A unified lead-oriented synthesis of over fifty molecular scaffolds

被引：51

作者：

Doveston, Richard G. ^{[1
]}

Tosatti, Paolo ^{[1
]}

Dow, Mark ^{[1
]}

Foley, Daniel J. ^{[1
]}

Li, Ho Yin ^{[1
]}

Campbell, Amanda J. ^{[2
]}

House, David ^{[2
]}

Churcher, Ian ^{[2
]}

Marsden, Stephen P. ^{[1
]}

Nelson, Adam ^{[1
,3
]}

机构：

[1] Univ Leeds, Sch Chem, Leeds LS2 9JT, W Yorkshire, England

[2] GlaxoSmithKline Med Res Ctr, Stevenage SG1 2NY, Herts, England

[3] Univ Leeds, Astbury Ctr Struct Mol Biol, Leeds LS2 9JT, W Yorkshire, England

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2015年 / 13卷 / 03期

基金：

英国工程与自然科学研究理事会;

关键词：

CATALYZED CARBOAMINATION REACTIONS; ASYMMETRIC ALLYLIC SUBSTITUTIONS; DRUG DISCOVERY; DIVERSITY; CHEMISTRY; PIPERAZINES; IMPACT;

D O I：

10.1039/c4ob02287d

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Controlling the properties of lead molecules is critical in drug discovery, but sourcing large numbers of lead-like compounds for screening collections is a major challenge. A unified synthetic approach is described that enabled the synthesis of 52 diverse lead-like molecular scaffolds from a minimal set of 13 precursors. The divergent approach exploited a suite of robust, functional group-tolerant transformations. Crucially, after derivatisation, these scaffolds would target significant lead-like chemical space, and complement commercially-available compounds.

引用

页码：859 / 865

页数：7

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