Synthesis of a Drug-Like Focused Library of Trisubstituted Pyrrolidines Using Integrated Flow Chemistry and Batch Methods

被引：34

作者：

Baumann, Marcus ^{[2
]}

Baxendale, Ian R. ^{[2
]}

Kuratli, Christoph ^{[1
]}

Ley, Steven V. ^{[2
]}

Martin, Rainer E. ^{[1
]}

Schneider, Josef ^{[1
]}

机构：

[1] F Hoffmann La Roche Ltd, Div Pharmaceut, Chem Technol & Innovat, CH-4070 Basel, Switzerland

[2] Univ Cambridge, Dept Chem, Innovat Technol Ctr, Cambridge CB2 1EW, England

来源：

ACS COMBINATORIAL SCIENCE | 2011年 / 13卷 / 04期

关键词：

integrated flow; trisubstituted pyrrolidines; focused library; ORGANIC-SYNTHESIS; DISCOVERY; ACID; MICROREACTORS; DERIVATIVES; TECHNOLOGY; ABSORPTION; EFFICIENCY; SCAVENGERS; OXIDATION;

D O I：

10.1021/co2000357

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

A combination of flow and batch chemistries has been successfully applied to the assembly of a series of trisub-stituted drug-like pyrrolidines. This study demonstrates the efficient preparation of a focused library of these pharmaceutically important structures using microreactor technologies, as well as classical parallel synthesis techniques, and thus exemplifies the impact of integrating innovative enabling tools within the drug discovery process.

引用

页码：405 / 413

页数：9

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