Rapid construction of substituted 3-amino-1,5-benzothiazepin-4(5H)-one dipeptide scaffolds through an Ugi-4CR - Ullmann cross-coupling sequence.
Org Biomol Chem
; 16(8): 1242-1246, 2018 02 21.
Article
in En
| MEDLINE
| ID: mdl-29379930
ABSTRACT
A 3-step methodology for the synthesis of 1,5-benzothiazepin-4(5H)-one dipeptidomimetics has been elaborated via an Ugi-4CR followed by a S-trityl deprotection and an intramolecular Cu(i)-catalyzed Ullmann condensation with moderate to good yields. In silico and NMR conformational studies showed that the lowest energy conformers stabilize γ- and ß-turn structures.
Full text:
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Collection:
01-internacional
Database:
MEDLINE
Language:
En
Journal:
Org Biomol Chem
Year:
2018
Document type:
Article