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Open AccessAuthor Correction: Catalytic enantioselective reductive alkynylation of amides enables one-pot syntheses of pyrrolidine, piperidine and indolizidine alkaloids
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Open AccessCatalytic enantioselective reductive alkynylation of amides enables one-pot syntheses of pyrrolidine, piperidine and indolizidine alkaloids
The primary objective in synthetic organic chemistry is to develop highly efficient, selective, and versatile synthetic methodologies, which are essential for discovering new drug candidates and agrochemicals....
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Article
Iridium and B(C6F5)3 co-catalyzed chemoselective deoxygenative reduction of tertiary amides: application to the efficient synthesis and late-stage modification of pharmaceuticals
The Vaska’s complex—tris(pentafluorophenyl)borane combination was found to be a highly efficient cooperative catalysis system for the hydrosilylative reduction of tertiary amides to yield amines under mild con...
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Article
Open AccessEnantioselective total syntheses of (+)-stemofoline and three congeners based on a biogenetic hypothesis
The powerful insecticidal and multi-drug-resistance-reversing activities displayed by the stemofoline group of alkaloids render them promising lead structures for further development as commercial agents in ag...
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Catalytic diastereoselective and enantioconvergent C(sp3)—C(sp3) cross-coupling of racemic partners
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Ni-catalyzed direct alcoholysis of N-acylpyrrole-type tertiary amides under mild conditions
N-Acylpyrrole-type amides are a class of versatile building blocks in asymmetric synthesis. We report that by employing Ni(COD)2/2,2′-bipyridine (5 mol%) catalytic system, the direct, catalytic alcoholysis of N-a...
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Article
Amides as surrogates of aldehydes for C-C bond formation: amide-based direct Knoevenagel-type condensation reaction and related reactions
Aldehydes are perhaps the most versatile compounds that enable many C-C bond forming reactions, which are not amenable for other subclasses of carbonyl compounds. We report the first use of amides as surrogate...
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Article
Metal-free synthesis of quinolines by direct condensation of amides with alkynes: revelation of N-aryl nitrilium intermediates by 2D NMR techniques
Employing triflic anhydride/2-fluoropyridine as an activation system, the coupling reactions of secondary N-aryl amides with terminal alkynes yielded substituted quinolines in moderate to excellent yields. The re...
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Open AccessDual catalysis for enantioselective convergent synthesis of enantiopure vicinal amino alcohols
Enantiopure vicinal amino alcohols and derivatives are essential structural motifs in natural products and pharmaceutically active molecules, and serve as main chiral sources in asymmetric synthesis. Currently...
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Tf2O-TMDS combination for the direct reductive transformation of secondary amides to aldimines, aldehydes, and/or amines
The direct partial reduction of highly stable secondary amides to more reactive aldimines and aldehydes is a challenging yet highly demanding transformation. In this context, only three methods have been repor...
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Open AccessMetal-Free C–H Alkyliminylation and Acylation of Alkenes with Secondary Amides
Carbon–carbon bond formation by metal-free cross-coupling of two reactants with low reactivity represents a challenge in organic synthesis. Secondary amides and alkenes are two classes of bench-stable compound...
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Article
Impeding the interaction between Nur77 and p38 reduces LPS-induced inflammation
The orphan nuclear receptor Nur77 blocks inflammation through inhibition of p65 DNA binding and is suppressed by p38α-mediated phosphorylation. A small-molecule compound, PDNPA, disrupts p38α-Nur77 interaction...
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The first enantioselective total synthesis of (+)-preussin B and an improved synthesis of (+)-preussin by step-economical methods
The first enantioselective total synthesis of (+)-preussin B and an improved synthesis of the antifungal alkaloid (+)-preussin are described. Our approach relied on the four step-economical synthetic methods d...
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Article
Orphan nuclear receptor TR3 acts in autophagic cell death via mitochondrial signaling pathway
TR3 is an orphan nuclear receptor with roles in apoptosis. A TR3-binding compound induces mitochondrial translocation of TR3 and autophagy via the Nix–Toms–ANT1/VDAC1 pathway, providing a mechanism for cell de...
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The orphan nuclear receptor Nur77 regulates LKB1 localization and activates AMPK
A small molecule that disrupts interaction between Nur77 and LKB1 leads to LKB1 exit from the nucleus to activate cytoplasmic AMPK and, ultimately, reduces blood glucose and insulin in diabetic mice. ...
