Back to results
US 2018/0022690 A1Published application
Process and intermediates for the preparation of nep inhibitors
AssigneeNovartis AG
InventorsBenjamin MARTIN, Francesca MANDRELLI, 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. It further relates to new intermediate compounds and their use for said new chemical synthesis route.
Claims24
A compound of formula (1), or a salt thereof
- wherein R1 is hydrogen or C1-C6-alkyl.
A compound of formula (2) or a salt thereof,
A compound of the formula (7),
(canceled)
(canceled)
A process for the manufacture of a compound of the formula (8),
- wherein R′ and R″ are independently of each other hydrogen or a nitrogen protecting group, preferably tert-butyloxycarbonyl, and R1 is hydrogen or C1-C6-alkyl, comprising hydrogenating a compound of the formula (1), or a salt thereof,
- wherein R1 is hydrogen or C1-C6-alkyl,
- optionally including or followed by the introduction of a nitrogen protecting group.
(canceled)
An organocatalyst selected from the group consisting of those with the following formulae:
(canceled)
Dependencies are inferred from the claim text.