Synfacts

Ausgabe 06 · Juni 2022

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A81
Zanda, Matteo: SYNFORM ISSUE 2022/06 FREIER ZUGRIFF

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Synthesis of Natural Products and Potential Drugs
z0579
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0579
Synthesis of Belzutifan FREIER ZUGRIFF

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PDF (139 kb)
0580
Synthesis of Antimalarial INE963

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0581
Total Synthesis of (–)-Grayanotoxin III FREIER ZUGRIFF

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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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PDF (95 kb)
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 FREIER ZUGRIFF

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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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PDF (86 kb)
0601
Regioselective Functionalization of Azoles

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0602
C2-Selective S_NH 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_NV 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 FREIER ZUGRIFF

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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 FREIER ZUGRIFF

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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 FREIER ZUGRIFF

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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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PDF (98 kb)
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(sp³)–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 Couple: 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 FREIER ZUGRIFF

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Polymer-Supported Synthesis
z0653
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0653
Acceptorless Alcohol Dehydrogenation with an Iron–Cobalt Double-Atom Catalyst FREIER ZUGRIFF

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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-C₃N₄-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 C₃N₄

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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 CO₂ 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 FREIER ZUGRIFF

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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(sp³)−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 FREIER ZUGRIFF

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PDF (149 kb)
0678
Take it Easy on the Synthesis of Cannabidiol Derivatives

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PDF (78 kb)
0679
Spatiotemporal Labeling Through Photocatalytic Oxidation of Dihydrotetrazines

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PDF (186 kb)
0680
Acyl Silanes: The Newest Photoaffinity Labeling Probe

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PDF (84 kb)
0681
LZ-2112 – A Diterpene that Potentiates Antibiotics

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PDF (110 kb)
0682
A Dual Inhibitor as a Potential Treatment for Alzheimer’s Disease

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PDF (86 kb)
0683
Scalable Synthesis of a Payload for Antibody–Drug Conjugate Studies

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PDF (92 kb)
0684
Sweet Mannose Antibiotic: Stereoselective Synthesis and Stereochemical Assignment of A-94964

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PDF (99 kb)
0685
Potent Anti-Gastric Cancer Alkaloids from Traditional Medicine

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PDF (85 kb)
0686
Live-Cell Imaging of Glycosidase Activity Using Bis-Acetal-Based Fluorogenic Probes

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PDF (95 kb)
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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PDF (90 kb)
0689
First Asymmetric Synthesis of (+)-Thienamycin FREIER ZUGRIFF

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PDF (136 kb)
0690
Evaluation of Benzopyrrolizidinone Pharmacophores Against NMDA-Induced Nerve Cell Injury

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Peptide Chemistry
z0691
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PDF (363 kb)
0691
Dipeptide Synthesis by Two-Component Organocatalysis FREIER ZUGRIFF

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PDF (117 kb)
0692
Site-Selective Alkylation for the Synthesis of Azapeptides

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PDF (71 kb)
0693
Urethane-Protected Amino Acid N-Carboxyanhydride Synthesis in a Microflow System

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PDF (93 kb)
0694
Nickel-Catalyzed Enantioselective Synthesis of Unnatural Amino Acids

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PDF (71 kb)
0695
C–H Azidation of Peptides and Applications of the Products

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PDF (73 kb)
0696
Arene Triazene Reaction for Macrocyclization of Unprotected Peptides

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PDF (88 kb)
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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PDF (94 kb)
0699
Synthesis of Versatile N-Protected Amino Acid Esters from Aryl 4-Nitrosulfonates FREIER ZUGRIFF

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PDF (129 kb)
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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PDF (73 kb)
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