Histidine protection
AssigneeNational Research Development Corporation
InventorsJohn H. Jones, Tom Brown
Life of this patent
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AssigneeNational Research Development Corporation
InventorsJohn H. Jones, Tom Brown
Estimating the term…
Histidine derivatives of formula I are useful inter alia in peptide synthesis. ##STR1## wherein: X represents --CH.sub.2 OCH.sub.2 Ar, in which Ar is a phenyl substituent optionally substituted by one or more halogen, alkoxy, alkyl or nitro groups; Y, which differs from X, represents hydrogen, a protective group capable of inhibiting self coupling during formation of a peptide bond, an amino acid residue, a peptide chain or an antibiotic residue; E represents OH,OM,M representing an alkali metal or ammonium, OR, R representing an alkyl, aryl, aralkyl or alkaryl group, an amino acid residue, a peptide chain or an antibiotic residue; the compound I being optionally in the form of a hydrate or acid salt. In compounds I of especial interest, X represents benzyloxymethyl or p-bromobenzyloxymethyl, Y represents t-butyloxycarbonyl and E represents --OH.
A compound of formula I ##STR4## wherein X is --CH.sub.2 OCH.sub.2 Ar in which Ar represents phenyl or p-bromophenyl, Y represents Boc, Fmoc or, benzyloxycarbonyl, or hydrogen, and E represents OH or OR, wherein R is a C.sub.1 -C.sub.6 alkyl group.
A compound of formula I ##STR5## wherein X is --CH.sub.2 OCH.sub.2 Ar in which Ar represents phenyl or p-bromophenyl, Y represents Boc, Fmoc or benzyloxycarbonyl, and E represents OH.
Dependencies are inferred from the claim text.