- pyridine-3,5-dicarbonitrile derivatives by four-component piperidine-catalyzed reactions a ketone, malononitrile, ethyl cyanoacetate and hydrazine hydrate under ultrasound irradiation is described. This method provides several advantages such as shorter reaction times, excellent yields, simple workup procedure.

An improved synthesis of multifunctionalized pyrrolo[2,3,4-kl]acridine derivatives with different substituted patterns using silica sulfuric acid (SSA) as a heterogeneous catalyst under microwave irradiation conditions was developed. The reaction could be conducted by readily available and inexpensive substrates within short periods 12–15 min. irradiation. Compared the conventional methods, remarkable advantages this method are milder conditions, operational simplicity, higher yields, times,...

α,α′-Bis(substituted-benzylidene)cycloalkanones were synthesized via a solvent-free cross-aldol condensation of aromatic aldehydes with cycloalkanones in the presence catalytic amount 1-methyl-3(2-(sulfooxy)ethyl)-1H-imidazol-3-ium chloride at room temperature excellent yields. The screening for optical properties indicated that size cycloalkanone has an influence on fluorescence emission products. Products coming from cyclohexanone have stronger than those cyclopentanone.

A series of chromeno[4,3‐ d ]pyrazolo[3,4‐ b ]pyridin‐6(3 H )‐one derivatives was easily and efficiently synthesized by the reaction 2 ‐chromen‐2‐ones with pyrazol‐5‐amines catalyzed CuCl ⋅2H O in ethanol. This protocol has advantages mild conditions, easy work‐up, high yields. These compounds were showed to have fluorescence quantum yields, which mentioned their value as luminescence or probe.

A concise and efficient route to new interesting heterohelicene-like molecules has been developed through the one-pot, cascade reductive coupling reaction of o-hydroxydiimines or o-nitrodiimines triphosgene in presence TiCl4/Sm. Purification final products only required a single recrystallization leading high purity. High diastereoselectivity was also achieved, two structures were confirmed by X-ray diffraction analysis.