Synfacts

Issue 05 · May 2022

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Synform
A68
SYNFORM ISSUE 2022/05
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Synthesis of Natural Products and Potential Drugs
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0457
Synthesis of a Human Immunodeficiency Virus Maturation Inhibitor

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0458
Synthesis of GSK973

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0459
Synthesis of Four Kopsane Alkaloids
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0460
Synthesis of (–)-Jimenezin

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0461
Synthesis of Molibresib
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0462
Total Synthesis of Erectones A and B

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0463
Total Synthesis of (+)-Hyperforin and (+)-Pyrohyperforin

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0464
Synthesis of (+)-Euphorikanin A

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0465
Synthesis of BMS-813160

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0466
Synthesis of Orexin Receptor Antagonist YZJ-1139

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0467
Total Synthesis of (–)-Exiguolide

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0468
Synthesis of an Adaptor-Associated Kinase 1 Inhibitor

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0469
Synthesis of (±)-Emtricitibine

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0470
One-Pot Synthesis of Molnupiravir from Cytidine

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0471
Synthesis of Foscarbidopa

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0472
Synthesis of GDC-0134

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0473
Total Synthesis of (±)-Reserpine
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Synthesis of Heterocycles
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0475
New Silaazacycles: Syntheses of 1,3,5-Diazasilinan-2-ones and 1,3,5-Thiazasilinan-2-imines

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0476
Synthesis of Fluoroalkylated Benzimidazole- or Indole-Fused Benzoxazines

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0477
One-Pot Transition-Metal-Free Synthesis of Thiadiazine 1-Oxides

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0478
Modular Access to Functionalized Pyrroles

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0479
Copper Photocatalyzed Synthesis of Heterocycles

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0480
Synthesis of Bioactive Fluoropyrrolidines through 1,3-Dipolar Cycloadditions of Azomethine Ylides

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0481
Stereoselective Synthesis of Sulfinate Esters via a Chiral Ion Pair

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0482
Synthesis of 1,2,4-Thiadiazoles in Ethanol at Room Temperature by Using Hydrogen Peroxide

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0483
Synthesis of Novel Isoxazoloazaborines from 4-N-Propargylaminoisoxazoles

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0484
Enhanced Potency and Properties by Exploiting Substituted Oxetane as a Cyclobutane Bioisostere

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0485
Synthesis of Triazolopyridines with Nitrous Oxide

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0486
Electrochemical Syntheses of Substituted Morpholine Derivatives

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0487
Heteroaromatic C–H Etherification by Using (Benzo)thiophene-Based Halogen-Transfer Reagents

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0488
Access to Densely Substituted Furans by a Tsuji–Wacker-Type Cyclization

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0489
Expanding Substrate Scope of the Chemoenzymatic Functionalization of Tetrahydroisoquinolines

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Synthesis of Materials and Unnatural Products
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0491
Surpassing Sumanene with Ring Expansion

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0492
Buckybowl Waterwheels

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0493
Transcending Benzoborirene Instability

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0494
Building Silacyclohexanones from Divinylsilanes and Allylamines via Rh-Catalyzed Cyclization

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0495
Chemoselective Synthesis of Sulfenylated Spiroindolenines from Indolyl-ynones

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0496
Upcycling Polyethylene with Mi(tsunobu)das Touch

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0497
Closing the Ring with Hydrazine to Make PHAs

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0498
Jumbo Calixarene Ligands

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0499
Synthesis of Armchair- and Chiral-Type Belts

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0500
Queueing Up Cumulenes with Copper Catalysis

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0501
Fold-in Approach for Curved Heteronanographene

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0502
Through-Space Conjugation to (Violo)generate Longer-Lived Charge Separation

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Metals in Synthesis
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0503
An Alternative to Norbornene: Unstrained Alkene Ligands with a Coordination Site for Catellani Reactions
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0504
Iridium-Catalyzed Hydroiodination and Formal Hydroamination with N-Iodo Reagents and Hydrogen

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0505
General Strategy for the Synthesis of Rare Sugars via Ru(II)-Catalyzed and Boron-Mediated Selective Epimerization of 1,2-trans-Diols to 1,2-cis-Diols
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0506
Enantioselective Reductive Coupling of Dienes with Oxetanones and N-Acyl-Azetidinones

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0507
Iron Made It: Asymmetric Oxidative Cross-Coupling of 2-Naphthols with 2-Aminonaphthalenes

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0508
Asymmetric Allenylation of β-Keto Esters via Cooperative Palladium/Brønsted Acid Catalysis

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0509
Iridium-Catalyzed Reductive Alkylation of Amides for the Synthesis of α-Difluoroalkylated Amines

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0510
Preparation of α,β-Unsaturated Ketones by Nickel-Catalyzed Reductive Hydroacylation of Alkynes

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0511
Palladium-Catalyzed Hydrohalogenation of Terminal and Internal Alkenes under Chain-Walking

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0512
Asymmetric Hydrogenation/Cyclization Cascade of Aliphatic Ketoacids: Access to Chiral Lactones

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0513
Copper-Catalyzed Cross-Coupling of Alkyl Iodides and Organoboronates via Halogen-Atom Transfer

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0514
Acetate-Assisted Thioetherification of Aryl Chlorides under Nickel Catalysis

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0515
Nickel/Photoredox Dual-Catalytic Reductive Cross-Coupling of α-Bromo Phosphonates

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0516
Rhodium-Catalyzed Enantioselective Ring Expansion of Azetidines

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0517
Enantioselective Cross-Coupling of Alkenyl Boronates and Carbamoyl Chlorides

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0518
Access to Chiral Tertiary Alkyl Halides by Catalytic Reductive Desymmetrization of Malonic Esters

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0519
Synthesis of Skipped Dienes and Vinylcyclopropanes by Pd-Catalyzed Cross-Coupling of Alkenyl Hydrazones

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0520
Directed Allene C(sp²)−H Activation Catalyzed by Palladium

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0521
Cooperative Stereoinduction in Asymmetric Photocatalysis

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0522
Enantioselective Copper-Catalyzed Cyanobenzoyldifluoromethylation of Olefins

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0523
Where to Go? Selective 1,2- or 1,4-Diarylation of 1,3-Dienes under Ni/Cr Cocatalysis

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0524
Zinc About It: Highly Regio- and Stereoselective Iron-Catalyzed Alkylzincation of Terminal Alkynes

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0525
Nickel-Catalyzed Cross-Coupling of Aryl Bromides with Aryl Sulfonium Salts

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0526
Peptide Bond Formation via Silacyclic Compounds

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0527
The Enantioselective Overman Rearrangement
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0528
Amino-Acid Promoted Ullmann-Type C–N Coupling
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Polymer-Supported Synthesis
z0529
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0529
Catalytic Hydration/Enantioselective Reductive Amination Cascade Reaction of Propargyl Ethers
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0530
Copper-Catalyzed Synthesis of Aminobenzotriazoles from o-Phenylenediamines

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0531
Photocatalytic Enantioselective α-Benzylation of Aldehydes on a Covalent Organic Framework

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0532
An Iron-Modified Molybdenum-Based Polyoxometalate Catalyst for Direct Amide Synthesis

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0533
Photochemical Hydroxylation of β,γ-Unsaturated Oximes on Carbon Nitride

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0534
Novel Palladium–Zirconia Nanocomposites for the Carbonylative Suzuki–Miyaura Coupling

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0535
Cycloaddition of Carbon Dioxide to Epoxides on N,S Co-Doped Carbon

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0536
A Zinc(II) Catalyst for the Synthesis of Cyclic Carbonates and Cyclic Carbamates from Carbon Dioxide

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0537
Photocatalyzed Oxidative Coupling of Tetrahydroisoquinolines with Carbon Nucleophiles

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0538
Alcohol Ammoxidation Catalyzed by Palladium Nanoparticles under Visible-Light Irradiation

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0539
Arylation of C(sp³)–H Bonds with a Cerium-Based Metal–Organic Framework Catalyst

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Organo- and Biocatalysis
z0541
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0541
Directed Evolution Toward Nonstandard Amino Acids by a Decarboxylative Aldol Reaction
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0542
Synthesis of Cyclobutanes through Enantioselective Intermolecular [2+2] Photocycloadditions

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0543
Engineered Metalloenzymes Permit Enantiodivergent N–H Insertion of Carbenes into Primary Amines

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0544
Design and Application of a Novel Chiral Brønsted C−H Superacid

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0545
Photo- and Organocatalytic Enantioselective Giese-Type Addition to Alkenyl Azaarenes

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0546
Bifunctional Pyridoxal-Catalyzed Asymmetric α-Allylation of Glycinates with Switched Chemoselectivity

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0547
Reagent-Dependent Photoredox-Catalyzed Radical 5-exo and 6-endo Cyclization of Allyloxypyridines

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0548
Pyridinium Umpolung through N-Heterocyclic Carbene Catalysis

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0549
Prolylurea-Catalyzed Pictet–Spengler Reaction of Tryptamine and Keto Amides

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0550
Organophotocatalytic Site-Selective Heteroarylation of Indoles

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0551
A Biocatalytic Cascade Approach to Chiral N-Substi-tuted 1,2-Amino Alcohols from Simple Building Blocks

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0552
Biocatalytic Production of N-Hydroxycytidine

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Chemistry in Medicine and Biology
z0553
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0553
A Wakeup Call for Exhausted CAR T Cells – Targeted Delivery of an Immune Stimulant
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0554
An Alternative Reactivity of Sulfonyl Fluorides

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0555
A Testimony of Hergenrother’s Rule

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0556
Asymmetric Synthesis of Bioactive Lignans and Enantiomeric Antiviral Activity of Niranthin

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0557
Total Synthesis of Two Fusicoccanes Identified Potent Anticancer Activities of a Synthetic Intermediate

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0558
A Photoswitchable Butyrylcholinesterase Inhibitor for Investigating Alzheimer’s Disease

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0559
Fluorogenic Labeling of Nucleic Acids in Living Cells

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0560
Potent and Selective PI3Kδ Inhibitors for the Treatment of Hepatocellular Carcinoma

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0561
Synthesis of a Redshifted Photolabile Protecting Group Based on a NIR Dye via a DFT-Based Design

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0562
Discovery of Non-Nucleotide STING Agonists

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0563
The First Total Synthesis of (±)-Forskolin
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Peptide Chemistry
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0565
Cyclopeptide Synthesis by Ring-Closing Metathesis
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0566
Iridium-Catalyzed Synthesis of α-Amino Esters by α-Amidation

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0567
Synthesis of Fluorine-Containing Amino Acids from Sulfamidates and Potassium Fluoride

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0568
Diastereoselective Allylation of α-Imino Esters for the Synthesis of Sterically Hindered Amino Ester and Peptides

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0569
Copper-Catalyzed Silylamination for the Synthesis of β-Silyl-α-amino Acids

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0570
Enantioselective Synthesis of Unnatural Amino Acids Catalyzed by a Chiral Phosphoric Acid

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0571
Double Mannich Alkylamination to Form Benzofuran-Fused Amino Acid Derivatives

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0572
Trimethoxy(methyl)silane-Mediated Amidation of Carboxylic Acids

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0573
Design and Synthesis of a Thiazolium-Based Coupling Reagent for Peptide Synthesis
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Flow Chemistry
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0575
Alkyl Phosphonate Synthesis in a Continuous-Flow System

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0576
Oxidative Photocyclization of N-Arylenaminones to Indoles in Flow

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0577
Continuous Flow, Cyanide-Free Cyanation Procedure via a Suzuki Coupling, [4+2] retro-[4+2] Sequence

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0578
Efficient Synthesis of AZD4635 using Oxygen in Flow

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