Back to results
US 9,802,886 B2Granted
Process for making lysine-glutamic acid dipeptide derivatives
AssigneeHoffmann-La Roche Inc.
InventorKurt Puentener
Life of this patent
Estimating the term…
Abstract
The invention relates to compounds of the formula and to a process for making same and to the use of the products in the solid phase peptide synthesis. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain.
Claims16
A process for the preparation of compounds of formula I,
- and enantiomers and salts thereof, wherein:
- R1 is hydrogen or an ester protecting group;
- R2 is hydrogen;
- R3 is hydrogen or an amino protecting group and
- R4 is C12-20-alkyl;
- the process comprising:
- a) coupling the glutamic acid derivative of formula II
- or a salt thereof with a lysine derivative of formula III
- wherein R2′ is an ester protecting group, or a salt thereof to form a compound of the formula Ic;
- and
- b) removing the ester protecting group R2′ to provide the compound of formula I.
8 more elements
Dependencies are inferred from the claim text.