Deracemisation of Amines
AssigneeGlaxo Group Limited
InventorsMarina Alexeeva, Alexis Enright, Mahmoud Mahmoudian, Nicholas Turner
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Abstract
Methods are described for the deracemisation or chiral inversion of chiral amines by enzymatic treatment, such as by a stereoselective enzymatic conversion and either a non-selective or partially selective chemical or enzymatic conversion, simultaneously or sequentially. Also described are methods for selecting a suitable enzyme, particularly a suitable amine oxidase, and for the generation of novel enzymes suitable for use in the deracemisation method.
Claims25
A method for the enantiomeric conversion of amines comprising treating a homochiral amine or a mixture of amine enantiomers with an enzyme capable of catalysing oxidation of the amine in a stereoselective manner and, subsequently or simultaneously, treating with a reducing agent.
A method of improving the activity, substrate specificity, or enantioselectivity of an amine oxidase enzyme by directed evolution, the method comprising mutation of the enzyme and selection of a mutant having improved activity against an homochiral substrate.
A method of directing the evolution of an amino oxidase enzyme comprising the steps of:
- a) mutating the enzyme to create at least one enzyme variant;
- b) screening said enzyme variant for activity against a homochiral substrate;
- and
- c) selecting one or more enzyme variants which show greater activity toward the substrate than does the originator enzyme.
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Dependencies are inferred from the claim text.