Synfacts

Issue 01 · January 2025

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Synthesis of Natural Products
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1
Total Synthesis of (+)-Garajonone FREE ACCESS

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2
Synthesis of (–)-Bipolarolide D

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3
Synthesis of (±)-Berkeleyone A and (±)-Preaustinoid A

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4
Total Syntheses of (–)-β- and (–)-γ-Naphthocyclinones

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5
Total Synthesis of (+)-Cylindricine C

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6
Formal Synthesis of (±)-Morphine

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7
Total Synthesis of (+)-Pumiliotoxin A FREE ACCESS

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Synthesis of Heterocycles
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9
Facile Synthesis of Pyridones from Cyclopentenones FREE ACCESS

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10
Photochemical Pathway for Synthesis of 2- or 3-Cyanoindoles and Mechanistic Insights

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11
Synthesis of Tetrahydroquinolines from Arylaminomenthyl Cyclopropanes

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12
Photoenyzmatic Reductive Coupling of Electron-Deficient Heterocycles with Alkenes

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13
Enzymatic Synthesis of Pyrrolines/Indolines

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14
Diastereoselective Synthesis of Densely Functionalized 1-Pyrrolines

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15
Strain-Release of Azetidines for the Synthesis of 3,4,5-Trisubstituted Piperidines

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16
Diversity-Oriented Synthesis of Macrocycles

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17
Rational Catalyst Design for an Optimized Aza-Michael Addition

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18
Modular Access to Oxymorphinan Derivatives

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Synthesis of Materials and Unnatural Products
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Click-Clip FREE ACCESS

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20
Controlling 1,4-Palladium Aryl to Aryl Migration

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21
A Catenate Interlocked 2D Covalent Organic Framework

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22
γ-Graphynes from S_NAr Reactions

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23
A New Luminescent Dicarbazolyl Methyl Radical

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24
A Pentacene Tetraimide

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25
Thiahelicenes into Coronenes

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26
Highly Twisted Fenestrindanes

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27
Weaving Molecules

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28
BN₃-Bridged D-π-A Molecules with Narrow-Band Near-Infrared Emissions

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29
Large Dibora-Polycyclic Aromatic Hydrocarbons from Alkyne Annulation

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30
Seleno- and Telluroesters from Photoreactions of Acylsilanes

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Metals in Synthesis
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31
Amidyl Radical Insertion to Bicyclo[1.1.0]butanes Using Photocatalysis FREE ACCESS

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32
Palladium-Catalyzed Formamidation of Aryl Halides Using Sodium Azide and Oxalic Acid FREE ACCESS

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33
Remote Alkylation of Alkenes via an Iridium-Mediated Chain-Walking and Carbene Insertion Cascade

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34
Synthesis of 1-Indanones by Photoredox-Catalyzed (3+2) Annulation of Aromatic Amides with Olefins

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35
Iridium-Catalyzed Anti-Markovnikov Hydrocarboxylation of Olefins

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36
Propargylic C(sp³)–H Etherification via an Allenyl–Iron Organometallic Species

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37
Asymmetric Addition of Organozinc Reagents to Aldehydes

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38
Asymmetric Semipinacol Rearrangement of Diarylallylic Alcohols to α-Aryl Ketones under Cobalt Catalysis

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39
Dual-Metal-Catalyzed Synthesis of Fused Quinolin-2(1H)-one Scaffolds

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40
Nickel Hydride Catalyzed Enantioselective Synthesis of Alkenyl Cyclobutanols from 1,4-Alkynones

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41
Palladium-Catalyzed Synthesis of Homoallylic Alcohols via an Umpolung Hydrazone Strategy

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42
Photoredox-Catalyzed Hydronitration and Hydronitroalkylation of Alkenes

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43
Indazole Synthesis through the Copper-Catalyzed Cyclization of 2-Alkynylazobenzenes

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44
Asymmetric Allylic C(sp³)–H Acyloxylation of Internal Alkenes Enabled by Photoexcited Copper Catalysis

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45
Access to Non-canonical Tryptophan Derivatives by Rhodium-Catalyzed C–H Functionalization of Anilines

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46
Nickel-Catalyzed Enantioselective Decarboxylative Difluoromethylation of Phthalimide Esters

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47
Palladium-Catalyzed Synthesis of Cyclic Boronates from Vicinal-diboronates and 2-Halophenols and Anilines

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48
Reductive Ring Opening of N-Benzoyl Pyrrolidines under Lewis Acid Assisted Photoredox Catalysis

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49
Shuttle Catalysis Enabled by Cobalt Hydrides: Efficient Hydrofunctionalization of Terminal Alkenes

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50
Nickel-Catalyzed Tertiary C(sp³)–H Bond Methylation Enabled by Photochemically Activated Alkyl Peroxides

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51
Dehydrogenation of Apolar Amino Acids to Access Versatile Non-Canonical Amino Acids

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52
Photoredox-Catalyzed Direct Olefination of Carboxylic Acids with Phenyl Vinyl Ketones

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53
Asymmetric Synthesis of α-Amino Nitriles from Carboxylic Acids

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54
A New Class of Pyridine-Derived NHCs Enables Copper-Catalyzed Asymmetric Allylic Alkylation

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55
The Heck Carbonylation: Palladium-Catalyzed Alkoxycarbonylation of Organic Halides FREE ACCESS

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56
Copper-Accelerated Palladium-Catalyzed Cross-Coupling of Terminal Alkynes and sp² C–X Bonds FREE ACCESS

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Polymer-Supported Synthesis
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57
Photoelectrochemical Alkene Epoxidation with Water Using a TiO₂-Ru Anode FREE ACCESS

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58
Montmorillonite-Catalyzed Construction of Hantzsch Derivatives Using UHP under Microwave Irradiation

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59
Alkylidene Bisamide Condensation with a Graphene Oxide Based Hydrogen Sulfate Nanocomposite

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60
LDH-Supported Nano Cu(I)-Catalyzed Multicomponent Reaction Forming Benzopyrans

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61
Dehydrogenative Annulation of 3-Amino Alcohols with Secondary Alcohols by Cobalt Nanoparticles

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62
Photocatalytic Cycloaddition and Oxidation by a Benzothiadiazole-Based Ordered Mesoporous Polymer

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63
Photocatalytic Synthesis of 2-Hydroxybenzofuran-3(2H)-ones Using Double Perovskite Cs₂AgBiBr₆ Nanocrystals

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64
Markovnikov Selective Hydroamination of Vinylarenes with Aromatic Amides Using Hβ Zeolite

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65
Nitrogen-Doped Carbon-Encapsulated Ni Nanoparticles for Selective Hydrogenation of Nitroarenes

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66
Oxidative Amidation of Alcohols Using Lead-Free Metal Halide Perovskite

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67
Photoinduced Oxidation of Sulfides Using Donor–Acceptor Heterojunction Fiber-Like Micelles

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Organo- and Biocatalysis
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69
Electrochemical Organocatalytic Production of Methane FREE ACCESS

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70
Transaldolases Enable Asymmetric Aldol Addition to Unactivated Ketones

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71
Asymmetric Synthesis of Chiral α,α-Dialkyl Amines

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72
Enantioselective Hydrogen Atom Abstraction Catalysis

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73
Photocatalytic Carboxylation of Benzylic Tertiary C−H Bonds with CO₂ in the Presence of Stoichiometric Base

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74
Catalytic Asymmetric Cracking of Cyclopropanes

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75
Brønsted Acid–HFIP Combination Allows Amination of 2-Arylethanols via Phenonium Intermediate

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76
Sustainable Silane Oxidation to Silanols via Frustrated Lewis Pair Catalysis with Water

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77
Photocatalytic Functionalization of Weakly Nucleophilic Alkenes with Electrophiles

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78
Formal [3+2] Cycloaddition Catalyzed by Lewis Base: A Straightforward Route to 1,3-Dioxolane Derivatives

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Innovative Drug Discovery and Development
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79
Gatekeeper Pocket as Auxiliary Interaction Site for Macrocyclic Cyclophilin Inhibitors FREE ACCESS

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80
Radiosynthesis of [¹⁸F]Trifluoroiodomethane and Its Use for Radical ¹⁸F-Trifluoromethylation Reactions FREE ACCESS

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81
Synthesis of Enantiopure Piperidines on Industrial Scale

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82
Convenient Synthetic Access to 1,5-Disubstituted 2‑Oxabicyclo[2.1.1]hexanes as ortho-Substituted Benzene Mimics

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83
Enantioselective, Catalytic HFL Reaction to Access Chiral 2,5-Pyrrolidines

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84
A Two-Step Approach to Functionalized Aziridines

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85
A Photoswitchable Analogue of the GABA_A Agonist-Potentiator Abecarnil

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86
Multigram-Scale Macrobicyclic Thiolincosamine Synthesis

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87
New Procedure for On-DNA Diazo-Transfer

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88
Shedding Some New Light on 1,2-Dicarbonyl Deoxygenations

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89
Umpoled Approach to Silicon Glycomimetics

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90
Generation of Tertiary Alkylamines by Photoredox Catalysis and Nickel-Catalyzed Cross-Coupling

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91
Photoswitchable Negative Allosteric Modulator of GluN2B-Containing NMDA Receptors

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92
SAR Analysis Delivers Promising Piezo1 Channel Agonist

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93
Metal-Free Deuteration of Arenes with D₂O Enabling Late-Stage Functionalization

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Peptide Chemistry
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95
Electrochemical Ring-Opening Reaction of Piperidine-Containing Peptides FREE ACCESS

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96
Palladium-Catalyzed Late-Stage Functionalization for Installation of Maleimide Scaffolds into Peptides

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97
Flavin-Catalyzed Synthesis of 4,5-Dihydroxynorvaline

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98
BODNs as New Reagents for Visible-Light Photocatalytic Bromination of Tyrosine Residue

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99
Synthesis of (2S,3R,4R)-Dihydroxyisoleucine (DHIle) and Its Application in Amatoxin Synthesis

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100
Asymmetric Synthesis of β³-Tryptophan via C–H Amination

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101
Pd-Catalyzed Synthesis of Thioglycopeptide

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102
Synthesis of Diketopiperazines from α-Amino Amides and Diazophosphonate Ester Using Cp^*Rh(III) Catalyst

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103
Synthesis of Unnatural Amino Acids and Peptides via Desulfurative Alkylation of Cysteine Derivatives

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104
Advanced Thiol Nucleophiles and Peptide Hydrazides in the Synthesis of Peptide Alkyl Thioesters

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105
N-Terminal Thiazolidine-Containing Peptide Thioesters via a Thioproline-Based Oxidation Approach

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106
1,2-Phospha-Brook Rearrangement for Synthesis of Phosphorylated Tyrosine Derived Peptides

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107
Ethyl Propiolate Mediated Peptide Synthesis FREE ACCESS

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Flow Chemistry
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109
Avoiding PFAS in the Preparation of Functionalized Trifluoromethylated Heteroatoms

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