- 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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- Phenylalkylamines and phenylalkylureas in combinations to suppress gastric bleeding in aspirin therapy
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Novel pharmaceutical methods, combinations and compositions for reducing gastric bleeding during aspirin therapy for inflammation are disclosed. Compounds used in combination with aspirin are phenylalkylamines and phenylalkylureas having the formula: STR1 wherein Z is selected from the group consisting of --NHR2 or STR2 and R is selected from the group consisting of hydrogen, halogen, lower-alkoxy and trifluoromethyl and R1, R2, R3 and R4 are selected from the group consisting of hydrogen and lower-alkyl, where R3 and R4 taken together with the adjacent nitrogen atom may form a heterocyclic ring selected from the group of piperidino, pyrrolidino, piperazino, and morpholino.
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