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US 10,590,156 B2Granted
Galnac cluster phosphoramidite
AssigneeHoffmann-La Roche Inc.
InventorRene Trussardi
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Abstract
The invention comprises GalNAc phosphoramidite derivatives of the formula I wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/or optical isomers thereof. The invention further comprises a process for the preparation of the GalNAc phosphoramidite derivatives of the formula I and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.
Claims19
A GalNAc phosphoramidite derivative comprising formula I:
- wherein,
- R1 is a hydroxy protecting group;
- n is an integer from 0 to 10;
- and
- m is an integer from 0 to 20;
- or an enantiomer or optical isomer thereof.
3 more elements
A process for the preparation of a GalNAc phosphoramidite derivative of the formula I:
- the process comprising:
- a) reacting a GalNAc acid derivative of formula III:
- wherein R1 is a hydroxy protecting group and n is an integer from 0 to 10 with an amine of formula IV:
- wherein R3 is a hydroxy protecting group and m is an integer from 0 to 20, to form an amide of formula V:
- b) removing R3 to form a GalNAc acid amide of formula VI:
- and
- c) reacting the GalNAc acid amide of formula VI with a phosphoroamidating agent to form the GalNAc phosphoramidite derivative of the formula I.
4 more elements
Dependencies are inferred from the claim text.