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 …

Shortening synthetic routes to small molecule active pharmaceutical ingredients employing biocatalytic methods

S Simić, E Zukić, L Schmermund, K Faber… - Chemical …, 2021 - ACS Publications
Biocatalysis, using enzymes for organic synthesis, has emerged as powerful tool for the
synthesis of active pharmaceutical ingredients (APIs). The first industrial biocatalytic …

A perspective on late-stage aromatic C–H bond functionalization

L Zhang, T Ritter - Journal of the American Chemical Society, 2022 - ACS Publications
Late-stage functionalization of C–H bonds (C–H LSF) can provide a straightforward
approach to the efficient synthesis of functionalized complex molecules. However, C–H LSF …

The crucial role of methodology development in directed evolution of selective enzymes

G Qu, A Li, CG Acevedo‐Rocha, Z Sun… - Angewandte Chemie …, 2020 - Wiley Online Library
Directed evolution of stereo‐, regio‐, and chemoselective enzymes constitutes a unique way
to generate biocatalysts for synthetically interesting transformations in organic chemistry and …

[PDF][PDF] Innovation by evolution: bringing new chemistry to life (Nobel Lecture)

FH Arnold - Angew. Chem. Int. Ed, 2019 - fenix.ciencias.ulisboa.pt
I am a chemist and engineer who looks upon the living world with the deepest admiration.
Nature, herself a brilliant chemist and by far the best engineer of all time, invented life that …

Advances in ultrahigh-throughput screening for directed enzyme evolution

U Markel, KD Essani, V Besirlioglu, J Schiffels… - Chemical Society …, 2020 - pubs.rsc.org
Enzymes are versatile catalysts and their synthetic potential has been recognized for a long
time. In order to exploit their full potential, enzymes often need to be re-engineered or …

Enzymatic late‐stage modifications: better late than never

E Romero, BS Jones, BN Hogg… - Angewandte Chemie …, 2021 - Wiley Online Library
Enzyme catalysis is gaining increasing importance in synthetic chemistry. Nowadays, the
growing number of biocatalysts accessible by means of bioinformatics and enzyme …

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 …

Biocatalysis in drug discovery and development

A Fryszkowska, PN Devine - Current Opinion in Chemical Biology, 2020 - Elsevier
Enzyme catalysis, enabled by advances in protein engineering and directed evolution, is
beginning to transform chemical synthesis in the pharmaceutical industry. This review …

Repertoire of computationally designed peroxygenases for enantiodivergent C–H oxyfunctionalization reactions

P Gómez de Santos, I Mateljak, MD Hoang… - Journal of the …, 2023 - ACS Publications
The generation of enantiodivergent biocatalysts for C–H oxyfunctionalizations is ever more
important in modern synthetic chemistry. Here, we have applied the FuncLib algorithm …