An overview of late-stage functionalization in today's drug discovery
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
synthesis of diverse analogues from readily available building blocks. This endeavor …
Organogel delivery vehicles for the stabilization of organolithium reagents
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 …
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 …
skeletal editing strategy that can be used to construct molecules with new skeletons, but …