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Studies on the dynamic resolution of Crizotinib intermediate.
de França, Alexandre da S; Silva, Marcus V M; Neves, Rebeca V; de Souza, Stefania P; Leão, Raquel A C; Monteiro, Carlos M; Rocha, Ângelo; Afonso, Carlos A M; de Souza, Rodrigo O M A.
Afiliación
  • de França ADS; Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
  • Silva MVM; Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
  • Neves RV; Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
  • de Souza SP; Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
  • Leão RAC; Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil; Pharmacy School, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
  • Monteiro CM; Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal.
  • Rocha Â; Institute for Bioengineering and Biosciences, Department of Bioengineering, Instituto Superior Técnico, University of Lisbon, Portugal.
  • Afonso CAM; Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal.
  • de Souza ROMA; Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil; Pharmacy School, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil. Electronic address: souzarod21@gmail.com.
Bioorg Med Chem ; 26(7): 1333-1337, 2018 04 01.
Article en En | MEDLINE | ID: mdl-28802669
ABSTRACT
Crizotinib is an anti-cancer agent approved for treatment of non-small cell lung carcinoma. Retrosynthetic analysis revels 1-(2,6-dichloro-3-fluorophenyl)ethanol as an important intermediate, which can be made available by different biocatalytic approaches. Herein we report our results on the kinetic and dynamic resolution towards the desired chiral intermediate for Crizotinib synthesis. The results obtained show that very good conversions and high selectivity could be obtained for the kinetic resolution (45% conv. and E>200) while dynamic kinetic resolution under continuous-flow conditions afforded the desired product in 57% conversion and 98% e.e.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Piridinas / Simulación de Dinámica Molecular Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Brasil
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Piridinas / Simulación de Dinámica Molecular Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Brasil