- Hybrid Organo- and Biocatalytic Process for the Asymmetric Transformation of Alcohols into Amines in Aqueous Medium
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A hybrid organo- and biocatalytic system for the asymmetric conversion of racemic alcohols into amines was developed. Combining an organocatalyst, AZADO, an oxidant, NaOCl, and an enzyme, ω-transaminase, we implemented a one-pot oxidation-transamination sequential process in aqueous medium. The method showed broad substrate scope and was successfully applied to conventional secondary alcohols and sterically hindered β-substituted cycloalkanols, where a highly stereoselective dynamic asymmetric bioamination enabled us to set up both contiguous stereocenters with very high enantio- and diastereomeric ratio (>90% yield, >99% ee, and up to 49:1 dr).
- Liardo, Elisa,Ríos-Lombardía, Nicolás,Morís, Francisco,Rebolledo, Francisca,González-Sabín, Javier
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p. 4768 - 4774
(2017/07/24)
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- Broadening the chemical scope of laccases: Selective deprotection of N-benzyl groups
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Laccase from Trametes versicolor together with TEMPO has been found to be a very efficient system to deprotect N-benzylated primary amines, differing from previously described methods since it uses oxygen as a mild oxidant in aqueous medium. Chemoselective removal of the benzyl group was achieved with excellent yields when secondary amines and alcohol moieties were also present.
- Martínez-Montero, Lía,Díaz-Rodríguez, Alba,Gotor, Vicente,Gotor-Fernández, Vicente,Lavandera, Iván
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supporting information
p. 2794 - 2798
(2015/05/27)
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- Method for Producing O-Alkylated Aminoalcohols
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A process for preparing O-alkylated amino alcohols by reacting N-unsubstituted or N-monosubstituted amino alkoxide salts with alkyl halides, the amino alkoxide salts being formed by means of alkali metal or alkaline earth metal hydroxides.
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Page/Page column 3
(2011/06/26)
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- Method For Producing O-Alkylated Cyclic Aminoalcohols
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A process for preparing O-alkylated amino alcohols of the formula (I) by reacting N-unsubstituted or N-monosubstituted amino alkoxide salts with alkyl halides, the amino alkoxide salts being formed by means of alkoxides
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Page/Page column 3
(2009/01/20)
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- IL-8 RECEPTOR ANTAGONISTS
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This invention relates to the use of phenyl ureas of formulas (I) and (II) in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). The variables of (I) and (II) are defined herein. STR1
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