An asymmetric three-component reaction of diazo compounds and alcohols with imines catalyzed cooperatively by a rhodium complex chiral Brønsted acid provides general efficient entry to β-amino-α-hydroxyl derivatives in high yields excellent stereoselectivities.

Sustained changes in blood flow modulate the size of conduit arteries through structural alterations vessel wall that are dependent on transient accumulation and activation perivascular macrophages. The leukocytic infiltrate appears to be confined adventitia, is responsible for medial remodeling, resolves once hemodynamic stresses have normalized without obvious intimal changes. We report inward remodeling mouse common carotid artery after ligation ipsilateral external chemokine receptor...

Abstract Metal-catalyzed enantioselective construction of the loosening axial allene chirality spreading over three carbon atoms using a chiral ligand is still significant challenge. In literature, steric effect substrates major strategy applied for such purpose. Herein, we present general palladium-catalyzed asymmetrization readily available racemic 2,3-allenylic carbonates with different types non-substituted and 2-substituted malonates ( R )-(−)-DTBM-SEGPHOS as preferred to afford...

Enantioselective four-component reactions of aryl diazoacetates with alcohols, aldehydes and amines catalyzed cooperatively by a rhodium complex chiral Brønsted acid produce beta-amino-alpha-hydroxyl derivatives in single step excellent control chemo-, diastereo- enantioselectivity.

A new one-pot electrophilic aminoalkoxylation reaction using olefin, cyclic ether, amine, and N-bromosuccinimide has been developed. The olefinic substrates the ether partners can be flexibly varied to produce a range of amino derivatives. This novel protocol applied in facile efficient synthesis biologically active morpholine compounds.

Abstract [IPrAuCl]/AgSbF 6 ‐catalyzed cyclization of the readily available 4‐benzoxyl‐1‐(indol‐2‐yl)‐2‐alkynols occurred smoothly in 1,2‐dichloroethane (DCE) presence 4 Å MS to form a series differently polysubstituted 2‐oxygenated carbazole derivatives efficiently. Based on mechanistic study, possible mechanism involving 1,3‐migration benzoate group allene, Au + ‐mediated cyclization–elimination gold–carbene intermediate, and subsequent highly selective 1,2‐migration has been proposed for...

Purpose Prefabricated building projects (PBPs) require multiple stakeholder collaboration due to the strong linkages between design, production and installment of precast components. Current contractual governance fails foster a trusting environment for collaboration, leading conflicts interest, cost overrun delays in project schedules. Previous studies revealed that terminating shortcomings can be mitigated by implementing relational mechanisms. This study aims explore configurational...

A novel cationic Br initiated one-pot imidazoline synthesis has been developed using olefin, nitrile, amine, and N-bromosuccinimide. The olefinic substrates the nitrile partners can be flexibly varied to achieve a range of derivatives.

Abstract Chiral molecules, which may contain one or more different type(s) of stereocentres, such as central, axial, planar, and helical chiralities, etc ., are indispensable in chemistry, pharmaceutical industry, life science. Despite many advances for the preparation chiral molecules usually with a single type chirality have been realized, simultaneous construction types chiralities is still significant challenge. Here, we wish to report protocol allenes both central axial via catalytic...

A novel N-bromosuccinimide induced aminocyclization–aziridine ring expansion cascade is reported. Substituted azepanes were isolated exclusively in good yields. The azepane products could be transformed into a number of functional molecules including piperidines, bicyclic amine, and bridgehead amide.

B-cell lymphoma 6 (BCL6) is a transcriptional repressor frequently deregulated in lymphoid malignancies. BCL6 engages with number of corepressors, and these protein–protein interactions are being explored as strategy for drug development. Here, we report the development an irreversible inhibitor TMX-2164 that uses sulfonyl fluoride to covalently react hydroxyl group Tyrosine 58 located lateral groove. exhibits significantly improved inhibitory activity compared its reversible parental...

Abstract γ-( E )-Vinylic and γ-alkylic γ-butyrolactones are two different types of lactones existing extensively in animals plants many them show interesting biological activities. Nature makes alkylic by enzymatic lactonization processes. Scientists have been mimicking the natural strategy developing new catalysts. However, direct efficient access to )-vinylic is still extremely limited. Here, we wish present our modular allene approach, which provides an asymmetric approach ( from allenoic...

An unexpected PtCl4-catalyzed cyclization reaction of tertiary indol-2-yl-3-alkynols occurred smoothly in toluene to form various poly-substituted carbazole derivatives efficiently. A possible mechanism involving the formation a spiro-tricyclic intermediate via indole C-2 attack, highly selective ring expansion and then 1,2-migration has been proposed for carbazoles.

Dual to the death: Catalyzed by [Rh2(OAc)4] and a chiral phosphoric acid, an enantioselective symmetric three-component reaction of diazo compounds with imines water is reported give β-amino-α-hydroxy acid derivatives in good yield (up 86 %) excellent diastereoselectivity 98:2 d.r.) enantioselectivity 97 % ee). Detailed facts importance specialist readers are published as "Supporting Information". Such documents peer-reviewed, but not copy-edited or typeset. They made available submitted...

Arteriosclerosis is characterized by the local activation of effector T cells leading to production proinflammatory cytokines, such as IFN (interferon)-γ and IL-17, within vessel wall. Conversely, antiinflammatory for example, TGF-β, regulatory lymphocytes known inhibit both differentiation naïve into development arteriosclerosis in murine models. We investigated role TGF-β on alloreactivity human memory (Tem). Quiescent vascular cells, but not Tem, expressed TGF-β. Blockade activity...

Pd-Catalyzed one-pot direct <italic>ortho</italic> C–H arylation of pyrrolo[2,3-<italic>d</italic>]pyrimidine derivatives is reported. This protocol provides a variety biphenyl-containing pyrrolo[2,3-<italic>d</italic>]pyrimidines in good to excellent yields.

A highly switchable,diastereoselectivity-controlled, three-component reaction of aryldiazoacetate, alcohol,and β,γ-unsaturated α-keto esters has been achieved through a dual-metal cooperative catalysis strategy.

An efficient aziridine ring expansion cascade of cinnamylaziridine has been developed. N-Bromosuccinimide was used as the promoter. The resulting functionalized pyrrolidines are fundamental units many useful molecules.

A simple and efficient method for the synthesis of 1,4-dihydroarenes by gold-catalyzed 6-endo cyclization benzylic allenes has been developed. Furthermore, asymmetric hydroarylation enantioenriched realized to offer a practical convergent approach aromatic ring-fused six-membered cycles containing chiral stereocenter such as 1,4-dihydronaphthalenes, 1,4-dihydrodibenzo[b,d]thiophenes, 4,7-dihydrobenzo[b]thiophenes applying dinuclear [(dppm)Au2 Cl2 ] [dppm=methylenebis(diphenylphosphane)]...

A unique TfOH-catalyzed domino cycloisomerization/hydrolytic defluorination reaction of easily available<italic>n</italic>-perfluoroalkyl allenones in the presence H₂O providing furanyl perfluoroalkyl ketones has been developed.

S was successfully doped into carbon via calcination and Pd size modulated by adjusting the content. Sulfur species were considered to be anchor sites, contributing highly dispersion of nanoparticles. In addition, Pd/CS4 achieved 99.9% sel. With complete conversion in hydrogenation o-chloronitrobenzene compared Pd/AC (99.9% con., 61.6% sel.). Interestingly, catalysts with smaller metal exhibited higher selectivity lower activity, which contrary previous studies. It suggested that electronic...

Transition-metal-free catalyzed direct C(sp²)–H acetoxylation of pyrrolo[2,3-<italic>d</italic>]pyrimidine derivatives is reported. This protocol provides a variety acetoxylated pyrrolo[2,3-<italic>d</italic>]pyrimidines in good to excellent yields.