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US 9,040,539 B2Granted
Process for the preparation of chiral triazolones
AssigneeSandoz Ltd.
InventorsMichael Oberhuber, Joerg Salchenegger, Dominic De Souza, Martin Albert, Thorsten Wilhelm, Martin Langner, Hubert Sturm, Hans-Peter Spitzenstaetter
Life of this patent
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Abstract
A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y3—NH2; of formula (IIa) 0=C═N—Y0 and/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V).
Claims59
An optionally crystalline chiral compound of formula (IVa)
- or a salt thereof,
- wherein R1 is an alkyl residue having from 1 to 6 carbon atoms and wherein —R is —H or the hydroxyl protecting group —SiRaRbRc, where Ra, Rb and Rc are the same or different and selected from the group consisting of optionally suitably substituted alkyl and aryl residues.
Dependencies are inferred from the claim text.