Process Development of C–N Cross-Coupling and Enantioselective Biocatalytic Reactions for the Asymmetric Synthesis of Niraparib
| العنوان: | Process Development of C–N Cross-Coupling and Enantioselective Biocatalytic Reactions for the Asymmetric Synthesis of Niraparib |
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| المؤلفون: | Guy R. Humphrey, Nelo R. Rivera, Donald Bachert, Paul G. Bulger, Birgit Kosjek, Mark E. Scott, Khateeta M. Emerson, John Limanto, Kevin M. Belyk, Cheol K. Chung |
| المصدر: | Organic Process Research & Development. 18:215-227 |
| بيانات النشر: | American Chemical Society (ACS), 2013. |
| سنة النشر: | 2013 |
| مصطلحات موضوعية: | chemistry.chemical_classification, Indazole, Stereochemistry, Process development, Organic Chemistry, Enantioselective synthesis, Regioselectivity, Metathesis, Aldehyde, Coupling (electronics), chemistry.chemical_compound, chemistry, Physical and Theoretical Chemistry, Derivative (chemistry) |
| الوصف: | 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-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. |
| تدمد: | 1520-586X 1083-6160 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::a5f0cb44149fe5fc326ba73527a33f07 https://doi.org/10.1021/op400233z |
| رقم الأكسشن: | edsair.doi...........a5f0cb44149fe5fc326ba73527a33f07 |
| قاعدة البيانات: | OpenAIRE |
Find this issue from the American Chemical Society | تدمد: | 1520586X 10836160 |
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