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Synfacts 2009(7): 0706-0706  
DOI: 10.1055/s-0029-1217246
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Reboxetine Analogues

Contributor(s): Philip Kocienski
P. V. Fish*, M. Mackenny*, G. Bish, T. Buxton, R. Cave, D. Drouard, D. Hoople, A. Jessiman, D. Miller, C. Pasquinet, B. Patel, K. Reeves, T. Ryckmans, M. Skerten, F. Wakenhut
Pfizer Global Research and Development, Sandwich, UK
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Publication History

Publication Date:
22 June 2009 (online)

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Significance

The analogue M of the antidepressant reboxetine is being investigated as a dual ­noradrenaline and serotonin reuptake inhibitor. The synthesis depicted features an efficient lipase-catalyzed kinetic resolution of the morpholine-2-carboxylic ester derivative D as a key step.