Sunday, 26 October 2014

A flow process using microreactors for the preparation of a quinolone derivative as a potent 5HTIB antagonist


QuinolonesThe quinolone derivative shown below is a potent 5HT1B antagonist developed by AstraZeneca. The continuous flow synthesis (the final steps shown below) of this pharmaceutical agent was completed using a combination of flow microreactors, while incorporating polymer-supported reagents and scavengers to aid reaction telescoping and purification [14]. The result is encouraging, as it clearly demonstrates that multi-step sequences can be incorporated into flow chemistry platforms leading to polyfunctional molecules of biological interest. Moreover, we were able to improve on the overall yield via a batch method using the new reactors.


A flow process using microreactors for the preparation of a quinolone derivative as a potent 5HTIB antagonistZ. Qian, I. R. Baxendale, S.V. Ley
Synlett 2010, 505-508

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