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

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 exten...

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Published inOrganic process research & development Vol. 15; no. 4; pp. 831 - 840
Main Authors 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
Format Journal Article
LanguageEnglish
Published American Chemical Society 15.07.2011
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Summary: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.
ISSN:1083-6160
1520-586X
DOI:10.1021/op2000783