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Late-Stage C(sp2)-C(sp3) Diversification via Nickel Oxidative Addition Complexes.
Odena, Carlota; Santiago, Tomás G; Linares, María Lourdes; Castellanos-Blanco, Nahury; McGuire, Ryan T; Chaves-Arquero, Belén; Alonso, Jose Manuel; Diéguez-Vázquez, Alejandro; Tan, Eric; Alcázar, Jesús; Buijnsters, Peter; Cañellas, Santiago; Martin, Ruben.
Afiliación
  • Odena C; Institute of Chemical Research of Catalonia (ICIQ), The Barcelona Institute of Science and Technology, Avenida Països Catalans 16, 43007 Tarragona, Spain.
  • Santiago TG; Departament de Química Orgànica, Universitat Rovira i Virgili, c/Marcel·lí Domingo 1, 43007 Tarragona, Spain.
  • Linares ML; Institute of Chemical Research of Catalonia (ICIQ), The Barcelona Institute of Science and Technology, Avenida Països Catalans 16, 43007 Tarragona, Spain.
  • Castellanos-Blanco N; Janssen-Cilag, S.A., a Johnson & Johnson Company, C/Jarama 75A, 45007 Toledo, Spain.
  • McGuire RT; Institute of Chemical Research of Catalonia (ICIQ), The Barcelona Institute of Science and Technology, Avenida Països Catalans 16, 43007 Tarragona, Spain.
  • Chaves-Arquero B; Institute of Chemical Research of Catalonia (ICIQ), The Barcelona Institute of Science and Technology, Avenida Països Catalans 16, 43007 Tarragona, Spain.
  • Alonso JM; Janssen-Cilag, S.A., a Johnson & Johnson Company, C/Jarama 75A, 45007 Toledo, Spain.
  • Diéguez-Vázquez A; Janssen-Cilag, S.A., a Johnson & Johnson Company, C/Jarama 75A, 45007 Toledo, Spain.
  • Tan E; Janssen Pharmaceutica Nv, A Johnson & Johnson Company, Turnhoutseweg 30, 2340, Beerse, Belgium.
  • Alcázar J; Janssen Pharmaceutica Nv, A Johnson & Johnson Company, Turnhoutseweg 30, 2340, Beerse, Belgium.
  • Buijnsters P; Janssen-Cilag, S.A., a Johnson & Johnson Company, C/Jarama 75A, 45007 Toledo, Spain.
  • Cañellas S; Janssen Pharmaceutica Nv, A Johnson & Johnson Company, Turnhoutseweg 30, 2340, Beerse, Belgium.
  • Martin R; Janssen-Cilag, S.A., a Johnson & Johnson Company, C/Jarama 75A, 45007 Toledo, Spain.
J Am Chem Soc ; 146(31): 21264-21270, 2024 Aug 07.
Article en En | MEDLINE | ID: mdl-39052124
ABSTRACT
Herein, we describe nickel oxidative addition complexes (Ni-OACs) of drug-like molecules as a platform to rapidly generate lead candidates with enhanced C(sp3) fraction. The potential of Ni-OACs to access new chemical space has been assessed not only in C(sp2)-C(sp3) couplings but also in additional bond formations without recourse to specialized ligands and with improved generality when compared to Ni-catalyzed reactions. The development of an automated diversification process further illustrates the robustness of Ni-OACs, thus offering a new gateway to expedite the design-make-test-analyze (DMTA) cycle in drug discovery.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: J Am Chem Soc Año: 2024 Tipo del documento: Article País de afiliación: España
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: J Am Chem Soc Año: 2024 Tipo del documento: Article País de afiliación: España