Towards Niraparib
Niraparib is a PARP inhibitor approved as a maintenance therapy for the treatment of ovarian, fallopian tube and peritoneal cancers. GSK bought Tesaro in January 2019 for the rights to this drug in a deal worth US$5.1 billion.
Its impact continues to increase as this therapy becomes approved for a wider group of patients and a wider group of cancers. In October 2019, Niraparib was granted ‘breakthrough therapy designation’ by the FDA for the treatment of prostate cancer, which is a development owned by Janssen.
Current patented asymmetric routes towards this molecule install the key sp2-sp3 bond with poor enantioselectivity, and many routes produce the racemate and require separation.
ASR has established three enantioselective formal syntheses of Niraparib.