Efficient asymmetric synthesis of novel gastrin receptor antagonist AG-041R via highly stereoselective alkylation of oxindole enolates.
J Org Chem
; 71(22): 8559-64, 2006 Oct 27.
Article
em En
| MEDLINE
| ID: mdl-17064034
ABSTRACT
An efficient method for asymmetric synthesis of the potent Gastrin/CCK-B receptor antagonist AG-041R was developed. Core oxindole stereochemistry was established by asymmetric alkylation of oxindole enolates with bromoacetic acid esters, using l-menthol as a chiral auxiliary. The key alkylation reaction of the oxindole enolates generated tetrasubstituted chiral intermediates with high diastereoselectivity. The stereoselective alkylation reactions are described in detail.
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Base de dados:
MEDLINE
Assunto principal:
Receptor de Colecistocinina B
/
Indóis
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article