Kilogram Synthesis of a Selective Serotonin Reuptake Inhibitor
Organic Process Research & Development2008Vol. 12(2), pp. 168–177
Citations Over Time
Robert Anthes, Osagie Bello, Serge Benoit, Chien‐Kuang Chen, Elisabeth Corbett, Richard M. Corbett, Albert J. DelMonte, Stéphane Gingras, R. C. Livingston, Justin B. Sausker, Maxime Soumeillant
Abstract
Process development of a selective serotonin reuptake inhibitor (1) is described. The synthesis features Nishiyama catalyst-mediated asymmetric cyclopropanation of vinyl indole 2 with ethyldiazoacetate to install the trans-disubstituted cyclopropane. The active pharmaceutical ingredient (1) was prepared in 13 chemical steps with 9 isolations and proceeded in an overall yield of 34%.
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