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

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• 作者：Debra J. Wallace ; Carl A. Baxter ; Karel J. M. Brands ; Nadine Bremeyer ; Sarah E. Brewer ; Richard Desmond ; Khateeta M. Emerson ; Jennifer Foley ; Paul Fernandez ; Weifeng Hu ; Stephen P. Keen ; Peter Mullens ; Daniel Muzzio ; Peter Sajonz ; Lushi Tan ; Robert D. Wilson ; George Zhou ; Guoyue Zhou
• 刊名：Organic Process Research & Development
• 出版年：2011
• 出版时间：July 15, 2011
• 年：2011
• 卷：15
• 期：4
• 页码：831-840
• 全文大小：981K
• 年卷期：v.15,no.4(July 15, 2011)
• ISSN：1520-586X

文摘

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.