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

被引:163
作者
Clarke, Aimee K. [1 ]
Unsworth, William P. [1 ]
机构
[1] Univ York, Dept Chem, York YO10 5DD, N Yorkshire, England
基金
英国工程与自然科学研究理事会;
关键词
DIVERSITY-ORIENTED SYNTHESIS; ZIP-REACTION; MACROCYCLIC LACTAMS; CLOSURE REACTIONS; FACILE SYNTHESIS; LACTONES; CYCLIZATION; DISCOVERY;
D O I
10.1039/d0sc00568a
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:2876 / 2881
页数:6
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