Three-dimensional saturated C(sp3)-rich bioisosteres for benzene

J Tsien, C Hu, RR Merchant, T Qin - Nature Reviews Chemistry, 2024 - nature.com
Benzenes, the most ubiquitous structural moiety in marketed small-molecule drugs, are
frequently associated with poor 'drug-like'properties, including metabolic instability, and poor …

A general three-component alkyl petasis boron–mannich reaction

C Hu, J Tsien, SJ Chen, M Kong… - Journal of the …, 2024 - ACS Publications
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 …

Electrochemical deoxygenative amination of stabilized alkyl radicals from activated alcohols

J Xu, Y Liu, Q Wang, X Tao, S Ni, W Zhang, L Yu… - Nature …, 2024 - nature.com
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 …

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 …

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 …

CF3-Cyclobutanes: Synthesis, Properties, and Evaluation as a Unique tert-Butyl Group Analogue

V Ahunovych, AA Klipkov, M Bugera, K Tarasenko… - JACS Au, 2024 - ACS Publications
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 …

Isosteric 3D Bicyclo [1.1. 1] Pentane (BCP) Core-Based Lipids for mRNA Delivery and CRISPR/Cas Gene Editing

S Wu, Y Yang, X Lian, F Zhang, C Hu… - Journal of the …, 2024 - ACS Publications
Lipid nanoparticles (LNPs) are an essential component of messenger RNA (mRNA)
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 …

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 …

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 …