Synfacts

Issue 04 · April 2025

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Synthesis of Natural Products
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331
Synthesis of (+)-Moluccensin G and (+)-Krishnolide F

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332
Total Synthesis of (–)-Veratramine

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333
Synthesis of (–)-Azorellolide

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Total Synthesis of (+)-Isochamaecydin

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335
Total Synthesis of (–)-Strempeliopine

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336
Total Synthesis of (–)-Isolinearol

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337
Synthesis of (±)-Roseophilin

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Synthesis of Heterocycles
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339
Skeletal Editing to Access Substituted Aminoisoquinolines

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340
Construction of Pyridoquinazolinones from Benzoic Acids and 2-Aminopyridines Using Copper Catalysis

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341
A One-Step Approach for the Synthesis of C–C-Linked Glutarimides

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342
Easy Access to 2‑Methylquinazolin-4(3H)‑ones from 2-Aminobenzamides and Calcium Carbide

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343
An IMDA/Aromatization Sequence for Isoindolinone Synthesis

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344
Azlactone Incorporation Facilitating Versatile Ring Expansion of Unstrained N-Heterocycles

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345
Pyrrole Derivatization through a Haloform Reaction

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346
Synthesis of 2-Quinolones via Intramolecular Electrophilic Amination by Nitrenium Ions

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347
Development of Library Protocols Based on Core Syntheses of Heterocycles

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348
A Transition-Metal-Free Approach to Access Pyrazolopyridines and Pyrazolopyrimidines

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349
Nitrene-Mediated Ring Expansion of Five-Membered N-Heterocycles

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350
Modular Synthesis and Reactivity of Hetero[3.1.1]propellanes

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351
Logistical Ligand Design Enables Enantioselective Remote C–H Activation

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Synthesis of Materials and Unnatural Products
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353
Supramolecular Snub Cubes with Chirality

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354
An M₉L₆ Supermolecular Cage

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355
Cyclic [4]Catenanes

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356
Zigzag Aromatic Nanotubes of Truncated Cone Shape

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357
A Triplet Dianthraceno[2,3-a:3′,2′-h]-s-indacene

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358
Conjugated Ladder Polymers of Cyclooctatetraene

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359
Unsymmetrical Pyrenes via a Quadruple Photochemical Cascade

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360
Centrosymmetric Double Difluoroboron Cores: New Narrowband Emitters

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361
Diboron-Enabled [5,5]-Sigmatropic Rearrangement

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362
Octacyclic Scaffolds from Diaryl Alkynes in One Pot

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363
Arenesulfenyl Fluorides for Fluorosulfenylation

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364
π-Extended Arsabenzenes

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Metals in Synthesis
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365
Photoredox-Catalyzed Acylesterification of Alkenes Using Acyloxime Esters as Bifunctional Reagents

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366
Copper-Catalyzed Enantioselective Hydrocupration of Cyclic Allenol Esters

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367
β-Trifluoromethylalkylation of Silyl Enol Ethers under Dual Nickel and Photoredox Catalysis

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368
Palladium-Catalyzed β-C–H Activation and Arylation of Ketones and Esters

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369
Asymmetric Addition of N-Heterobiaryl Triflates to Aldehydes under Dual Cobalt and Photoredox Catalysis

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370
Regioselective Product Formation Induced by Selection of the Base Cation

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371
Copper-Photocatalyzed Defluorinative C(sp³)–O Coupling of Trifluoromethylarenes and Alcohols

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372
Sequential C–H Activations for the Synthesis of P‑Stereogenic Benzophosphole Oxides

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373
Magnesium-Promoted Ring Expansion of Donor–Acceptor Cyclopropanes to Azetidines

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374
Synthesis of Silacycles via Double Hydroalumination and Intramolecular Cyclization

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375
C4-Alkylation and Arylation of Pyridine via Metalation with Butylsodium

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376
Photocatalytic Decarboxylative Fluoroalkylation of α,β-Unsaturated Carboxylic Acids

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377
A Hydrogen-Borrowing Strategy for the Construction of Carbocycles Containing Quaternary Stereocenters

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378
Asymmetric Synthesis of Allylic Amines by Reductive Coupling of Internal Alkynes and Imines

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379
Metallaphotoredox-Catalyzed Single-Carbon-Atom Insertion into Alkenes for Allene Synthesis

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380
Silver-Catalyzed Z-Selective Hydroalkylation of Terminal Conjugated Alkynes Using Alkyl Boranes

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381
Thermodynamic Isomerization of cis-1,2- to trans-1,2-Cyclopropanols

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382
Copper-Catalyzed Asymmetric Alkylboration of 3,3-Disubstituted Cyclopropenes

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383
Nickel-Catalyzed Arylation of 1,1-Disubstituted Alkenes To Access Stereodefined Quaternary Carbons

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384
Photocatalytic Dehydrogenation of Cycloalkanes to Arenes

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385
Silver-Mediated Peptide Coupling of Thioamides via O–N Acyl Transfer

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386
Enantioselective C(sp³)–H Arylation of Acetonides by Dual Nickel and Decatungstate Photocatalysis

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387
Ruthenium-Catalyzed Hydration of N-Heterocycles Enables Access to Lactams

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388
Photoredox-Catalyzed Bromocyanodifluoromethylation of Unsaturated Hydrocarbons

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389
An Asymmetric Karasch–Sosnovsky Oxygenation of Allylic and Propargylic C–H Bonds

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390
Gold(I)-Catalyzed Propargyl Claisen Rearrangement

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Polymer-Supported Synthesis
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391
Triarylamine-Mediated Electrochemical [2+2+2] Cycloaddition Forming 3,6-Diarylpyridines

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392
Synthesis of N-Sulfonyl Amidines in Water Using a Magnetic CoFe₂O₄-Supported CuI Catalyst

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393
Synthesis of γ-Sultines through Photo-induced Sulfonylation–Sulfinylation of Terminal Arylalkenes

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394
Decarbonylative Silylation of Cinnamaldehydes Using a Zr-Based MOF-Supported Ru Photocatalyst

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395
Phenolic Resin Photocatalysts for Aerobic Oxidation of Sulfides and Benzylamines

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396
The Synthesis of Quinazolines and Quinazolinones Promoted by a Single-Cobalt-Atom Catalyst under Air

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397
Amination of Phenols Using Single-Site Palladium on CeO₂

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398
Oxidative Dehydrogenation of Tetrahydroquinolines Using a Three-Dimensional Mesoporous COF

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399
CuPd Bimetallic Nano Catalysts for the C–H Arylation of Azoles

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400
Synthesis of Cyclic Carbonates from Epoxides and CO₂ Using Polystyrene-Supported Ionic Liquid Catalysts

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401
Ni- or Ru-Zeolite-Catalyzed Continuous-Flow Dehydrative Synthesis of Macrocyclic Ethers and Lactones

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Organo- and Biocatalysis
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403
Photoredox- and Metalloenzyme-Catalysis Enables Enantioselective Radical Azidations and Thiocyanations

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404
Bifunctional Dihydrazide Catalysis Involves Nucleophilic Enamine Activation

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405
Asymmetric N-Alkylation of o-Carboranyl Amines Using Chiral Phosphoric Acids

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406
Silylium-Based Asymmetric Counteranion-Directed Catalysis Involving Peroxycarbenium Intermediate

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407
Organocatalytic Asymmetric Transfer Hydrogenation of 2-Substituted Quinolines

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408
Taming Highly Enolizable Aldehydes via Enzyme Catalysis

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409
Stereoselective Trifluoromethylation of Olefins and Nitro Compounds Catalyzed by Old Yellow Enzymes

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410
Organocatalytic Decarboxylation of Indoline-3-carboxylic Acids

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411
Synthesis of Complex Piperidines via a Biocatalytic C–H Oxidation/Radical Cross-Coupling Sequence

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412
Organophotocatalytic Alkene and Indole Carboxyalkylation via CO₂^•–

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Innovative Drug Discovery and Development
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413
Practical Approach toward gem-Difluorinated Ring Expansion of Exocyclic Alkenes

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414
Aminoalkylation of Alkenes via Triple Radical Sorting

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415
Leveraging Metabolic Reprogramming 2-Quinolones to Treat MRSA-Infected Wounds

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416
Decarboxylation: Innovation and Functionalization

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417
Iron-Enabled Anti-Markovnikov Photocatalytic Hydro- and Deuterochlorination

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418
Practical Approach for Diverse Functionalization of Complex Small Molecules via Thianthrenium Salts

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419
Development of a Tepotinib-Based PROTAC as a Potential Lung Cancer Therapeutic

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420
Convenient Access to Heteroaromatic Methyl Sulfones

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421
Chemoselective and Mild Conditions for Controlled Reductions of Carboxylic Acid Esters

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422
Diazirines in a New Light: Chromophore Conjugation Indicates a Functional sp²-Hybridized Carbon Center

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423
Scaffold Hopping with IL-17 Antagonists – Exploiting an Oxygen-to-Sulfur Interaction to Favor Planarity

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424
Getting to the Root of Pulmonary Arterial Hypertension: Designing Novel Pyridine-2-one AMPK Inhibitors

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425
Diastereoselective Synthesis of Benzazepines via Pd(II)-Catalyzed [3+2] Cycloaddition

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426
One Starting Material, Two Directions: Acyl and Decarbonylative Couplings of Anhydrides

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Peptide Chemistry
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427
Cobalt-Catalyzed Synthesis of Silicon-Containing Amino Acids and Peptides

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428
Peptide Bond Formation of Unprotected Amino Acids in H₂O–THF

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429
S–S-Linked Peptide Synthesis via Disulfuration of Azlactone

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430
Gram-Scale Synthesis of Spirocyclic Prolines and Pyroglutamic Acids

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431
Photoredox-Catalyzed Synthesis of Unnatural Amino Acid Derivatives

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432
Synthesis of Chiral Amino Esters by Asymmetric Branched-Selective Ring-Opening Functionalization

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433
Synthesis of α-Amino Esters via Catalytic Enantioselective Nucleophilic Amination

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434
Backbone Amidoxime Ether Directed C(sp³)–H Functionalization of Peptides by Palladium Catalysis

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435
Synthesis of Metallo-Azapeptides by Composed Chelation of Peptide Backbone Nitrogen with a Metal

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436
Accessing Unblocked Racemic Tryptophan Derivatives by Using a Nickel(II) Complex of Gramine

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437
Palladium-Catalyzed Aminocarbonylation of Peptides for the Synthesis of N-Capped Peptides

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438
Photoinduced Regiodivergent and Enantioselective Alkylation of Glycine Derivatives

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439
Copper-Catalyzed Difluoroalkylation for Glycine Derivatives

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440
Chemoselective Deprotection of Fmoc and OMe in N-Fmoc-Amino Acid and N-Fmoc-Dipeptide Methyl Esters

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Flow Chemistry
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441
Highly Efficient and Reusable Resin Catalyzes the Ritter Reaction in Flow

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