An overview of late-stage functionalization in today's drug discovery

M Moir, JJ Danon, TA Reekie… - Expert Opinion on Drug …, 2019 - Taylor & Francis
Introduction: Late-stage functionalization (LSF) can introduce important chemical groups in
the very last steps of the synthesis. LSF has the potential to speed up the preparation of …

Hydroaminoalkylation for the catalytic addition of amines to alkenes or alkynes: diverse mechanisms enable diverse substrate scope

RC DiPucchio, SC Rosca… - Journal of the American …, 2022 - ACS Publications
Hydroaminoalkylation is a powerful, atom-economic catalytic reaction for the reaction of
amines with alkenes and alkynes. This C–H functionalization reaction allows for the atom …

Enantioselective alkylation of α-amino C(sp3)−H bonds via photoredox and nickel catalysis

J Li, B Cheng, X Shu, Z Xu, C Li, H Huo - Nature Catalysis, 2024 - nature.com
The catalytic enantioselective construction of C (sp 3)− C (sp 3) bonds remains a substantial
challenge in organic synthesis. One particularly promising approach is the use of transition …

Photomediated ring contraction of saturated heterocycles

J Jurczyk, MC Lux, D Adpressa, SF Kim, Y Lam… - Science, 2021 - science.org
Saturated heterocycles are found in numerous therapeutics and bioactive natural products
and are abundant in many medicinal and agrochemical compound libraries. To access new …

Site- and enantioselective cross-coupling of saturated N-heterocycles with carboxylic acids by cooperative Ni/photoredox catalysis

X Shu, D Zhong, Q Huang, L Huan, H Huo - Nature Communications, 2023 - nature.com
Site-and enantioselective cross-coupling of saturated N-heterocycles and carboxylic acids—
two of the most abundant and versatile functionalities—to form pharmaceutically relevant α …

Organocatalytic C− H Functionalization of Simple Alkanes

F Su, F Lu, K Tang, X Lv, Z Luo, F Che… - Angewandte …, 2023 - Wiley Online Library
The direct functionalization of inert C (sp3)‐H bonds to form carbon‐carbon and carbon‐
heteroatom bonds offers vast potential for chemical synthesis and therefore receives …

Deconstructive diversification of cyclic amines

JB Roque, Y Kuroda, LT Göttemann, R Sarpong - Nature, 2018 - nature.com
Deconstructive functionalization involves carbon–carbon (C–C) bond cleavage followed by
bond construction on one or more of the constituent carbons. For example, ozonolysis and …

High-throughput synthesis provides data for predicting molecular properties and reaction success

J Götz, MK Jackl, C Jindakun, AN Marziale, J André… - Science …, 2023 - science.org
The generation of attractive scaffolds for drug discovery efforts requires the expeditious
synthesis of diverse analogues from readily available building blocks. This endeavor …

Organogel delivery vehicles for the stabilization of organolithium reagents

P Slavík, BR Trowse, P O'Brien, DK Smith - Nature Chemistry, 2023 - nature.com
Organolithium reagents are a vital tool in modern organic chemistry, enabling the synthesis
of carbon–carbon bonds. However, due to their high reactivity, low temperatures, inert …

N‐atom deletion in nitrogen heterocycles

H Qin, W Cai, S Wang, T Guo, G Li… - Angewandte Chemie, 2021 - Wiley Online Library
Excising the nitrogen in secondary amines, and coupling the two residual fragments is a
skeletal editing strategy that can be used to construct molecules with new skeletons, but …