Three-dimensional saturated C(sp3)-rich bioisosteres for benzene
Benzenes, the most ubiquitous structural moiety in marketed small-molecule drugs, are
frequently associated with poor 'drug-like'properties, including metabolic instability, and poor …
frequently associated with poor 'drug-like'properties, including metabolic instability, and poor …
A general three-component alkyl petasis boron–mannich reaction
Aryl amines are one of the most common moieties in biologically active molecules, and
approximately 37% of drug candidates contain aromatic amines. Recent advancements in …
approximately 37% of drug candidates contain aromatic amines. Recent advancements in …
Electrochemical deoxygenative amination of stabilized alkyl radicals from activated alcohols
Alkylamine structures represent one of the most functional and widely used in organic
synthesis and drug design. However, the general methods for the functionalization of the …
synthesis and drug design. However, the general methods for the functionalization of the …
Taming of Furfurylidenes by Chiral Bismuth‐Rhodium Paddlewheel Catalysts. Preparation and Functionalization of Optically Active 1, 1‐Disubstituted (Trifluoromethyl) …
M Peeters, J Decaens, A Fürstner - … Chemie International Edition, 2023 - Wiley Online Library
Abstract Although 2‐furyl‐carbenes (furfurylidenes) are prone to instantaneous electrocyclic
ring opening, chiral [BiRh]‐paddlewheel complexes empowered by London dispersion …
ring opening, chiral [BiRh]‐paddlewheel complexes empowered by London dispersion …
Photocatalytic O‐ to S‐Rearrangement of Tertiary Cyclopropanols
JJ Monteith, JW Pearson… - Angewandte Chemie …, 2024 - Wiley Online Library
Despite the importance of heteroatom‐substituted cyclopropane derivatives in drug design
and organic synthesis, cyclopropanethiols remain critically underexplored. Inspired by the …
and organic synthesis, cyclopropanethiols remain critically underexplored. Inspired by the …
CF3-Cyclobutanes: Synthesis, Properties, and Evaluation as a Unique tert-Butyl Group Analogue
Isosteric replacement of functional groups is an emerging strategy for optimizing bioactive
molecules in drug discovery. tert-Butyl group is a particularly important moiety, yet its …
molecules in drug discovery. tert-Butyl group is a particularly important moiety, yet its …
Isosteric 3D Bicyclo [1.1. 1] Pentane (BCP) Core-Based Lipids for mRNA Delivery and CRISPR/Cas Gene Editing
Lipid nanoparticles (LNPs) are an essential component of messenger RNA (mRNA)
vaccines and genome editing therapeutics. Ionizable amino lipids, which play the most …
vaccines and genome editing therapeutics. Ionizable amino lipids, which play the most …
Photoinduced Formation of Cubyl Aryl Thioethers and Synthesis of Monocubyl Analogue of Dapsone
L Donnier-Valentin, S Kassamba, J Legros… - Organic …, 2023 - ACS Publications
1, 4-Disubstituted cubyl aryl thioethers were generated from the corresponding iodocubanes
and aryl thiolates upon UV irradiation in dimethyl sulfoxide at room temperature. This simple …
and aryl thiolates upon UV irradiation in dimethyl sulfoxide at room temperature. This simple …
Direct Introduction of the 1‐Fluorocyclopropyl Group via Stille Cross‐Coupling – A Way of Getting Around Per‐ and Polyfluoroalkyl Substances (PFASs)
F Audet, M Donnard, A Panossian… - Advanced Synthesis …, 2024 - Wiley Online Library
We are reporting the preparation and use in cross‐coupling reactions of a newly developed,
bench‐stable (1‐fluorocyclopropyl) metalloid reagent. The Stille cross‐coupling reaction …
bench‐stable (1‐fluorocyclopropyl) metalloid reagent. The Stille cross‐coupling reaction …
Palladium-Catalyzed Allylation of Endocyclic 1-Azaallyl Anions
X Yang, B Zhang, J Ruan, K Duanmu… - The Journal of Organic …, 2024 - ACS Publications
Endocyclic 1-azaallyl anions engage allyl acetates in a palladium-catalyzed allylation
followed by reduction to give unprotected 2-(hetero) aryl-3-allylpiperidines and 2-allyl-3 …
followed by reduction to give unprotected 2-(hetero) aryl-3-allylpiperidines and 2-allyl-3 …