1284448-67-4Relevant academic research and scientific papers
Process development of C-N cross-coupling and enantioselective biocatalytic reactions for the asymmetric synthesis of niraparib
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.
, p. 215 - 227 (2014)
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 Narylation 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-aryl-piperidine coupling partner. Conversion of the C-N cross-coupling product to the final API was achieved by deprotection and salt metathesis to isolate the desired crystalline salt form.
Asymmetric synthesis of di- and trisubstituted cyclopropanes through an intramolecular ring closure
Kallemeyn, Jeffrey M.,Mulhern, Mathew M.,Ku, Yi-Yin
supporting information; experimental part, p. 535 - 538 (2011/05/04)
An asymmetric synthesis of di- and trisubstituted cyclopropanes proceeding through an intramolecular ring closure of activated chiral benzyl alcohols has been developed. The chiral alcohol intermediates are obtained from asymmetric reduction of readily av
