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US 8,618,310 B2Granted
Process for preparing n-protected 4-ketoproline derivatives
AssigneeEvonik Degussa GmbH
InventorsKai Rossen, Rolf Hoffmann, Martin Sarich
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Abstract
The present invention is concerned with a process for preparing compounds of the general formula (I). These compounds can preferably be used to prepare bioactive agents. The reaction of the invention starts from the corresponding hydroxy compounds which are oxidized, with Ru catalysis, in a one-phase aqueous system.
Claims20
A process for preparing N-protected 4-ketoproline compounds of formula (I):
- in which
- X is an acid, ester or amide function,
- PG is an N-protective group which comprises a carbonyl function and is bonded via this function to the nitrogen,
- said process comprising oxidizing a 4-hydroxyproline compound with an oxidizing agent in the presence of catalytically active ruthenium compounds,
- wherein the oxidation is carried out in an aqueous one-phase system, and the oxidation product (I) is induced to crystallize out during the addition of said oxidizing agent.
2 more elements
Dependencies are inferred from the claim text.