Issue 11, 2020

A happy medium: the synthesis of medicinally important medium-sized rings via ring expansion

Abstract

Medium-sized rings have much promise in medicinal chemistry, but are difficult to make using direct cyclisation methods. In this minireview, we highlight the value of ring expansion strategies to address this long-standing synthetic challenge. We have drawn on recent progress (post 2013) to highlight the key reaction design features that enable successful ‘normal-to-medium’ ring expansion for the synthesis of these medicinally important molecular frameworks, that are currently under-represented in compound screening collections and marketed drugs in view of their challenging syntheses.

Graphical abstract: A happy medium: the synthesis of medicinally important medium-sized rings via ring expansion

Article information

Article type
Minireview
Submitted
30 Jan 2020
Accepted
27 Feb 2020
First published
02 Mar 2020
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY license

Chem. Sci., 2020,11, 2876-2881

A happy medium: the synthesis of medicinally important medium-sized rings via ring expansion

A. K. Clarke and W. P. Unsworth, Chem. Sci., 2020, 11, 2876 DOI: 10.1039/D0SC00568A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements