Bench-Stable Transfer Reagent Facilitates the Generation of Trifluoromethyl-sulfonimidamides.
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.
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MEDLINE
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En
Ano de publicação:
2018
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Article