Synfacts

Ausgabe 07 · Juli 2020

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A92
SYNFORM ISSUE 2020/07

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Synthesis of Natural Products and Potential Drugs
z0749
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0749
Synthesis of (–)-Scabrolide A FREIER ZUGRIFF

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0750
Synthesis of Tafluprost

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0751
Synthesis of GDC-0022 FREIER ZUGRIFF

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0752
Total Synthesis of (±)-Phyllantidine

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0753
Total Synthesis of Lycojaponicumin A

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0754
Synthesis of a Carfilzomib Fragment

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0755
Synthesis of Esketamine

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0756
Total Syntheses of Kopsane Alkaloids

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0757
Synthesis of (–)-Minovincine and (–)-Aspidofractinine

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0758
Synthesis of an Indoleamine-2,3-Dioxygenase-1 Inhibitor

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0759
Synthesis of a Phosphodiesterase 1 Inhibitor

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0760
Synthesis of AZD9742

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0761
Synthesis of AZD7648

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0762
Synthesis of (–)-Spirochensilide A

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0763
Synthesis of (±)-Daphnilactone A FREIER ZUGRIFF

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0764
Synthesis of Lanraplenib

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0765
Synthesis of Remdesivir (GS-5734) — A Candidate for the Treatment of Ebola and COVID-19 Infections FREIER ZUGRIFF

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Synthesis of Heterocycles
z0767
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0767
Automated Approach to the Modular Synthesis of Drug-Like Molecules

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0768
Transition-Metal-Free Synthesis of 3,4-Disubstituted 2-Piperidinones

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0769
Synthesis of Oxazolidines, Pyrrolidines and Mannich Bases from Aliphatic Aldehydes

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0770
A Scalable Route to N-Difluoromethylated Heterocycles

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0771
Modular Rhodium-Catalyzed Synthesis of Quinolines from Anthranils and Acrylic Acids

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0772
Reactions of Epoxides, Thiiranes, Aziridines and Azirines with Cyanoform FREIER ZUGRIFF

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0773
Synthesis of Alkene Carbonates by Carbon Dioxide Fixation Using Perfluorinated Triol Catalysts

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0774
Palladium-Catalyzed β-Cycloalkenylation of Saturated Cyclic Ketones

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0775
Palladium-Catalyzed Enantioselective Synthesis of Isoxazolines

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0776
Rhodium-Catalyzed Synthesis of Isoquinolines from Aryl Ketones and Alkynes

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0777
Ruthenium-Catalyzed Diastereoselective Synthesis of Tetrasubstituted Pyrrolidines

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0778
One-Pot Synthesis of 2-Trifluoromethyl-6-azaindoles

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0779
Copper-Mediated Synthesis of N²-Aryl-1,2,3-Triazoles

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0780
Mild Synthesis of 3H-Indoles and Benzazepinones from Nonactivated Anilines

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0781
Asymmetric Synthesis of Cyclopropane-Fused Pyrrolidines

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Synthesis of Materials and Unnatural Products
z0783
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0783
How Germane: Polyfluorobiaryls via C–H Functionalization Cross-Coupling

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0784
Aminohelicenes to Helical ortho-Diketones FREIER ZUGRIFF

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0785
Double or Nothing

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0786
A New Member in the Family of Pyrazinophane

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0787
N-Doped Nanotube with Periodic Defects

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0788
Golden Gateway to Au(I)–Aryls

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0789
No Directing Group? No Problem!

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0790
A One-Step, Three-Component Reaction to Synthesize Phenothiazines

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0791
One, Two, Five, Six: Guanidino-Naphthalenes Get New Tricks

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0792
Texas-Sized BODIPY Analogues

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0793
Multiple Arylation of Cubanes

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0794
Peri-Peri: Spicy Radical Double Annulations

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Metals in Synthesis
z0795
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0795
Dual-Catalyst Photoinduced Alkenylation of Alkanes and Aldehydes via C–H Activation FREIER ZUGRIFF

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0796
Intramolecular Hydroacylation of Benzaldehyde Derivatives by Cobalt-Catalyzed C–C Bond Cleavage

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0797
Nickel-Catalyzed Enantioconvergent Coupling of Racemic Partners FREIER ZUGRIFF

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0798
Asymmetric Allylation of N-Methyl Anilines by Palladium/Photoredox Cooperative Catalysis

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0799
Nickel-Catalyzed Electrochemical Synthesis of Diarylmethanes

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0800
Stereoselective Preparation of Fluoroenynes

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0801
Ruthenium-Catalyzed ortho-C–H Arylation

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0802
Synthesis of Enantioenriched Secondary Alcohols by Enantioselective Ru-Catalyzed Coupling of Two Alcohols

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0803
Bicyclo[1.1.1]pentanes as Electrophiles for Iron-Catalyzed Cross-Coupling

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0804
Palladium-Catalyzed Oxidation of β-C–H Bonds of Primary Alkylamines

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0805
Dual Photoredox Catalysis for the C–H Arylation/Decarboxylative Vinylation of Cyclic Oxalates

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0806
Ruthenium-Catalyzed Synthesis of Vinylamides

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0807
Rhodium-Catalyzed Hydroaminative Cyclizations

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0808
Enantioselective Annulation of N-Methoxybenzamides with Quinones by Rhodium-Catalyzed C–H Activation

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0809
New Ru(II)-NHC-Diamine Precatalysts for Asymmetric Hydrogenation

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0810
Cobalt-Catalyzed Synthesis of Eight-Membered Rings

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0811
Photocatalyzed Difunctionalization of Carbonyls

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0812
Photoredox-Catalyzed Diastereoselective C–H Arylation/Epimerization of Piperidines

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0813
Iron-Catalyzed Photoinduced C–H Bond Amination Using Organic Azides

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0814
Dual Cobalt Ruthenium Photoredox-Catalyzed Oxidative Hydrofunctionalization

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0815
Chemo- and Enantioselective Reduction of β-Keto-Enamides by Transfer Hydrogenation

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0816
Electrosynthetic Reductive Pyridylation of Alkenes in an Undivided Cell

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0817
Iridium-Catalyzed Ring-Expansion Proceeding via Hydrogen Borrowing

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0818
Enantioselective Copper-Catalyzed Cycloaddition: Preparation of Pyrrole-Fused Bridged [2.2.1] Scaffolds

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0819
Synthesis of Functionalized Enamides via Rhodium-Catalyzed Cleavage of Triazoles

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0820
Enantioselective Synthesis of Tetrahydrobenzofurans by Gold/Cobalt Dual Catalysis

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0821
Photoinduced Copper-Catalyzed Alkynylation of Redox-Active Esters

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0822
Dual Light-Driven Palladium-Catalyzed Carbonylation

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0823
Miyaura Borylation Reaction FREIER ZUGRIFF

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Polymer-Supported Synthesis
z0825
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0825
Hydroformylation of Styrene Derivatives Catalyzed by Rhodium Single-Atoms Supported on CeO₂ FREIER ZUGRIFF

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0826
Allylation of Aldehydes and Ketones Catalyzed by Cu-Impregnated Mg–La Mixed Oxide

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0827
Dehydrogenative Coupling of Amines on Cobalt Nanoparticles Coated with N-Doped Graphene

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0828
Synthesis of 1,4-Benzodiazepine Derivatives in Water Using Ni NPs Supported on CoFe₂O₄@GO-Kryptofix 22

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0829
Oxidation of Alkenes to Ketones and 1,2-Diketones Catalyzed by a Bifunctional Iron Nanocomposite

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0830
Oxidation of Alcohols in Water on a Mesoporous Polypyrrole/Carbon-Supported Palladium Catalyst

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0831
Brønsted Acid Catalyzed Aromatic C–H Insertion of α-Aryl Diazoacetates with H₂SO₄–SiO₂

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0832
Synthesis of Chromeno-pyrido[d]pyrimidines by Using a Fe₃O₄@ZnO Nanocomposite Supported on Polyaniline

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0833
Chemoselective Hydrogenation of 4-Chloronitrobenzene on a Supported Platinum Catalyst

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0834
A Polyethylene-Supported Imidazolium Salt for the Synthesis of Cyclic Carbonates from CO₂

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Organo- and Biocatalysis
z0835
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0835
Enzymatic Depolymerization of Poly(ethylene terephthalate) FREIER ZUGRIFF

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0836
NHC-Catalyzed Radical Relay δ‑Ketocarbonyl Synthesis

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0837
Lewis Acid Catalyzed Hydridodeamination

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0838
Catalytic Hydroetherification of Alkenes Mediated by Proton-Coupled Electron Transfer

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0839
Biocatalytic Functionalization of Primary and Secondary α-Amino C–H Bonds

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0840
Unprecedented Selectivities in the C7-Hydroxylation of Steroids Enabled by a P450-BM3 Mutant

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0841
DFT-Assisted Substrate Optimization Permits Desymmetrization of 1,3-Diol Acetals

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0842
New Chiral P₂-Phosphazene Organosuperbases Combine High Basicity and Control of Stereoselectivity

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0843
Sulfide-Catalyzed Synthesis of Allylic gem-Difluorides through a Meyer–Schuster-Like Rearrangement

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0844
Brønsted Acid Catalyzed Pseudotransannular Desymmetrization Permits Access to Tropanols

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0845
Enantioselective Protonation of Enol Intermediates Derived from Light-Mediated C–H Functionalization

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Chemistry in Medicine and Biology
z0847
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0847
Selectively Binding a Bromodomain FREIER ZUGRIFF

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0848
Bicyclic Arginase Inhibitors to Enhance Cancer Immunotherapy

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0849
Sterically Shielded Heptamethine Cyanine Dyes with Enhanced Photophysical Properties

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0850
DNA-Compatible Cycloadditions for Rapid Library Synthesis

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0851
Chemically Induced Vinylphosphonothiolate Electrophiles for Thiol–Thiol Bioconjugations

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0852
Optical Control of Gene Silencing by Azobenzene-Modified siRNA

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0853
A Nucleolus-Targeted, Photocaged Pt(IV) Prodrug Overcomes Cancer Resistance

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0854
Unraveling Masked GPX4 Inhibitors

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0855
The First Selective Inhibitor of DCLK-1

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0856
How to Overcome Vancomycin Resistance

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0857
Total Synthesis of Galactosyl-Queuosine

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0858
A Broadly Reactive Covalent Ligand for Glutamates and Aspartates

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0859
Chemoselective Methionine Bioconjugation in the Synthesis of Antibody Drug Conjugates (ADCs)

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0860
Potent TAS2R8 Antagonists as Bitterness Blockers

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0861
Chemically Induced Dimerization FREIER ZUGRIFF

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0862
A Photocrosslinkable Mycobacteria Glycolipid Probe

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Peptide Chemistry
z0863
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0863
Synthesis of Peptides with Acyl N-Methylimidazolium Cations FREIER ZUGRIFF

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0864
Photocatalytic Conjugate Addition of Amino Acids or Peptides

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0865
Chiral Nonnatural α-Amino Acid Synthesis by Enantio-selective Mannich Reaction and Hydrogenation

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0866
Base-Controlled Synthesis of α- and β-Amino Acid Derivatives from Azirine Rings and Arylacetic Acids

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0867
Synthesis of Amino Acid Derivatives from Glycine Derivatives and Ketones/Aldehydes

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0868
Conjugation of Two Peptides via Disulfide Linkage FREIER ZUGRIFF

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0869
Iridium-Catalyzed Site-Selective Thiolation

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0870
Iridium-Photocatalyzed Synthesis of Nonnatural α-Amino Acids

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0871
Palladium-Catalyzed Synthesis of Glycopeptides through C–H Activation

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0872
Amidation of Amino Acids with 4-[(Fluorosulfonyl)oxy]-benzoic Acid Toward Prodrugs

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Flow Chemistry
z0873
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0873
Synthesis of α-Chloro Aldehydes in a Flow Microreactor

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0874
Generation and Use of Fluoroorganolithiums in Flow Microreactors

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