Three-component synthesis of highly functionalized aziridines containing a peptide side chain and their one-step transformation into ß-functionalized α-ketoamides.
Beilstein J Org Chem
; 12: 1772-7, 2016.
Article
en En
| MEDLINE
| ID: mdl-27559422
A sequential three-component process is described, starting from 3-arylmethylene-2,5-piperazinediones and involving a one-pot sequence of reactions achieving regioselective opening of the 2,5-diketopiperazine ring and diastereoselective generation of an aziridine ring. This method allows the preparation of N-unprotected, trisubstituted aziridines bearing a peptide side chain under mild conditions. Their transformation into ß-trifluoroacetamido-α-ketoamide and α,ß-diketoamide frameworks was also achieved in a single step.
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1
Colección:
01-internacional
Base de datos:
MEDLINE
Idioma:
En
Revista:
Beilstein J Org Chem
Año:
2016
Tipo del documento:
Article
País de afiliación:
España
Pais de publicación:
Alemania