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US 11,760,737 B2Granted
Process for manufacturing 4-(2,2,3,3-tetrafluoropropyl)morpholine
AssigneeADVERIO PHARM GmbH
InventorsPeter Fey, Sergii Pazenok, Christian Funke, Natalya Pavlovna Kolesnik, Olexandr Ivanovich Guzyr, Yuriy Grigorievich Shermolovich
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Abstract
The present application relates to a novel, cost-saving and efficient process for preparing 4-(2,2,3,3-tetrafluoropropyl)morpholine which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
Claims10
A process for preparing the compound of the formula (I)
- comprising reacting a compound of the formula (IIa)
- wherein
- R represents C1-C4 alkyl, phenyl, or naphthyl,
- where the phenyl is unsubstituted or substituted by one, two or three substituents independently of one another selected from the group consisting of linear or branched C1-C4 alkyl, chlorine, fluorine, bromine, amino, nitro, methylsulfonyl, (dimethyl-oxopropyl)amino, and sulfonic acid 2,2,3,3-tetrafluoropropylester,
- in an organic solvent or without solvent with morpholine of the formula (III)
- in a molar ratio of (IIa) to (III) of 1 to 2-5, in a sealed vessel or flow reactor under autogenic pressure or at 1 to 50 bar, at a temperature of 100-170° C. to give the compound of the formula (I)
- and a compound of the formula (IVa)
- wherein
- R is as defined for the compounds of the formula (IIa).
6 more elements
Dependencies are inferred from the claim text.