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ISSN: 2666-5549

The roles of computer-aided drug synthesis in drug development

With the improvements in computer computing ability, data accumulation and rapid algorithm development, the integration of artificial intelligence (AI) and drug synthesis has been accelerated, significantly...

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Electrochemical generation of nitrogen-centered radicals for organic synthesis

There is a resurgence of interests in organic electrochemistry, which is generally accepted as a green synthetic tool. In this context, many electrochemical methods have been developed in the past decade...

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Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization

C–H late-stage functionalization has gradually become a powerful approach for the rapid optimization of lead compounds’ bioactivity. Significant advances in this field have been achieved in the past...

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Copper-catalyzed 2,3-dihydro-1,2,4-triazoles synthesis through [3+2]-cycloaddition of nitrile ylides with azodicarboxylates

A copper-catalyzed three-component reaction of diazo compounds, nitriles, and azodicarboxylates to construct 2,3-dihydro-1,2,4-triazoles is reported. Key to the success is the utilization of azodicarboxylates...

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Radical azidation as a means of constructing C(sp3)-N3 bonds

The azido group is found in large numbers of natural products, drugs, biochemicals and materials and to date, many elegant and useful methods for the synthesis of organic azides and their transformations...

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Flow chemistry in the multi-step synthesis of natural products

The total synthesis of natural products is constantly facing many challenges derived from the complexed chemical structures, the lengthy synthetic routes, the time-consuming workup procedures and the...

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Recent advances in visible-light photoredox-catalyzed nitrogen radical cyclization

Visible-light photoredox catalysis is a powerful and attractive strategy for organic molecule activation and new reaction design owing to its environmental-friendly characteristics and unique catalytic...

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Transition-metal-catalyzed aromatic C–H functionalization assisted by the phosphorus-containing directing groups

Transition-metal-catalyzed C–H bond functionalization has attracted tremendous attention as an increasingly important protocol for the construction of C–C and C–X bonds. In particular, C–H bond functionalization...

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Asymmetric catalytic hydrogenation of imines and enamines in natural product synthesis

Asymmetric catalytic hydrogenations of imines and enamines with chiral transition-metal complexes bearing chiral ligands are among the most green and powerful approaches for the elaboration of chiral...

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Recent advances in the syntheses of pyrroles

The pyrrole moiety is an important structural motif in functional materials, natural products, and pharmaceuticals. More and more synthetic strategies toward pyrroles have emerged, where various efficient...

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Construction of axially chiral compounds via catalytic asymmetric radical reaction

The chemistry of axially chiral compounds has emerged as a subject of increasing interest due to their widespread presence in natural products, bioactive molecules, advanced materials, and chiral ligands/catalysts....

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Stereoselective construction of atropisomers featuring a C–N chiral axis

Atropisomeric C–N compounds belong to an important class of axially chiral compounds. However, whereas the asymmetric synthesis of biaryl atropisomers have been well established, general and efficient...

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Synthesis of indoles, indolines, and carbazoles via palladium-catalyzed C–H activation

The construction of indole, indoline and carbazole heterocycles has been of significant interest in the synthetic community over the last century due to their prevalence in natural products and other...

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Perspectives on green synthesis and catalysis

Despite their impressive capacity to access diverse functional groups and to synthesize structurally complex molecules, the majority of the organic reactions suffers from harsh conditions, low atom...

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Recent advances in transition-metal-free C–H functionalization of imidazo[1,2-a]pyridines

Imidazo[1,2-a]pyridines are unique nitrogen-containing organic compounds with wide applications in pharmaceuticals, natural products, material science and organometallics. Due to their significant biological...

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Recent trends and developments in the asymmetric synthesis of profens

The profens belong to a class of nonsteroidal anti-inflammatory drugs (NSAIDs), which exert significant anti-inflammatory, analgesic, antipyretic and other pharmacological effects. A considerable number...

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Organophosphorus catalytic reaction based on reduction of phosphine oxide

The special electronic configuration of phosphorus atoms endows organophosphorus reagents with unique chemical properties, which enable them to be used to catalyze various organic reactions, such as...

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Synthesis of 5-hydroxymethylfurfural from dehydration of biomass-derived glucose and fructose using supported metal catalysts

The global energy shortage has become more and more serious, which promotes the urgent need to shift to sustainable development. The value-added 5-hydroxymethylfurfural (HMF) can be derived from biomass...

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Recent advances in the radical-mediated decyanative alkylation of cyano(hetero)arene

Substituted pyridines are very important skeleton in natural products, agrochemicals and pharmaceuticals, which not only can be used to synthesis chiral ligands and functional materials but also as...

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Alternating current electrolysis: A photoredox catalysis mimic and beyond

Alternating current electrolysis (ACE) is an emerging powerful synthetic tool, which principally resembles photoredox catalysis strategies. Its periodically alternating polarity feature allows oxidation...

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Transition metal-catalyzed branch-selective hydroformylation of olefins in organic synthesis

Hydroformylation of olefins can generate linear and branched aldehydes, and the branched aldehydes are attractive precursors for the synthesis of fine chemicals and pharmaceuticals. Hydroformylation...

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Asymmetric reactions of N-heterocyclic carbene (NHC)-based chiral acyl azoliums and azolium enolates

N-Heterocyclic carbene (NHC) organocatalysis has been recognized as a powerful synthetic strategy for the construction of a wide variety of medicinally and biologically important molecules. Although...

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Pd-catalyzed functionalization of 1,3-enynes via alkylene-π-allylpalladium intermediates

In recent years, the concept of transition metal-catalyzed functionalization of unsaturated hydrocarbons has emerged as a promising strategy for developing new and valuable reactions, and has attracted...

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Recent developments in highly efficient construction of P-stereogenic centers

The construction of chiral phosphorus molecules with asymmetric center on the phosphorus atom has always been considered to be challenging in synthetic chemistry. Such P-stereogenic compounds possess...

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Carbon dioxide cycle via electrocatalysis: Electrochemical carboxylation of CO2 and decarboxylative functionalization of carboxylic acids

As one of the most important biogeochemical cycles, the carbon dioxide (CO2) cycle between atmosphere and biosphere has a profound impact on the life on earth. Therefore, the search for sustainable...

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