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

TY - JOUR

T1 - A happy medium

T2 - the synthesis of medicinally important medium-sized rings: Via ring expansion

AU - Clarke, Aimee K.

AU - Unsworth, William P.

N1 - © The Royal Society of Chemistry 2020

PY - 2020/3/21

Y1 - 2020/3/21

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=85082134102&partnerID=8YFLogxK

U2 - 10.1039/d0sc00568a

DO - 10.1039/d0sc00568a

M3 - Review article

AN - SCOPUS:85082134102

SN - 2041-6520

VL - 11

SP - 2876

EP - 2881

JO - Chemical Science

JF - Chemical Science

IS - 11

ER -