Process development for ABT-472, a benzimidazole PARP inhibitor

…, BJ Gaede, AR Haight, R Henry, B Kotecki…

文献索引：Barkalow, Jufang H.; Breting, Jeffrey; Gaede, Bruce J.; Haight, Anthony R.; Henry, Rodger; Kotecki, Brian; Mei, Jianzhang; Pearl, Kurt B.; Tedrow, Jason S.; Viswanath, Shekhar K. Organic Process Research and Development, 2007 , vol. 11, # 4 p. 693 - 698

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被引用次数: 20

摘要

A nine-step convergent process was developed for the synthesis of ABT-472, a benzimidazole PARP inhibitor. The identity and origin of several impurities were determined, and the process was modified to reduce or eliminate these impurities. A number of safety and control issues were investigated. The original synthesis was shortened to 9 steps and streamlined while maintaining a convergent strategy. A stable salt was selected, and ...