Ring‐Expansion Reactions in the Synthesis of Macrocycles and Medium‐Sized Rings

JR Donald, WP Unsworth - Chemistry–A European Journal, 2017 - Wiley Online Library
Functionalised macrocycles and medium‐sized rings have applications in a number of
scientific fields, ranging from medicinal chemistry and supramolecular chemistry, to catalysis …

Strategies for the diversity-oriented synthesis of macrocycles

KT Mortensen, TJ Osberger, TA King, HF Sore… - Chemical …, 2019 - ACS Publications
Macrocycles have long been recognized as useful chemical entities for medicine, with
naturally occurring and synthetic macrocycles clinically approved for use as prescription …

Scaffold diversity synthesis and its application in probe and drug discovery

M Garcia‐Castro, S Zimmermann… - Angewandte Chemie …, 2016 - Wiley Online Library
Scaffold diversity is a crucial feature of compound collections that has a huge impact on their
success in biological screenings. The synthesis of highly complex and diverse scaffolds …

1, 2, 3-Triazoles as biomimetics in peptide science

N Agouram, EM El Hadrami, A Bentama - Molecules, 2021 - mdpi.com
Natural peptides are an important class of chemical mediators, essential for most vital
processes. What limits the potential of the use of peptides as drugs is their low bioavailability …

Heteroaryl rings in peptide macrocycles

IV Smolyar, AK Yudin, VG Nenajdenko - Chemical reviews, 2019 - ACS Publications
This Review is devoted to the chemistry of macrocyclic peptides having heterocyclic
fragments in their structure. These motifs are present in many natural products and synthetic …

An updated synthesis of the diazo-transfer reagent imidazole-1-sulfonyl azide hydrogen sulfate

GT Potter, GC Jayson, GJ Miller… - The Journal of Organic …, 2016 - ACS Publications
Imidazole-1-sulfonyl azide and salts thereof are valuable reagents for diazo-transfer
reactions, most particularly conversion of primary amines to azides. The parent reagent and …

Rhodium (III)-Catalyzed Atroposelective Indolization to Access Planar-Chiral Macrocycles

H Zhai, K Lv, J Li, J Wang, T Liu… - Journal of the American …, 2024 - ACS Publications
Macrocycles incorporating conformationally defined indoles are widely found in bioactive
natural products. However, the catalytic enantioselective synthesis of planar-chiral indoles …

The synthesis of structurally diverse macrocycles by successive ring expansion

C Kitsiou, JJ Hindes, P I'Anson… - Angewandte Chemie …, 2015 - Wiley Online Library
Structurally diverse macrocycles and medium‐sized rings (9–24 membered scaffolds, 22
examples) can be generated through a telescoped acylation/ring‐expansion sequence …

Multicomponent coupling and macrocyclization enabled by Rh (III)-catalyzed dual C–H activation: Macrocyclic oxime inhibitor of influenza H1N1

H Wang, Z Li, X Chen, JJ Wong, T Bi, X Tong, Z Xu… - Chem, 2023 - cell.com
Herein, we describe a practical streamlined two-component dual C–H activation
macrocyclization strategy entailing an in situ-generated directing group. The reaction mode …

Ring‐Expansion Approach to Medium‐Sized Lactams and Analysis of Their Medicinal Lead‐Like Properties

LG Baud, MA Manning, HL Arkless… - … A European Journal, 2017 - Wiley Online Library
Medium‐sized rings are widely considered to be under‐represented in biological screening
libraries for lead identification in medicinal chemistry. To help address this, a library of …