Borylation via iridium catalysed C-H activation: a new concise route to duocarmycin derivatives.
Org Biomol Chem
; 22(27): 5603-5607, 2024 07 10.
Article
de En
| MEDLINE
| ID: mdl-38904084
ABSTRACT
The synthesis of the ethyl ester analogue of the ultrapotent antitumour antibiotic seco-duocarmycin SA has been achieved in eleven linear steps from commercially available starting materials. The DSA alkylation subunit can be made in ten linear steps from the same precursor. The route involves C-H activation at the equivalent of the C7 position on indole leading to a borylated intermediate 9 that is stable enough for peptide coupling reactions but can be easily converted to the free hydroxyl analogue.
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Duocarmycines
/
Indoles
/
Iridium
Langue:
En
Journal:
Org Biomol Chem
Sujet du journal:
BIOQUIMICA
/
QUIMICA
Année:
2024
Type de document:
Article
Pays de publication:
Royaume-Uni