Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Simon Breitler

Kurt Puentener

René Trussardi

Joerg Lill

Rene (deceased) Trussardi

The invention comprises a process for the preparation of a GalNAc phosphoramidite epimer of the formula (I), wherein Ris a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20, corresponding enantiomers and/or optical isomers thereof and the use of the process for the preparation of GalNAc-cluster oligonucleotide conjugates.

Process for the preparation of GalNAc phosphoramidite epimers

The invention comprises a process for the preparation of GalNAc oligonucleotide conjugates which comprises the coupling of a GalNAc cluster compound of the formula or corresponding salts, enantiomers and/or a stereoisomer thereof, with an oligonucleotide in the presence of an O-dicarboximidouronium salt as coupling agent.

Process for the preparation of GalNAc oligonucleotide conjugates

The invention comprises a process for the preparation of therapeutically valuable GalNAc cluster oligonucleotide conjugates. The process comprises the coupling of an alkali metal salt, earth alkali metal salt or a tetraalkylammonium salt of an oligonucleotide with a GalNAc cluster compound or with a salt thereof and a subsequent purification.

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Basel, Switzerland

Simon Breitler