Journal ArticleDOI
The emergence of the C–H functionalization strategy in medicinal chemistry and drug discovery
TLDR
In this paper, the authors discuss the recent trends of C-H activation methodologies such as synthesis of medicinal scaffolds through a cascade of cascade-based activation and activation/annulation cascade, arylation for sp2sp2 and sp2-sp3 cross-coupling, borylation/silylation to introduce a functional linchpin for further manipulation, amination for N-heterocycles and hydrogen bond acceptors, C-h fluorination/fluoroalkylation to tune polarity and lipophilicity, peptide modification andAbout:
This article is published in Chemical Communications.The article was published on 2021-10-19. It has received 31 citations till now. The article focuses on the topics: Peptide modification & Drug discovery.read more
Citations
More filters
Journal ArticleDOI
Recent Advances in Transition-Metal-Catalyzed C–H Alkylation with Three-Membered Rings
Journal ArticleDOI
Native Amides as Enabling Vehicles for Forging sp3–sp3 Architectures via Interrupted Deaminative Ni-Catalyzed Chain-Walking
TL;DR: In this article , an interrupted deaminative Ni-catalyzed chain-walking strategy was proposed to generate sp3-sp3 architectures at remote, yet previously unfunctionalized, methylene sp3 C-H sites enabled by the presence of native amides.
Journal ArticleDOI
Silver‐Free C−H Activation: Strategic Approaches towards Realizing the Full Potential of C−H Activation in Sustainable Organic Synthesis
Arup Mondal,Manuel van Gemmeren +1 more
TL;DR: In this article , the authors present a comparison of silver-based and silver-free methods for C−H activation, focusing on the strategic approaches to develop silver−free methods, and provide the reader with the means to develop sustainable methods.
Journal ArticleDOI
Rh(I)-catalysed imine-directed C-H functionalization via the oxidative [3 + 2] cycloaddition of benzylamine derivatives with maleimides.
Amrita Das,Naoto Chatani +1 more
TL;DR: Mechanistic studies suggest that a zwitterionic intermediate is formed and is a key intermediate through the Rh-catalysed activation of a benzylic C(sp3)-H bond of the imine.
Journal ArticleDOI
Mechanochemical Ruthenium-Catalyzed Ortho-Alkenylation of N-Heteroaryl Arenes with Alkynes under Ball-Milling Conditions.
TL;DR: The mechanochemical, solvent-free Ru(II)-catalyzed alkenylation of N-heteroaryl arenes with alkynes has been successfully described and exhibited excellent functional group compatibility, broad substrate scope, shorter reaction times, and no external heating.
References
More filters
Journal ArticleDOI
Click Chemistry: Diverse Chemical Function from a Few Good Reactions.
TL;DR: In this paper, a set of powerful, highly reliable, and selective reactions for the rapid synthesis of useful new compounds and combinatorial libraries through heteroatom links (C-X-C), an approach called click chemistry is defined, enabled, and constrained by a handful of nearly perfect "springloaded" reactions.
Journal ArticleDOI
Visible Light Photoredox Catalysis with Transition Metal Complexes: Applications in Organic Synthesis
TL;DR: The conversion of these bench stable, benign catalysts to redox-active species upon irradiation with simple household lightbulbs represents a remarkably chemoselective trigger to induce unique and valuable catalytic processes.
Journal ArticleDOI
Fluorine in medicinal chemistry.
TL;DR: This tutorial review provides a sampling of renowned fluorinated drugs and their mode of action with a discussion clarifying the role and impact of fluorine substitution on drug potency.
Journal ArticleDOI
Palladium(II)-catalyzed C-H activation/C-C cross-coupling reactions: versatility and practicality.
TL;DR: A review of palladium-catalyzed coupling of CH bonds with organometallic reagents through a PdII/Pd0 catalytic cycle can be found in this paper.
Journal ArticleDOI
Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals
TL;DR: This review reports on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals, and reports detailed substitution patterns, highlight common architectural cores, and discuss unusual or rare structures.