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Bench-Stable Transfer Reagent Facilitates the Generation of Trifluoromethyl-sulfonimidamides.
Wright, Miranda; Martínez-Lamenca, Carolina; Leenaerts, Joseph E; Brennan, Paul E; Trabanco, Andrés A; Oehlrich, Daniel.
Afiliação
  • Wright M; Structural Genomics Consortium & Target Discovery Institute, Nuffield Department of Medicine Research Building , University of Oxford , Old Road Campus, Roosevelt Drive , Oxford OX3 7FZ , U.K.
  • Martínez-Lamenca C; Neuroscience Medicinal Chemistry , Janssen Research & Development , Turnhoutseweg 30 , B-2340 Beerse , Belgium.
  • Leenaerts JE; Neuroscience Medicinal Chemistry , Janssen Research & Development , Turnhoutseweg 30 , B-2340 Beerse , Belgium.
  • Brennan PE; Structural Genomics Consortium & Target Discovery Institute, Nuffield Department of Medicine Research Building , University of Oxford , Old Road Campus, Roosevelt Drive , Oxford OX3 7FZ , U.K.
  • Trabanco AA; Neuroscience Medicinal Chemistry , Janssen Research & Development , C/Jarama 75A , 45007 Toledo , Spain.
  • Oehlrich D; Neuroscience Medicinal Chemistry , Janssen Research & Development , Turnhoutseweg 30 , B-2340 Beerse , Belgium.
J Org Chem ; 83(16): 9510-9516, 2018 08 17.
Article em En | MEDLINE | ID: mdl-29932332
Sulfonimidamides are an emerging bioisosteric replacement in medicinal chemistry projects, and therefore new chemistries are necessary to access this functionality. The general synthesis of CF3-sulfonimidamides from an activated bench-stable transfer reagent is described. A diverse reaction scope is demonstrated, with a wide range of nucleophilic amines being tolerated in this transformation. The CF3-sulfonimidamides obtained contain an additional diversity point, in the form a protected imine, that could be unmasked to allow late stage modifications.

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2018 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2018 Tipo de documento: Article