Chemoenzymatic resolution of β-azidophenylethanols by candida antarctica and their application for the synthesis of chiral benzotriazoles

The kinetic resolutions of (±)-β-azidophenylethanols were carried out using lipase from Candida antarctica, and enantiomerically enriched (R)-β-azidophenylethanols and their corresponding (S)-β-azidophenylethyl acetates were obtained in good enantiomeric excesses (up to > 99%). The enantiomerical...

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Detalhes bibliográficos
Autores: Rocha, Lenilson Coutinho, Rosset, Isac George, Melgar, Gliseida Zelayaran, Raminelli, Cristiano [UNIFESP], Porto, André Luiz Meleiro, Jeller, Alex Haroldo
Formato: artículo
Estado:Versión publicada
Fecha de publicación:2013
País:Brasil
Recursos:Universidade Federal de São Paulo (UNIFESP)
Repositorio:Repositório Institucional da UNIFESP
Idioma:inglés
OAI Identifier:oai:repositorio.unifesp.br:11600/7957
Acesso em linha:http://dx.doi.org/10.5935/0103-5053.20130181
http://repositorio.unifesp.br/handle/11600/7957
Access Level:acceso abierto
Palavra-chave:CALB
lipase
biocatalysis
click chemistry
[3 + 2]
cycloaddition
Descrição
Resumo:The kinetic resolutions of (±)-β-azidophenylethanols were carried out using lipase from Candida antarctica, and enantiomerically enriched (R)-β-azidophenylethanols and their corresponding (S)-β-azidophenylethyl acetates were obtained in good enantiomeric excesses (up to > 99%). The enantiomerically enriched (R)-β-azidophenylethanols were subjected to cyclization reaction with 2-(trimethylsilyl)phenyl triflate and CsF producing chiral 1,2,3-benzotriazole compounds in good yields (75-86%) by a [3 + 2] cycloaddition, which involves the benzyne formation.