Back to results
US 10,851,059 B2Granted
Processes and intermediates for NEP inhibitor synthesis
AssigneeNovartis AG
InventorsFlorian Karl Kleinbeck-Riniker, Ives Mafli, Benjamin Martin, Gerhard Penn, Gottfried Sedelmeier, Joerg Sedelmeier, Francesco Venturoni
Life of this patent
Estimating the term…
Abstract
The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.
Claims14
A compound of formula (1), or a salt thereof,
- wherein:
- R1 is hydrogen or C1-C6-alkyl;
- R3 is —NO2 or —NR′R″, wherein R′ and R″ are independently of each other hydrogen or a nitrogen protecting group;
- and
- R4 is selected from hydrogen, C1-C6-carbonyl, C1-C6-alkoxycarbonyl, and a sulphonyl group.
2 more elements
A process for producing a compound of formula (6)
- wherein R′ and R″ are independently of each other hydrogen or a nitrogen protecting group, and R1 is hydrogen or C1-C6-alkyl,
- said process comprising taking a compound of formula (1-b)
- wherein R′ and R″ are independently of each other hydrogen or a nitrogen protecting group, and R1 is hydrogen or C1-C6-alkyl,
- optionally treating the compound of formula (1-b) with an OH-activating agent to obtain a compound of formula (1-d)
- wherein R′ and R″ are independently of each other hydrogen or a nitrogen protecting group,
- R1 is hydrogen or C1-C6-alkyl, and
- R4 is an OH-activating group, and
- subjecting the compound of formula (1-b) or (1-d) to a hydrogenation reaction to obtain the compound of formula (6).
5 more elements
Dependencies are inferred from the claim text.