Synfacts
Issue 06 · June 2022
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SYNFORM
ISSUE 2022/06
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Synthesis of Natural Products and Potential Drugs
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0579
Synthesis of Belzutifan
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0580
Synthesis of Antimalarial INE963
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0581
Total Synthesis of (–)-Grayanotoxin III
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0582
Synthesis of (–)-Gukulenin B
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0583
Synthesis of (–)-3-Oxoisotaxodione
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0584
Asymmetric Synthesis of the Cyclohexyl Fragment of BMS-986251
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0585
Synthesis of the Tricyclic Core of BMS-986251
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0586
Total Synthesis of (–)-Daphenylline
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0587
Synthesis of (–)-γ-Lycorane
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0588
Large-Scale Synthesis of AZD4573
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0589
Synthesis of KRAS
G12C
Inhibitors
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0590
Asymmetric Synthesis of Giredestrant
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0591
Synthesis of (±)-Myrioneurinol
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0592
Second-Generation Synthesis of BMS-986224
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0593
Synthesis of Orexin 2 Receptor Agonist TAK-925
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0594
Synthesis of MK-1029
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0595
Process for the Manufacture of Giredestrant (GDC-9545)
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0596
Synthesis of a KRAS
G12C
Inhibitor
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0597
Total Synthesis of (±)-Ishwarane
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Synthesis of Heterocycles
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0599
Cross-Coupling Approach to Partially Saturated Heterocycles
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0600
Non-Radical-Mediated C–H Alkylation of Pyridines
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0601
Regioselective Functionalization of Azoles
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0602
C2-Selective S
N
H Amination of Pyrimidines through Selective Iminium Formation
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0603
Robust Difluoromethylation of Nonactivated Ketones
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0604
Synthesis of 5-Fluoroindolizines by Photocatalytic Defluorinative Coupling and S
N
V Cyclization
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0605
2-Amino-3,3-difluoro-2,3-dihydrofurans from Difluorocarbenes and Enaminones
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0606
Nickel-Mediated Allylation of Heterocycles
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0607
Oxindole Synthesis through a Polar–Radical Crossover
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0608
Naphthyridinone Formation through Palladium-Catalyzed Annulation of 1,6-Enynes and 2-Iodoanilines
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0609
Synthesis of 2-Pyridones by Ring Expansion of Furans or γ-Lactams
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0610
Gold and N-Heterocyclic Carbene Relay Catalyzed Synthesis of Pyrrole-Fused Lactones
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0611
Selective Synthesis of Pyridines and Pyrimidines Using Isopropene Derivatives
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0612
Synthesis of β-Aryl-γ-lactams and 2-Oxo-1,2-dihydroquinolines
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Synthesis of Materials and Unnatural Products
z0613
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0613
Trouncing the Troublesome Trilactam
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0614
Nonperipheral Functionalization of Triazatruxenes
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0615
Nucleophilic Cyclodehydration of Enantiomerically Pure Helical Quinones
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0616
Bundling Fluorine and Iodine on Unactivated Alkenes
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0617
Ring, Ring! Directed Aromatic Homologation
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0618
Copper-Catalyzed Unsymmetrical Trimerization of Indole towards Isotriazatruxene
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0619
An Iterative Synthetic Route towards Unsaturated and Partially Saturated [7]Helicenes
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0620
Cycloaddition with Stannoles to Make PAHs
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0621
Helicenes Featuring Azulene
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0622
Annulation à la Alumina
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0623
Belt-Like Expanded Carbaporphyrins
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0624
Solution-Mediated Synthesis of Cove-Edged Nanographene
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Metals in Synthesis
z0625
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0625
Zirconium-Catalyzed Asymmetric β-Oxygen Elimination for the Desymmetrization of
meso
-Ketene Acetals
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0626
Nickel-Catalyzed, Three-Component Silylalkylation and -Benzylation of Alkenes using Silylzinc Pivalates
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0627
Biocatalytic Enantioselective 1-Carbon Ring Expansion via 1,2-Stevens Rearrangement
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0628
Copper-Catalyzed Asymmetric Dynamic Kinetic C–P Coupling
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0629
Cobalt-Catalyzed Aryl Cyanation of Symmetric Alkynes to Access
E
- and
Z
-Acrylonitriles
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0630
Ni-Catalyzed Cyanation of Aryl Halides Using 1,4-Dicyanobenzene as an Easily Accessible Cyanide Source
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0631
Pd-Catalyzed Deoxygenative Allylation and Olefination of Carbohydrates by an Umpolung Strategy
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0632
NHCs as Remote Controls: Access to Isoindolines and β-Lactams via Pd-Catalyzed Remote C–H Functionalization
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0633
Rhodium-Catalyzed Synthesis of Indanones via Ring Expansion of Benzocyclobutenones
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0634
Dual NHC/Photocatalytic Dearomative Acyl Fluorination Reaction of Benzofurans
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0635
Pd-Catalyzed Cross-Electrophile Coupling of Benzyl- and (Hetero)Arylbromides without External Reductant
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0636
Selective Pd-Catalyzed β- and γ-C(sp
3
)–H Arylation of Aldehydes Enabled by Transient Directing Groups
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0637
Cobalt- and Iridium-Catalyzed Mizoroki–Heck Reaction of Imidates Enabled by Energy and Electron Transfer
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0638
Palladium-Catalyzed Synthesis of Chiral
gem
-Difluoromethylene-Containing 1,3-Dioxanes
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0639
Rhodium-Catalyzed Transfer C−H Borylation of Alkenes with Vinyl Boronic Esters
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0640
The A-Team: Iridium-Catalyzed Asymmetric Allylic Alkylation of Azaarenes (AAAA)
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0641
Enantioselective Intramolecular Ir-Catalyzed Allylic Substitution Generating 8–11-Membered Lactones
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0642
One-Carbon Homologation of Aryl Ketones via Formal 1,1-Insertion of Olefins via Rh-Catalyzed ‘Cut and Sew’
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0643
Accessing Diamines from Free Amines via Nickel-Catalyzed Olefin Difunctionalization
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0644
Deaminative Allylation of Katritzky Pyridinium Salts by Dual Cobalt/Organophotoredox Catalysis
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0645
Triple Catalysis Enables the Preparation of Aromatic Aldehydes by a Desaturative Strategy
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0646
Access to Chiral
N
-Alkylanilines by Enantioconvergent Alkylation with Racemic Tertiary Alkyl Electrophiles
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0647
Desymmetrization of Malononitriles by Intramolecular Nickel-Catalyzed Reductive Cross-Coupling
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0648
Ligand-Controlled Regiodivergent Asymmetric Cu-Catalyzed Carbonyl Addition of Vinyl Heteroarenes
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0649
The Perfect
Co
uple: Dehydrogenative Ring-Opening of Cycloalkanols by Cobalt/Organophotoredox Catalysis
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0650
Catalyst-Controlled Regiodivergent Transformations of Internal Propargyl Esters
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0651
The Narasaka–Heck Cyclization
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Polymer-Supported Synthesis
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0653
Acceptorless Alcohol Dehydrogenation with an Iron–Cobalt Double-Atom Catalyst
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0654
Photocatalytic Synthesis of Trisubstituted Pyridines with Vinylene-Linked Covalent Organic Frameworks
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0655
Borrowing-Hydrogen Reaction Catalyzed by Iridium on a Porous Polypyridine-Oxadiazole
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0656
Palladium-Catalyzed Benzylic Oxidation of Alkylarenes with Water as an Oxygen Source
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0657
Meerwein–Ponndorf–Verley Reduction on Zirconium(IV) Coordinated to Amberlyst-15
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0658
Photocatalytic Giese-Type Reaction on a Truxene-Based Hypercrosslinked Polymer
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0659
Intermolecular [2+2] Photocycloadditions of Aromatic Alkenes Promoted by CdSe Quantum Dots
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0660
PdAu/g-C
3
N
4
-Catalyzed Hydrodeoxygenation of Benzaldehydes with Formic Acid as a Hydrogen Donor
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0661
Three-Component Regioselective Cycloaddition by a Copper Single-Atom Catalyst Supported on C
3
N
4
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0662
Hydrophosphinylation of Alkenes Catalyzed by Single-Atom Copper on Aluminum-Doped Magnesia
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0663
Carboxylation of Sodium Arylsulfinates with CO
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on a Potassium–Copper–Titania Composite
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Organo- and Biocatalysis
z0665
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0665
Modified Flavins Permit Catalytic Reductive Cyclization
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0666
Organocatalytic Enantioselective Cascade Process for Constructing Azabicyclo[3.3.1]nonane Scaffolds
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0667
Atroposelective Synthesis of
N
-Arylindoles by Brønsted Acid-Catalyzed Cyclization of Ynamides
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0668
An Organocatalytic Approach for Remote C(sp
3
)−H Bond Hydroxylation
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0669
Biocatalytic Synthesis of Azetidines by Enantioselective [1,2]-Stevens Rearrangement of Aziridines
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0670
Biocatalytic Decarboxylative Bromination of Electron-Rich Cinnamic Acids
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0671
Hypoiodite Permits Enantioselective Dearomatization of Indoles
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0672
Biaryl Bond Formation Enabled by Biocatalytic Oxidative Cross-Coupling Reactions
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0673
Photoredox Organocatalytic Enantioselective Synthesis of 1,7-Dicarbonyl Compounds via γ-Keto Radicals
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0674
Dual Carbene and Photoredox Catalysis Permits Tandem Cyclization to Cyclic Benzylic Ketones
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0675
Organocatalytic Hydrogen Atom Transfer System for C−H Functionalization
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0676
Friedel–Crafts Polymerization Approach to Easily Recyclable Heterogeneous Chiral Phosphoric Acids
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Chemistry in Medicine and Biology
z0677
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0677
Targeted Protein Stabilization with DUBTACs
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0678
Take it Easy on the Synthesis of Cannabidiol Derivatives
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0679
Spatiotemporal Labeling Through Photocatalytic Oxidation of Dihydrotetrazines
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0680
Acyl Silanes: The Newest Photoaffinity Labeling Probe
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0681
LZ-2112 – A Diterpene that Potentiates Antibiotics
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0682
A Dual Inhibitor as a Potential Treatment for Alzheimer’s Disease
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0683
Scalable Synthesis of a Payload for Antibody–Drug Conjugate Studies
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0684
Sweet Mannose Antibiotic: Stereoselective Synthesis and Stereochemical Assignment of A-94964
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0685
Potent Anti-Gastric Cancer Alkaloids from Traditional Medicine
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0686
Live-Cell Imaging of Glycosidase Activity Using Bis-Acetal-Based Fluorogenic Probes
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0687
Enlightening a Radical: A Convergent Total Synthesis of (+)-Actinobolin and Potent Analogues
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0688
Synthesis of the Potent Antibiotic Amycolamicin
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0689
First Asymmetric Synthesis of (+)-Thienamycin
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0690
Evaluation of Benzopyrrolizidinone Pharmacophores Against NMDA-Induced Nerve Cell Injury
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Peptide Chemistry
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0691
Dipeptide Synthesis by Two-Component Organocatalysis
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0692
Site-Selective Alkylation for the Synthesis of Azapeptides
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0693
Urethane-Protected Amino Acid
N
-Carboxyanhydride Synthesis in a Microflow System
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0694
Nickel-Catalyzed Enantioselective Synthesis of Unnatural Amino Acids
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0695
C–H Azidation of Peptides and Applications of the Products
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0696
Arene Triazene Reaction for Macrocyclization of Unprotected Peptides
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0697
Ruthenium-Catalyzed Synthesis of Unnatural Amino Acids through Transfer Hydrogenation of Enamides
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0698
Iridium-Catalyzed N-Alkylation of α-Amino Esters and Amides
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0699
Synthesis of Versatile N-Protected Amino Acid Esters from Aryl 4-Nitrosulfonates
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0700
Construction of
N
,
O
-Acetals of Unnatural Amino Acids from Diethyl Mesoxalate Derivatives
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Flow Chemistry
z0701
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0701
Synthesis of (
R
)-Tamsulosin Using Heterogeneous Catalysis in Flow
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0702
Amide Bond Formation under Flow Conditions
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