Branched amino acids
OwnerRichard Francis William Jackson, Urszula Grabowskainventors
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OwnerRichard Francis William Jackson, Urszula Grabowskainventors
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The invention relates to novel branched amino acids and novel methods for their production. The amino acids are useful in the preparation of non-natural peptides and peptidomimetics, by efficient synthesis methodology allowing good enantiomeric specificity at the alpha carbon. Typically the stereochemistry at the alpha carbon is at least 85%, preferably at least 95%, such as in excess of 99% enantiomerically pure. L-stereochemistry at this location is convenient as most biological interactions will favour this configuration, but the invention also extends to enantiomerically enriched and preferably at least 85%, preferably at least 95% such as at least 99% enantiomerically pure D stereoconfiguration. Compounds of the invention will find utility in the preparation of non-natural peptides and peptidomimetics, such as those used in the exploration of receptor specificity and activity or in peptidomimetic inhibitors of enzyme function. The compounds of the invention are built into such peptides/peptidomimetics using standard peptide chemistry.
A compound of the formula I:
A compound according to any preceding claim, wherein R″ is H.
A compound according to any preceding claim wherein R″ is H and R″ is an amine protecting group.
A compound according to any preceding claim wherein C′, C″ and D′ are hydrogen and E′ and E″ are independently Alk.
A compound according to any preceding claim wherein n is 0, that is ( ) is a bond.
Use of a compound as defined in any preceding claim in the synthesis of a peptide or peptidomimetic.
A method of synthesising a compound of the formula I
Dependencies are inferred from the claim text.