Process development for ABT-472, a benzimidazole PARP inhibitor
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 control of the API solid form was established. The process was successfully scaled up to provide 8.5 kg of final product of >99% purity in 33% yield over 9 steps.
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.
p. 693 - 698
(2012/12/29)
Substituted benzimidazoles and their use as parp inhibitors
Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4- to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.
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(2008/06/13)
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