Synthesis of many different types of organic small molecules using one automated process

被引：410

作者：

Li, Junqi ^{[1
]}

Ballmer, Steven G. ^{[1
]}

Gillis, Eric P. ^{[1
]}

Fujii, Seiko ^{[1
]}

Schmidt, Michael J. ^{[1
]}

Palazzolo, Andrea M. E. ^{[1
]}

Lehmann, Jonathan W. ^{[1
]}

Morehouse, Greg F. ^{[1
]}

Burke, Martin D. ^{[1
]}

机构：

[1] Univ Illinois, Howard Hughes Med Inst, Dept Chem, Urbana, IL 61801 USA

来源：

SCIENCE | 2015年 / 347卷 / 6227期

基金：

美国国家科学基金会;

关键词：

SOLID-PHASE SYNTHESIS; COUPLING REACTIONS; POLYKETIDE; CHEMISTRY; STRATEGY;

D O I：

10.1126/science.aaa5414

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

Small-molecule synthesis usually relies on procedures that are highly customized for each target. A broadly applicable automated process could greatly increase the accessibility of this class of compounds to enable investigations of their practical potential. Here we report the synthesis of 14 distinct classes of small molecules using the same fully automated process. This was achieved by strategically expanding the scope of a building block-based synthesis platform to include even Csp3-rich polycyclic natural product frameworks and discovering a catch-and-release chromatographic purification protocol applicable to all of the corresponding intermediates. With thousands of compatible building blocks already commercially available, many small molecules are now accessible with this platform. More broadly, these findings illuminate an actionable roadmap to a more general and automated approach for small-molecule synthesis.

引用

页码：1221 / 1226

页数：6

共 32 条

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