Late-stage C–H functionalization offers new opportunities in drug discovery

L Guillemard, N Kaplaneris, L Ackermann… - Nature Reviews …, 2021 - nature.com
Over the past decade, the landscape of molecular synthesis has gained major impetus by
the introduction of late-stage functionalization (LSF) methodologies. C–H functionalization …

Trifluoromethoxylation reactions of (hetero) arenes, olefinic systems and aliphatic saturated substrates

S Barata‐Vallejo, SM Bonesi… - Chemistry–A European …, 2022 - Wiley Online Library
Direct fluoroalkoxylation reactions of (hetero) arenes, carbon‐carbon multiple bonds, and
substitution reactions at Csp3 carbon centers by CF3O, CHF2O, and (CF3) 2CFO groups are …

Carbene-catalyzed chemoselective reaction of unsymmetric enedials for access to Furo [2, 3-b] pyrroles

G Fan, Q Wang, J Xu, P Zheng, YR Chi - Nature Communications, 2023 - nature.com
A carbene-catalyzed chemoselective reaction of unsymmetric enedials is disclosed. The
reaction provides a concise access to bicyclic furo [2, 3-b] pyrroles derivatives in excellent …

[HTML][HTML] Diversification of pharmaceutical molecules via late-stage C (sp2)–H functionalization

W Shang, H Sun, W Chen, J Liu - Green Synthesis and Catalysis, 2023 - Elsevier
C–H late-stage functionalization has gradually become a powerful approach for the rapid
optimization of lead compounds' bioactivity. Significant advances in this field have been …

Review and Theoretical Analysis of Fluorinated Radicals in Direct CAr−H Functionalization of (Hetero)arenes

AJ Fernandes, R Giri, KN Houk… - Angewandte Chemie, 2024 - Wiley Online Library
We highlight key contributions in the field of direct radical CAr− H (hetero) aromatic
functionalization involving fluorinated radicals. A compilation of Functional Group Transfer …

Electrochemical Trifluoromethoxylation of (Hetero) aromatics with a Trifluoromethyl Source and Oxygen

Y Ouyang, XH Xu, FL Qing - Angewandte Chemie International …, 2022 - Wiley Online Library
Trifluoromethoxylated aromatics (ArOCF3) are valuable structural motifs in the area of drug
discovery due to the enhancement of their desired physicochemical properties upon the …

Photoinitiated anti‐Hydropentafluorosulfanylation of Terminal Alkynes

M Birepinte, PA Champagne, JF Paquin - Angewandte Chemie, 2022 - Wiley Online Library
A photoinitiated anti‐hydropentafluorosulfanylation of terminal alkynes using SF5Cl and
(TMS) 3SiH as the hydrogen atom donor is reported. This transformation generates …

An update on late-stage functionalization in today's drug discovery

AP Montgomery, JM Joyce, JJ Danon… - Expert Opinion on Drug …, 2023 - Taylor & Francis
Introduction Late-stage functionalization (LSF) allows for the introduction of new chemical
groups toward the end of a synthetic sequence, which means new molecules can be rapidly …

Catalyst‐Free Trifluoromethoxylation of Silyl Enol Ethers and Allyl Silanes with Bis (trifluoromethyl) peroxide

LM Maas, C Fasting, P Voßnacker… - Angewandte Chemie …, 2024 - Wiley Online Library
Radical trifluoromethoxylation is an attractive approach to prepare compounds featuring the
important OCF3 group, however most existing methods have focused on aromatic …

Development and application of trifluoromethoxylating reagents

Y Si, P Tang - Chinese Journal of Chemistry, 2023 - Wiley Online Library
Comprehensive Summary The trifluoromethoxy functional group has received increasing
attention in recent years due to its distinctive properties such as good metabolic stability …