在二元反应器系统中全自动流通合成仲磺酰胺。

Fully automated flow-through synthesis of secondary sulfonamides in a binary reactor system.

作者信息

Griffiths-Jones Charlotte M, Hopkin Mark D, Jönsson Daniel, Ley Steven V, Tapolczay David J, Vickerstaffe Emma, Ladlow Mark

机构信息

GlaxoSmithKline Cambridge Technology Centre, University Chemical Laboratory, Lensfield Road, Cambridge, CB2 1EW, UK.

出版信息

J Comb Chem. 2007 May-Jun;9(3):422-30. doi: 10.1021/cc060152b. Epub 2007 Mar 10.

DOI:10.1021/cc060152b

PMID:17348713

Abstract

A fully automated flow-through process for the production of secondary sulfonamides is presented. Primary sulfonamides were monoalkylated using a two-step "catch and release" protocol to generate library products of high purity. The automated flow synthesis platform incorporates four independent reactor columns and is able to perform automated column regeneration. A 48-member sulfonamide library was prepared as two 24-member sublibraries, affording library compounds in good yields and high purities without the need for further column chromatographic purification.

摘要

本文介绍了一种用于生产仲磺酰胺的全自动连续流工艺。伯磺酰胺通过两步“捕获与释放”方案进行单烷基化反应，以生成高纯度的文库产物。该自动连续流合成平台包含四个独立的反应柱，并且能够进行自动柱再生。制备了一个由48个成员组成的磺酰胺文库，分为两个由24个成员组成的子文库，无需进一步的柱色谱纯化即可高产率、高纯度地得到文库化合物。