Fluoride-Catalyzed Cross-Coupling of Carbamoyl Fluorides and Alkynylsilanes

Article Chemistry, Multidisciplinary

Enantioselective Synthesis of α-Alkenylated γ-Lactam Enabled by Ni-Catalyzed 1,4-Arylcarbamoylation of 1,3-Dienes

Feng He et al.

Summary: This article reports a new method for the synthesis of chiral quaternary alpha-alkenylated pyrrolidinones through nickel-catalyzed asymmetric 1,4-arylcarbamoylation. This method has significant importance in organic synthesis.

CCS CHEMISTRY (2023)

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Article Chemistry, Multidisciplinary

BF3-Catalyzed Intramolecular Fluorocarbamoylation of Alkynes via Halide Recycling

E. Ali McKnight et al.

Summary: A BF3-catalyzed atom-economical fluorocarbamoylation reaction was reported, which enables the insertion of alkynes into strong C-F bonds through a halide recycling mechanism. The developed method provides stereoselective access to 3-(fluoromethylene) oxindoles and gamma-lactams, including fluorinated derivatives of known protein kinase inhibitors. Experimental and computational studies support a stepwise mechanism for the fluorocarbamoylation reaction involving a cyclization step followed by internal fluoride transfer.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2023)

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Article Chemistry, Multidisciplinary

Cover Feature: Study of Carbamoyl Fluoride: Synthesis, Properties and Applications (Chem. Eur. J. 43/2022)

Clémence Bonnefoy et al.

CHEMISTRY-A EUROPEAN JOURNAL (2022)

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Article Chemistry, Organic

Synthesis of Carbamoyl Fluorides Using a Difluorophosgene Surrogate Derived from Difluorocarbene and Pyridine N-Oxides

Dusty Cadwallader et al.

Summary: This article introduces a method for synthesizing carbamoyl fluorides, which uses inexpensive and easily accessible starting materials, avoids the use of light-, temperature-, and moisture-sensitive chemicals, and has practical advantages over existing methods.

JOURNAL OF ORGANIC CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Selective inhibitors of JAK1 targeting an isoform-restricted allosteric cysteine

Madeline E. Kavanagh et al.

Summary: This study identified a novel allosteric approach for selectively inhibiting JAK1 with unprecedented isoform selectivity, while acting as 'silent' ligands for TYK2.

NATURE CHEMICAL BIOLOGY (2022)

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Article Chemistry, Applied

Palladium-Catalyzed 5-exo-dig Cyclization Cascade, Sequential Amination/Etherification for Stereoselective Construction of 3-Methyleneindolinones

Youpeng Zuo et al.

Summary: A cascade intramolecular 5-exo-dig cyclization of N-(2-iodophenyl)propiolamides and sequential amination/etherification protocol has been developed for the synthesis of amino- and phenoxy-substituted 3-methyleneindolinones using inexpensive Pd(PPh3)(4) as catalyst. The protocol allows for the assembly of oxindole cores with moderate functional group tolerance, providing a broad spectrum of products with diverse substituents in good to excellent yields.

ADVANCED SYNTHESIS & CATALYSIS (2021)

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Article Biotechnology & Applied Microbiology

Trends in peptide drug discovery

Markus Muttenthaler et al.

Summary: This Perspective summarizes key trends in peptide drug discovery and development, including human hormones, elegant medicinal chemistry and rational design strategies, peptide drugs derived from nature, and major breakthroughs in molecular biology and peptide chemistry. It also emphasizes lessons from earlier approaches that are still relevant today and discusses emerging strategies impact on peptide drug discovery.

NATURE REVIEWS DRUG DISCOVERY (2021)

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Article Biochemistry & Molecular Biology

Design, synthesis and evaluation of cinnamic acid hybrids as multi-target-directed agents for the treatment of Alzheimer's disease

Keren Wang et al.

Summary: The novel cinnamic acid hybrid compound 4e, combining 1,2,3,4-tetrahydroisoquinoline and benzylpiperidine groups, showed promising multi-targeted therapeutic activity for Alzheimer's disease (AD) through reversible enzyme inhibition, antioxidant properties, and inhibition of protein aggregation, among other mechanisms.

BIOORGANIC CHEMISTRY (2021)

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Article Chemistry, Multidisciplinary

Synthesis of N-CF3 Alkynamides and Derivatives Enabled by Ni-Catalyzed Alkynylation of N-CF3 Carbamoyl Fluorides

Christian D. -T. Nielsen et al.

Summary: The study reported a synthetic method for N-trifluoromethyl alkynamides and found that this synthetic compound can serve as a platform to unlock access to other valuable derivatives.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

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Article Chemistry, Multidisciplinary