Recent progress in synthetic applications of hypervalent iodine (III) reagents

A Yoshimura, VV Zhdankin - Chemical Reviews, 2024 - ACS Publications
Hypervalent iodine (III) compounds have found wide application in modern organic
chemistry as environmentally friendly reagents and catalysts. Hypervalent iodine reagents …

[HTML][HTML] Late-stage modification of bioactive compounds: Improving druggability through efficient molecular editing

T Huo, X Zhao, Z Cheng, J Wei, M Zhu, X Dou… - … Pharmaceutica Sinica B, 2024 - Elsevier
Synthetic chemistry plays an indispensable role in drug discovery, contributing to hit
compounds identification, lead compounds optimization, candidate drugs preparation, and …

Regioselective, catalytic 1, 1-difluorination of enynes

ZX Wang, K Livingstone, C Hümpel, CG Daniliuc… - Nature Chemistry, 2023 - nature.com
Fluorinated small molecules are prevalent across the functional small-molecule spectrum,
but the scarcity of naturally occurring sources creates an opportunity for creative endeavour …

Catalytic hydrodifluoroalkylation of unactivated olefins

WJ Yue, CS Day, AJ Brenes Rucinski, R Martin - Organic Letters, 2022 - ACS Publications
Herein, we report a modular catalytic technique that streamlines the preparation of gem-
difluoroalkanes from unactivated sp 3 precursors. The method is characterized by its …

Skeletal Ring Contractions via I(I)/I(III) Catalysis: Stereoselective Synthesis of cis-α,α-Difluorocyclopropanes

K Livingstone, K Siebold, S Meyer, V Martín-Heras… - ACS …, 2022 - ACS Publications
The clinical success of α, α-difluorocyclopropanes, combined with limitations in the existing
synthesis portfolio, inspired the development of an operationally simple, organocatalysis …

Expanding organofluorine chemical space: the design of chiral fluorinated isosteres enabled by I (I)/I (III) catalysis

S Meyer, J Häfliger, R Gilmour - Chemical Science, 2021 - pubs.rsc.org
Short aliphatic groups are prevalent in bioactive small molecules and play an essential role
in regulating physicochemistry and molecular recognition phenomena. Delineating their …

Regio‐and Enantioselective Intermolecular Aminofluorination of Alkenes via Iodine (I)/Iodine (III) Catalysis

M Schäfer, T Stünkel, CG Daniliuc… - Angewandte Chemie …, 2022 - Wiley Online Library
The regio‐and enantio‐selective, intermolecular vicinal fluoroamination of α‐trifluoromethyl
styrenes has been achieved by enantioselective II/IIII catalysis. Leveraging C2‐symmetric …

Catalytic, Regioselective 1, 4‐Fluorodifunctionalization of Dienes

YJ Yu, M Schäfer, CG Daniliuc… - Angewandte Chemie, 2023 - Wiley Online Library
Abstract A catalysis‐based regioselective 1, 4‐fluorofunctionalization of trifluoromethyl
substituted 1, 3‐dienes has been developed to access compact, highly functionalized …

Integrating I(I)/I(III) catalysis in reaction cascade design enables the synthesis of gem-difluorinated tetralins from cyclobutanols

J Häfliger, L Ruyet, N Stübke, CG Daniliuc… - Nature …, 2023 - nature.com
Partially saturated, fluorine-containing rings are ubiquitous across the drug discovery
spectrum. This capitalises upon the biological significance of the native structure and the …

Catalytic Ring Expanding Difluorination: An Enantioselective Platform to Access β, β‐Difluorinated Carbocycles

L Ruyet, C Roblick, J Häfliger, ZX Wang… - Angewandte Chemie …, 2024 - Wiley Online Library
Cyclic β, β‐difluoro‐carbonyl compounds have a venerable history as drug discovery leads,
but limitations in the synthesis arsenal continue to impede chemical space exploration. This …