Synthesis of vaniprevir (MK-7009): lactamization to prepare a 20-membered [corrected] macrocycle.
J Org Chem
; 76(19): 7804-15, 2011 Oct 07.
Article
em En
| MEDLINE
| ID: mdl-21838271
ABSTRACT
Development of a practical synthesis of MK-7009, a 20-membered [corrected] macrocycle, is described. A variety of ring-closing strategies were evaluated, including ring-closing metathesis, intermolecular palladium-catalyzed cross-couplings, and macrolactamization. Ring closure via macrolactamization was found to give the highest yields under relatively high reaction concentrations. Optimization of the ring formation step and the synthesis of key intermediates en route to MK-7009 are reported.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Macrocíclicos
/
Técnicas de Química Sintética
/
Indóis
/
Lactamas
Idioma:
En
Revista:
J Org Chem
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Estados Unidos