A Continuous Flow Process Using a Sequence of Microreactors with In-line IR Analysis for the Preparation of N,N-Diethyl-4-(3-fluorophenylpiperidin-4-ylidenemethyl)benzamide as a Potent and Highly Selective δ-Opioid Receptor Agonist
A Continuous Flow Process Using a Sequence of Microreactors with In-line IR Analysis for the Preparation of N,N-Diethyl-4-(3-fluorophenylpiperidin-4-ylidenemethyl)benzamide as a Potent and Highly Selective δ-Opioid Receptor Agonist
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DOI：
10.1002/chem.201002147
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发表时间：
2010-01-01
影响因子：
4.3
通讯作者：
Ley, Steven V.
中科院分区：
文献类型：
--
作者：
Qian, Zizheng;Baxendale, Ian R.;Ley, Steven V.
本文介绍了阿斯利康公司开发的强效δ阿片受体激动剂N，N-二乙基-4-（3-氟苯基哌啶-4-亚基甲基）苯甲酰胺的连续流合成的设计、优化和开发。该工艺采用了一系列基于流动的微反应器，采用固体支持的试剂和使用新开发的ReactIR流动池的在线IR分析协议进行集成纯化。利用该监测装置，可以在合成期间精确地控制第四输入流束的启动。
This article describes the design, optimisation and development of a continuous flow synthesis of N,N-diethyl-4-(3-fluorophenylpiperidin-4-ylidenemethyl)benzamide, a potent delta-opioid receptor agonist developed by AstraZeneca. The process employs a sequence of flow-based microreactors, with integrated purification employing solid-supported reagents and in-line IR analytical protocols using a newly developed ReactIR flow cell. With this monitoring device, initiation of the fourth input flow stream can be precisely controlled during the synthesis.