Development of a Fit-for-Purpose Large-Scale Synthesis of an Oral PARP Inhibitor

…, P Fernandez, W Hu, SP Keen, P Mullens…

Index: Wallace, Debra J.; Baxter, Carl A.; Brands, Karel J. M.; Bremeyer, Nadine; Brewer, Sarah E.; Desmond, Richard; Emerson, Khateeta M.; Foley, Jennifer; Fernandez, Paul; Hu, Weifeng; Keen, Stephen P.; Mullens, Peter; Muzzio, Daniel; Sajonz, Peter; Tan, Lushi; Wilson, Robert D.; Zhou, George; Zhou, Guoyue Organic Process Research and Development, 2011 , vol. 15, # 4 p. 831 - 840

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Citation Number: 14

Abstract

Compound (1) a poly (ADP-ribose) polymerase (PARP) inhibitor has been made by a fit-for- purpose large-scale synthesis using either a classical resolution or chiral chromatographic separation. The development and relative merits of each route are discussed, along with operational improvements and extensive safety evaluations of potentially hazardous reactions.