Synfacts

Issue 05 · May 2025

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Synthesis of Natural Products
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Total Synthesis of (–)-Rubriflordilactone B FREE ACCESS

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Total Synthesis of (+)-Kobusine

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Total Synthesis of (–)-Janthinoid A

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446
Total Synthesis of (+)-Berkeleyacetal D

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Total Synthesis of (–)-ent-Caucanolide E and (+)-Caucanolide F

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Total Synthesis of (–)-Asperone A

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Total Synthesis of (+)-Shahamin K FREE ACCESS

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Synthesis of Heterocycles
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451
Selective and Sequential Aryne Generations to Build Multisubstituted Naphthalenes FREE ACCESS

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452
Rational Catalyst Design for the Asymmetric Ring-Opening of Azetidines

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453
Transition-Metal-Free Selective C2- or C4-Alkylation of Pyridines

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454
Modular Bioisosteric Replacement of Pyridine Cores with Benzonitriles

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455
Three-Step Sequence for the Formal β-C(sp³)–H Fluorination of N-Substituted Amines

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456
A One-Pot Three-Component Synthesis of 2,4-Substituted Quinazolines

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457
Aerobic Oxidative Cyclization of N-Containing Heterocycles by Perylene Diimide Catalysis

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458
Construction of 5-Substituted Oxazoles from Aryl Methyl Ketones Using PIDA

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459
Employing Manganese in Cascade Cyclization of Tertiary Enamides into 1,2-Dihydropyridines and Pyridines

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Synthesis of Materials and Unnatural Products
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461
Ligand-Stabilized Triplet Nitrenes FREE ACCESS

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462
Silyllithium-Promoted Ring Expansion of Bicyclobutanes

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463
From Boroles to Borirenes

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464
π-Extended Indoloindolizine: A New Semiconducting Module

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465
A [2,2]Pyrenophane from Photodesulfurization

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466
Azuacenes: Azulene-Fused Acenes

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467
Imine-to-Olefin Switching in Single-Crystal Covalent Organic Frameworks

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468
Creating Spirocenters in Polymerization

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469
Dithioacetal Polymers from Photopolycondensation

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470
Ring Expansion Metathesis Polymerization of Polar Monomers

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471
Decarboxylative Ring-Opening Polymerization of N-Carboxyanhydrides

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Metals in Synthesis
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473
Synthesis of Bicyclic Piperidines Enabled by a Palladium(IV) Dyotropic Rearrangement FREE ACCESS

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474
Visible-Light-Driven Gold-Catalyzed Cross-Coupling of Aryl Bromides with Carboxylic Acids FREE ACCESS

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475
Regiodivergent Synthesis of Cyclohexenes and Cyclobutenes under Palladium Catalysis

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476
Iron-Catalyzed Alkenylzincation of Terminal Allenes with Abnormal Regioselectivity

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477
Enantioselective Aziridination of Methyleneoxindoles Enabled by Nickel Catalysis

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478
Catalytic Deoxygenative Arylation of Amides with Aryl Iodides to Access β-Aryl Amines

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479
One-Pot Diazotization and Asymmetric Heck Reaction between Anilines and Unactivated Alkenes

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480
Iridium-Catalyzed Enantioselective Partial Hydrogenation of Quinolines to 1,4-Dihydroquinolines

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481
Synthesis of Five- and Six-Membered Rings from Dienes Catalyzed by Nickel

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482
Asymmetric C(sp³)–H Functionalization of Allylic Ethers under Dual Nickel and Photoredox Catalysis

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483
A Rhodium- and NHC-Catalyzed One-Pot Sequence for the Synthesis of Pyrrole-Fused Lactones

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484
Synthesis of Isocyanates by Light-Driven Nickel-Catalyzed Carbonylative Azidation of Alkyl Iodides

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485
Directed Silylalkenylation of ortho-C–H Bonds Catalyzed by Rhenium

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486
Palladium-Catalyzed Skeletal Rearrangement of Small-Ring Carboxylic Acids to α,β-Unsaturated δ/γ-Lactones

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487
[8+1] Cycloaddition of Vinyl Biscyclopropanes with CO Catalyzed by Rhodium

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488
Copper-Catalyzed Asymmetric Epoxidation of Aldehydes with α-Trifluoromethyl Diazosilanes

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489
Photochemical Palladium-Catalyzed Functionalization of 4-Acetoxy Piperidines via 1,5-Hydrogen Atom Transfer

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490
Nickel-Catalyzed Regiodivergent Hydrocyanation of Alkynes

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491
Asymmetric Synthesis of Spirocycles via Nickel-Catalyzed Alkenylation of Bisnucleophiles

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492
Copper-Catalyzed anti-Selective Silylarylation of Benzylacetylenes

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493
Trifluoromethyl Thiosulfonylation of Aryl Silicon Nucleophiles under Bismuth Catalysis

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494
Regio- and Stereoselective Desymmetrization of Alkyne-Tethered Cyclic 1,3-Diones to Access Hydrobenzofurans

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495
Combination of Rh-Hydrogen-Borrowing Catalysis and Pd-Catalyzed α-Arylation to Access α-Aryl Amines

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496
Palladium-Catalyzed Asymmetric Heck/Tsuji–Trost Allylic Alkoxylation of Cyclohexadiene Derivatives

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497
Synthesis of Chiral Allylic Sulfones via Regio- and Enantioselective Protoboration of Allenyl Sulfones

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498
Accessing Cyclopentenones via Intramolecular Rhodium-Catalyzed Hydroacylation of Alkynyl Aldehydes FREE ACCESS

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Polymer-Supported Synthesis
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499
Photocatalytic Aerobic Oxidation of Amines Using Poly(phenylene ethynylene) FREE ACCESS

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500
Nickel-Catalyzed Aryl-Carbonylative Ring-Opening of Oxiranes/Oxetanes under Electroreductive Conditions

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501
Direct Dehydrative Esterification Using a Chitosan-Supported Ionic Liquid Catalyst

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502
Aerobic Oxidation of Alcohols and Sulfides Using a Terbium MOF Catalyst under Photoirradiation

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503
Diazenylation of Cyclic 1,3-Dicarbonyl Compounds with Aryldiazonium Tetrafluoroborates Using a TiO₂ Catalyst

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504
β-Selective Functionalization of Styrenes Using a Triazine-Based COF Photocatalyst

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505
Difluoromethylation/Cyclization of 2-Isocyanobiaryls with an N-Phenylphenothiazine-Based Polymer Catalyst

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506
Selective Hydrogenation of Nitroarenes with a Graphene-Supported Co/Mn Bimetallic Catalyst

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507
Borylation of C(sp³)–O Bonds of Alkyl Ethers by Using Gold Nanoparticles Supported on α-Fe₂O₃

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508
Hydrogenative Hydrogenolysis of Aromatic Aldehydes Using Single-Atom Palladium Supported on COF

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509
Formation of Quinoline N-Oxides by Electrochemical Reductive Cyclization of 2-AllylNitroarenes

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Organo- and Biocatalysis
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511
Synergistic Phase-Transfer Catalysis for Nucleophilic Fluorination FREE ACCESS

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512
An Acridinium Photocatalyst Enables Anti-Markovnikov Hydration of Unconjugated Olefins

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513
Biomimetic Photodecarboxylation of Amino Acids

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514
Asymmetric Radical Azidation via Bioinspired Copper/Amine Cooperative Catalysis

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515
para-Selective C–H Alkylation via Radical tele-Substitution

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516
Organo-Electro Catalysis for Asymmetric Biaryldiol Synthesis

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517
Haloperoxidases: Vanadium-Dependent Metalloenzymes for Sustainable Halogenation

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518
Controlled Partial and Complete Reductions of Furans Catalyzed by Simple Brønsted Acids

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519
Electrophilic Bromination of Electron-Deficient Arenes

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520
Asymmetric Imine Addition to Azabicyclo[1.1.0]butanes as Precursors to 2-Substituted Bicyclo[1.1.1]pentanes

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Innovative Drug Discovery and Development
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521
Organocatalyst for Regioselective Lactonization FREE ACCESS

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522
Regioselective Thiolation of 2,4-Dihalopyrimidines FREE ACCESS

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523
New Synthesis of Mirogabalin – A Counterintuitive Approach

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524
A Quick Ibogaine Synthesis Amenable to Late-Stage Diversification

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525
Stereodivergent Sequential Catalysis Provides Access to Highly Functionalized Oxindoles

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526
Are You Positive? Establishing Cocaine Protonation upon DAT Binding with pH-Sensitive Anthracene Probe

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527
‘Cut-and-Sew’ Aryne Insertion into Benzocyclobutenones

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528
Skeletal Editing Approach to Synthesize Fluorinated Oxetane Isosteres

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529
Ruthenium-Catalyzed N-Heterocycle Allylation via C–H Activation

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530
Tetrel Bonding between an sp² Nitrogen Atom and an sp³ C–N σ* Bond Stabilizes a cis-Amide Geometry

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531
The Development of a Ratiometric Low-Affinity Calcium Indicator

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532
Proteomic Profiling of Rabeprazole’s Cellular Targets and Its Zinc-Mediated Activity

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533
mRNA Display Elicits Cyclic Peptide Covalent Binders of Staphylococcus aureus Serine Hydrolase

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Peptide Chemistry
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535
Peptide Stapling and Conjugation via Reversible Crosslinking of Two Alkyl Amines Using Formamidine FREE ACCESS

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536
Cobalt-Catalyzed Reductive Tandem Reaction for the General Synthesis of Functional Amino Acids

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537
Synthesis of Biaryl α-Amino Acids from Tyrosine via One-Pot Palladium-Catalyzed Arylation

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538
Synthesis of Chiral β-Amino Esters from Diazoesters and N‐Methyl Tertiary Amines Using an Iridium Complex

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539
Synthesis of Quinoxalinones Containing Heteroaryl Alanines and Oligopeptides

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540
Synthesis of Cyclohexyl Analogues of Clovibactin

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541
Chemical Synthesis of Stylissamide H

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542
Pd(II)-Catalyzed C(sp²)–H Arylation of Dehydroalanine-Containing Peptides with Arylthianthrenium Salts

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543
Flavin-Catalyzed Deprotection of C-Terminus Arylacyl Esters

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544
Redox-Neutral Photocatalytic Phosphorylation of Tyrosine and Tyrosine-Containing Peptides

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545
C–S Bond Activation of N-Aryl-α-benzylthio Glycine Esters to Access N-Aryl-α-arylated Glycine Esters

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546
Asymmetric Strecker Synthesis for the Synthesis of α-Amino Nitriles FREE ACCESS

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Flow Chemistry
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547
Continuous-Flow Synthesis of Cyclopropanes Enabled by Electroreductive Nickel Catalysis

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