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 …

C–H deuteration of organic compounds and potential drug candidates

G Prakash, N Paul, GA Oliver, DB Werz… - Chemical Society …, 2022 - pubs.rsc.org
C–H deuteration has been intricately developed to satisfy the urgent need for site-selectively
deuterated organic frameworks. Deuteration has been primarily used to study kinetic isotope …

DNA-encoded chemical libraries: a comprehensive review with succesful stories and future challenges

A Gironda-Martínez, EJ Donckele… - ACS Pharmacology & …, 2021 - ACS Publications
DNA-encoded chemical libraries (DELs) represent a versatile and powerful technology
platform for the discovery of small-molecule ligands to protein targets of biological and …

Palladium-Catalyzed Enantioselective β-C(sp3)–H Activation Reactions of Aliphatic Acids: A Retrosynthetic Surrogate for Enolate Alkylation and Conjugate Addition

EL Lucas, NYS Lam, Z Zhuang, HSS Chan… - Accounts of chemical …, 2022 - ACS Publications
Conspectus Enolate alkylation and conjugate addition into an α, β-unsaturated system have
served as long-standing strategic disconnections for the installation of α-or β-substituents on …

The emergence of the C–H functionalization strategy in medicinal chemistry and drug discovery

R Jana, HM Begam, E Dinda - Chemical Communications, 2021 - pubs.rsc.org
Owing to the market competitiveness and urgent societal need, an optimum speed of drug
discovery is an important criterion for successful implementation. Despite the rapid ascent of …

[HTML][HTML] The expanding reaction toolkit for DNA-encoded libraries

RJ Fair, RT Walsh, CD Hupp - Bioorganic & Medicinal Chemistry Letters, 2021 - Elsevier
Over the past decade, DNA-encoded libraries (DELs) have emerged as a leading platform
for small molecule drug discovery among pharmaceutical companies, biotech companies …

Recent advances in external-directing-group-free C–H functionalization of carboxylic acids without decarboxylation

J Das, DK Mal, S Maji, D Maiti - ACS Catalysis, 2021 - ACS Publications
The selective functionalization of C–H bonds is an extremely important topic in present-day
organic synthesis, as it utilizes the most abundant portion of a molecule as a tool for …

Late-Stage β-C(sp3)–H Deuteration of Carboxylic Acids

A Uttry, S Mal, M van Gemmeren - Journal of the American …, 2021 - ACS Publications
Carboxylic acids are highly abundant in bioactive molecules. In this study, we describe the
late-stage β-C (sp3)–H deuteration of free carboxylic acids. On the basis of the finding that C …

Site‐ and Stereoselective C(sp3)−H Borylation of Strained (Hetero)Cycloalkanols Enabled by Iridium Catalysis

Q Gao, S Xu - Angewandte Chemie International Edition, 2023 - Wiley Online Library
Transition metal‐catalyzed site‐and stereoselective C− H activation of strained (hetero)
cycloalkanes remains a formidable challenge. We herein report a carbamate‐directed …

Functionalization of DNA-tagged alkenes with diazo compounds via photocatalysis

X Fu, J Tang, R Hua, X Li, Z Kang, H Qiu, W Hu - Organic Letters, 2022 - ACS Publications
To explore potential chemical space using DNA-encoded library (DEL) technology, the
development of various types of robust DNA-compatible reactions is urgently needed. Diazo …