Synfacts

Issue 03 · March 2025

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

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Total Synthesis of (+)-Kalmanol

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Total Synthesis of (+)-Hyperbeanol A

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Total Synthesis of (+)-Euphorbialoid A

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225
Total Synthesis of (−)-Macrocalin B

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226
Synthesis of (+)-Mannolide B

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Synthesis of (–)-Strychnine FREE ACCESS

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Synthesis of Heterocycles
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Manganese-Catalyzed Ring Expansion of Cycloalkenes To Access Pyridines and Isoquinolines FREE ACCESS

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230
Expanding Scope of Carbonylative Alkylative Amination

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231
Ligand-Controlled Synthesis of Azepine Derivatives

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232
Pd-Mediated Synthesis of Fused Azetidines/Oxetanes

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233
Diastereoselectivity Switch in the Synthesis of Spirocyclic Pyrrolidine Derivatives

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234
Electrochemically Mediated Synthesis of Cycloalkanes

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235
Orthogonal Approach to Aminated Heterocyclic Derivatives

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236
Visible-Light-Induced Radical Cyclization To Access Sulfamoylated Benzo[4,5]imidazo[2,1-a]isoquinolin-6(5H)-ones

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237
Base-Free Borylation of Aryl Bromides/Iodides Promoted by Zinc

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238
Synthesis of Tetrahydroquinolines from N-Benzylhydroxylamines and Alkenes in HFIP Solvent

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239
A Tandem Amination/Cyclization of Quinazolin-4(3H)-imines

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Synthesis of Materials and Unnatural Products
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241
Aromatic-Ring-Opening Metathesis FREE ACCESS

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242
Boron-Facilitated N/C Atom Swapping in Triple Bonds

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243
Benzo-2-azaboroles

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244
Poly(p-phenylene iminoborane)

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245
High MW Polyesters from Tishchenko Polymerizations

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246
Stable Triplet Metallocarbenes

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247
Stable High-Spin Hydrocarbon-Based Diradical

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248
Enantioselective Synthesis of Helical Bilayer Nanographenes

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249
Diameter-Controlled Growth of Single-Walled Carbon Nanotubes from Organic Nanobelts

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250
Graphene-Like Covalent Organic Frameworks

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251
Double-Hoop Cycloparaphenylene (CPP)

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252
Decafluoroanthracene

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Metals in Synthesis
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Synthesis of Spirocyclic Oxaheterocycles via a Copper-Catalyzed Cyclization Alkene Transposition Sequence FREE ACCESS

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254
Copper-Catalyzed Enantioselective Acyloxylation of Activated C(sp³)−H Bonds with Carboxylic Acids FREE ACCESS

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255
Synthesis of Aza- and Oxoheterocycles from Alkenyl Amines and Alkenyl Alcohols under Palladium Catalysis

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256
Stereodivergent Access to Glutamic Acid Derivatives under Pd/Cu Dual Catalysis

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257
Rhodium-Catalyzed (Z)-Alkenyl Transfer to Aryl Ketones and Chalcones from Tertiary Allylic Alcohols

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258
Accessing Asymmetric Spirooxindoles via Divergent [3+2] and [3+3] Cycloadditions on Cu-Allenylidenes

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259
Remote Desaturation of Aliphatic Silyl Ethers under Dual Photoredox and Cobalt Catalysis

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260
Enantioconvergent Difluoromethylation of α-Haloamides under Copper Catalysis

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261
NiH-Catalyzed Polarity-Reversed Functionalization of Aliphatic Aldehydes

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262
Difluoroalkylation of Alkenes via Visible-Light-Induced Palladium Catalysis

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263
Switchable Site-Selective C(sp³)─H and C(sp²)─H Functionalization via Cp*^CF3Ir(III) Catalysis

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264
Copper-Catalyzed Synthesis of Naphthols from Enaminones and 1,3-Dicarbonyl Compounds

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265
Synthesis of Fluorinated Bicyclo[4.1.1]octenes via (4+3) Annulation of BCBs and gem-Difluoroalkenes

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266
Synthesis of Cyclopentanones with Contiguous All-Carbon Quaternary Stereocenters under Nickel Catalysis

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267
Selective Alkylations and Alkenylations of Quaternary Ammonium Salts Using Photocatalysis

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268
Asymmetric α-Alkylation of 2-Acylimidazoles by Copper(I) Catalysis

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269
Use of Strained Vinyl BCBs in a [2σ+2π] Cycloaddition Catalyzed by Palladium

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270
Site-Selective Hydrogenation of Amides Enabled by a Bifunctional Copper(I)/NHC–Guanidine Catalyst

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271
[2+1] Enabled Skeletal Editing of N-Heterocycles

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272
Making Dinitriles from Cyclic Ketones by a Copper-Catalyzed Aerobic Ammoxidation Reaction

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273
Functionalization of Sulfonamides via a Multicomponent Cobalt-Catalyzed C–H Activation

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274
Nickel-Catalyzed Asymmetric Intramolecular Hydroamidation of N-Alkenyl Formamides to γ-Lactams

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275
Copper-Catalyzed Multicomponent Synthesis of Anilines

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276
Photonitration of Arenes Using Iron(III) Nitrate as Nitrogen Dioxide Source

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277
Double Nickel Migration Leads to the Synthesis of Silaindanes

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278
Enantio- and Stereospecific Synthesis of β-Lactams via Ring Expansion of Aziridines under Rhodium Catalysis FREE ACCESS

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Polymer-Supported Synthesis
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279
Oxidative Cleavage of Alkenes Promoted by a COF-Supported Fe Complex under Photoirradiation FREE ACCESS

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280
Synthesis of 4-Aryl-3-sulfonylquinolines through Radical Cascade Annulation Using a W₂C Photocatalyst

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281
Photocatalytic Coupling of N-Heteroarenes and Alkanes/Ethers with Ce-Doped g-C₃N₄ and Bu₄NCl

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282
Deoxygenative C2 Arylation of Quinoline N-Oxides with Phenylhydrazines Using Porous Tubular Graphitic C₃N₄

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283
Cyclization of Homopropargylic Amines and CO₂ Promoted by Cu Nanoparticles Supported on MOFs

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284
Photo-Induced Oxidative Hydroxylation of Aryl Boronic Acids Using COF

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285
Visible-Light-Switchable Oxidation of Benzyl Alcohols Using NiOOH Electrocatalyst

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286
Synthesis of Isoindolones through C–H Activation and Annulation Using Pd/Cu Nanoparticles

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287
Automated On-Resin Synthesis of Oligosaccharides Bearing a Phosphoethnolamine Unit

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288
On-Resin Mukaiyama Oxidation–Reduction Thioesterification for Peptide Synthesis

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289
α-Alkylation of Nitriles with a Nano Cobalt Catalyst Supported on a Porous N-Doped Carbon

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Organo- and Biocatalysis
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291
Unveiling and Engineering the Reverse Catalytic Potential of ‘Ene’-Reductases FREE ACCESS

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292
A Benzo[ghi]perylene Monoimide Photocatalyst Defluorinates ‘Forever Chemicals’ under Visible Light

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293
Intermolecular Electrocatalytic Cyclopropanation of Alkenyl Trifluoroborates with Methylene Compounds

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294
Photocatalytic Reduction of Benzenes to Cyclohexenes

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295
Oxidative Desymmetrization of meso-Diols via Photo and Base Catalysis

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296
Asymmetric SET–NHC Catalysis in Three-Component Dicarbofunctionalizations

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297
Enzymatic Enantioselective Radical Trifluoromethyl Azidation of Styrenes

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298
Chiral-Isothiourea-Catalyzed [1,2]-Rearrangement of Ammonium Ylides

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299
Catalytic Enantioselective Synthesis of 1,4-(Hetero) Dicarbonyl Compounds through α-Carbonyl Umpolung

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Innovative Drug Discovery and Development
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301
A Radical Approach to Secondary and Tertiary Amines FREE ACCESS

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302
Metal-Free Amination of (Hetero)aryl Boronic Acids FREE ACCESS

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303
Potassium Pivalate and Alcohol Cosolvents Enhance the Efficiency and Scalability of Miyaura Borylations

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304
1,4-Metallate Migration Enables the Direct Synthesis of Organosulfates from Organoboron Compounds

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305
Late-Stage E-to-Z Photoisomerization of Pharmaceuticals and Oligopeptides

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306
Highly Efficient Conversion of Nitriles into Alcohols

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307
Fluorine at the Forefront: Transforming Opioid Antagonism with C(20)-Modified Orvinols

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308
Photochemical [4+2] Annulation of Silylimines to Access 1-Aminotetralins

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309
Ruthenium-Catalyzed Carbocycle-Selective Asymmetric Hydrogenation of Fused N-Heteroarenes

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310
(1R,3aS,4S)-Octahydro-1,4-methanopyrrolo[3,4-c]pyrrole, a Potential Piperazine or 4-Aminopiperidine Mimetic

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311
Targeted Degradation of an ‘Undruggable’ Protein Scaffold to Treat Neuroblastoma

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312
An Artificial Photoenzyme with a Thioxanthone Amino Acid Forms a Highly Strained Azetidine–Indole Scaffold

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313
Synthesis of Eglumegad FREE ACCESS

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Peptide Chemistry
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315
Synthesis of β-Amino Acids from α-Amino Acids Using Visible-Light Photoredox Catalysis FREE ACCESS

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316
Copper-Photoredox-Catalyzed Site-Selective Arylation and Alkylation of Glycine-Containing Peptides

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317
TfOH-Mediated Late-Stage Functionalization of Tryptophan Peptide Residues

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318
NHC-Catalyzed β-Keto Amino Acid Synthesis from Aldehydes and Imines

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319
Copper-Catalyzed C(sp³)–H Benzylation at the α-Position of Glycine Derivatives

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320
A New Coupling Reagent with No Heteroatomic Bonds for Amidation

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321
Mn(OAc)₃·2H₂O-Mediated Phosphorylation of Dehydroamino Acids

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322
A Liquid-Phase Peptide Synthesis (LPPS) Support for the Synthesis of Octreotide

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323
Racemization-Free Visible-Light-Mediated Synthesis of Peptides

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324
Synthesis of Unnatural Cyclic Peptides via Cu-Catalyzed 1,3-Dipolar Cycloaddition of Azomethine Ylides

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325
Synthesis of Peptoids by a Flow Reaction Avoiding Undesired Diketopiperazine Formation

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326
Accessing Photoswitchable Peptides by Embedding Spiropyrans in the Backbone of Peptides

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327
A Facile Route to Accessing an Unusual Bicyclic Melanocortin-3 Receptor Antagonist: Compound 11

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328
PTC-Catalyzed Asymmetric Alkylation of Glycine Imines for the Synthesis of Unnatural Amino Acid Esters FREE ACCESS

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Flow Chemistry
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329
Electrochemical C–O and C–N Arylation Using Alternating Polarity in Flow

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