Stereoselective Crystallization as a Key Step for the Synthesis of New Epimers of Captopril Derivatives

The present work describes the synthesis of two new diastereomersof captopril derivatives. These epimers were achievedby conjugate addition of thioacetic acid and a-toluenethiol to aa,b-unsaturated system. The diastereomeric ratios obtained from thisreaction were low at 0 oC and moderate at -50 oC....

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Detalhes bibliográficos
Autores: Aurelio Ortiz, Omar Arellano, Estibaliz Sansinenea, Sylvain Bernès
Formato: artículo
Estado:Versión publicada
Fecha de publicación:2007
País:México
Recursos:Universidad Autónoma de Nuevo León
Repositorio:Redalyc-UANL
OAI Identifier:oai:redalyc.org:47551414
Acesso em linha:https://www.redalyc.org/articulo.oa?id=47551414
Access Level:acceso abierto
Palavra-chave:Química
Captopril
ACE inhibitor
antihypertensive
conjugate addition of thiols
Descrição
Resumo:The present work describes the synthesis of two new diastereomersof captopril derivatives. These epimers were achievedby conjugate addition of thioacetic acid and a-toluenethiol to aa,b-unsaturated system. The diastereomeric ratios obtained from thisreaction were low at 0 oC and moderate at -50 oC. The importanceof this synthesis, however, is that in one case, both epimers can beisolated in good yields. Their isolation was possible because of thehigh crystallinity showed by one epimer compared to the other one.The absolute configuration of the solid compound was established byX-ray analysis.