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US 2026/0258076 A1Published application
Process for the preparation of a fatty acid compound
AssigneeHoffmann-La Roche Inc.
InventorsChristian Steffen MOESSNER, Helene WOLLEB
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Abstract
The invention relates to a process for the preparation of a fatty acid compound of the formula Ia wherein AEEAc stands for 2-(2-(2-aminoethoxy) ethoxy) acetic acid and PROT1 is an ester protecting group and to the use of the fatty acid compound of the formula Ia for the preparation of peptides.
Claims23
A process for the preparation of a fatty acid compound of formula Ia
- wherein AEEAc stands for 2-(2-(2-aminoethoxy) ethoxy) acetic acid and PROT1 is an ester protecting group,
- comprising the steps;
- a) coupling the eicosanedioic acid ester of formula IIa
- wherein PROT1 is an ester protecting group,
- with a carboxyl group protected L-Glu of formula IIIa
- wherein PROT1 and PROT2 are ester protecting groups,
- to form the eicosanedioic acid L-Glu ester of formula IVa
- wherein PROT1 and PROT2 are as above;
- b) removing the ester protecting group PROT2 to form the eicosanedioic acid L-Glu acid of formula Va,
- wherein PROT1 is as above;
- c) forming the N-hydroxsuccinimide ester of formula VIa,
- wherein PROT1 is as above
- with a N-hydroxysuccinimide source compound;
- and
- d) coupling the N-hydroxsuccinimide ester of formula VIa with 2-(2-{2-[2-(2-amino-ethoxy)-ethoxy]-acetylamino}-ethoxy)-ethoxy]-acetic acid (AEEAc-AEEAc) to form the fatty acid compound of formula Ia.
12 more elements
Dependencies are inferred from the claim text.