Process development of C–N cross-coupling and enantioselective biocatalytic reactions for the asymmetric synthesis of niraparib
CK Chung, PG Bulger, B Kosjek, KM Belyk…
文献索引：Chung, Cheol K.; Bulger, Paul G.; Kosjek, Birgit; Belyk, Kevin M.; Rivera, Nelo; Scott, Mark E.; Humphrey, Guy R.; Limanto, John; Bachert, Donald C.; Emerson, Khateeta M. Organic Process Research and Development, 2014 , vol. 18, # 1 p. 215 - 227
Process development of the synthesis of the orally active poly (ADP-ribose) polymerase inhibitor niraparib is described. Two new asymmetric routes are reported, which converge on a high-yielding, regioselective, copper-catalyzed N-arylation of an indazole derivative as the late-stage fragment coupling step. Novel transaminase-mediated dynamic kinetic resolutions of racemic aldehyde surrogates provided enantioselective syntheses of the 3- ...
