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采用连续流工艺，使用一系列带有在线红外分析的微反应器，制备 N,N-二乙基-4-(3-氟苯基哌啶-4-亚甲基)苯甲酰胺，作为一种有效且高选择性的 δ-阿片受体激动剂。

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.

机构信息

Innovative Technology Centre, Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW UK.

出版信息

Chemistry. 2010 Nov 2;16(41):12342-8. doi: 10.1002/chem.201002147.

DOI:10.1002/chem.201002147
PMID:20859972
Abstract

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 δ-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.

摘要

本文描述了阿斯利康开发的强效 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。该工艺采用一系列基于流动的微反应器，采用集成的纯化方法，使用固体支撑试剂，并采用新开发的 ReactIR 流动池进行在线红外分析协议。使用这种监测设备，可以在合成过程中精确控制第四个输入流的启动。

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