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A simple scale-up strategy for organolithium chemistry in flow mode: From feasibility to kilogram quantities

Hafner, Andreas and Filipponi, Paolo and Piccioni, Lorenzo and Meisenbach, Mark and Schenkel, Berthold and Venturoni, Francesco and Sedelmeier, Joerg Mathias (2016) A simple scale-up strategy for organolithium chemistry in flow mode: From feasibility to kilogram quantities. Organic process research & development.

Abstract

A platform for conducting organolithium chemistry in continuous flow mode, covering the scales from medicinal chemistry to later phase process development, is described. The use of this flow setup which mimics the concept of flash chemistry on scale, has been demonstrated by the exemplary, large-scale preparation of (4-fluoro-2-(trifluoromethyl)phenyl)boronic acid following a reaction sequence of halogen/lithium exchange, borylation and semi-batch workup. Furthermore, the key factors and corresponding practical assessments required for the streamlined and seamless scale-up from lab environment to higher productivity are highlighted.

Item Type: Article
Keywords: continuous manufacturing, organolithium chemistry, aryl boronic acids, scale-up concept
Date Deposited: 04 Jan 2017 00:45
Last Modified: 04 Jan 2017 00:45
URI: https://oak.novartis.com/id/eprint/30593

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