Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid
AssigneeNovartis AG
InventorsDavid Hook, Thomas Ruch, Bernard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murlidhar Waykole
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Abstract
The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
Claims20
A process for producing a compound according to formula (18) or a salt thereof
- comprising the steps
- a) providing a compound according to formula (1), or tautomer, or salt thereof,
- b) methylating the compound according to formula (1), or tautomer, or salt thereof, to obtain a compound according to formula (2), or tautomer, or salt thereof,
- c) reacting the compound according to formula (2), or tautomer, or salt thereof, with a ring opening agent to obtain a compound according to formula (3) or a salt thereof
- d) reacting a compound according to formula (3) or a salt thereof to obtain a compound according to formula (18) or a salt thereof,
- wherein in the above formulae R1 and R2 are independently, of each other, hydrogen or a nitrogen protecting group and R3 is hydrogen or alkyl.
A process according to 3, wherein the configuration of the compounds of formulae (4), (5) and (1), or tautomers, or salts thereof, is according to formulae (4-a), (5-a) and (1-a), or tautomers thereof
Dependencies are inferred from the claim text.