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 …

Charting the evolution of chemoenzymatic strategies in the syntheses of complex natural products

CN Stout, NM Wasfy, F Chen… - Journal of the American …, 2023 - ACS Publications
Bolstered by recent advances in bioinformatics, genetics, and enzyme engineering, the field
of chemoenzymatic synthesis has enjoyed a rapid increase in popularity and utility. This …

Engineering Hydroxylase Activity, Selectivity, and Stability for a Scalable Concise Synthesis of a Key Intermediate to Belzutifan

WL Cheung‐Lee, JN Kolev, JA McIntosh… - Angewandte Chemie …, 2024 - Wiley Online Library
Biocatalytic oxidations are an emerging technology for selective C− H bond activation. While
promising for a range of selective oxidations, practical use of enzymes catalyzing aerobic …

Iron-and cobalt-catalyzed C (sp 3)–H bond functionalization reactions and their application in organic synthesis

Y Liu, T You, HX Wang, Z Tang, CY Zhou… - Chemical Society …, 2020 - pubs.rsc.org
Direct C–H bond functionalization catalyzed by non-precious transition metals is an
attractive strategy in synthetic chemistry. Compared with the precious metals rhodium …

C–H Bonds as Functional Groups: Simultaneous Generation of Multiple Stereocenters by Enantioselective Hydroxylation at Unactivated Tertiary C–H Bonds

A Palone, G Casadevall, S Ruiz-Barragan… - Journal of the …, 2023 - ACS Publications
Enantioselective C–H oxidation is a standing chemical challenge foreseen as a powerful
tool to transform readily available organic molecules into precious oxygenated building …

Engineered and artificial metalloenzymes for selective C–H functionalization

X Ren, R Fasan - Current opinion in green and sustainable chemistry, 2021 - Elsevier
The direct functionalization of C–H bonds constitutes a powerful strategy to construct and
diversify organic molecules. However, controlling the chemo-and site-selectivity of this …

Chemoenzymatic approaches for exploring structure–activity relationship studies of bioactive natural products

F Li, H Deng, H Renata - Nature Synthesis, 2023 - nature.com
Spurred by advancements in microbial genetics and enzyme engineering, chemoenzymatic
strategies, which combine enzymatic and synthetic transformations, have increasingly made …

P450 Monooxygenases Enable Rapid Late‐Stage Diversification of Natural Products via C−H Bond Activation

ND Fessner - ChemCatChem, 2019 - Wiley Online Library
The biological potency of natural products has been exploited for decades. Their inherent
structural complexity and natural diversity might hold the key to efficiently address the urgent …

C–N Bond Forming Radical Rebound Is the Enantioselectivity-Determining Step in P411-Catalyzed Enantioselective C(sp3)–H Amination: A Combined …

BK Mai, NM Neris, Y Yang, P Liu - Journal of the American …, 2022 - ACS Publications
Engineered metalloenzymes represent promising catalysts for stereoselective C–H
functionalization reactions. Recently, P450 enzymes have been evolved to allow for new-to …

Gene-guided discovery and ribosomal biosynthesis of moroidin peptides

RD Kersten, LS Mydy, TR Fallon… - Journal of the …, 2022 - ACS Publications
Moroidin is a bicyclic plant octapeptide with tryptophan side-chain cross-links, originally
isolated as a pain-causing agent from the Australian stinging tree Dendrocnide moroides …