Process for the manufacture of epoxy triazole derivatives
AssigneeBasilea Pharmaceutica AG
InventorsMarc Muller, Lin Xu
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Abstract
Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of −10 to 50° C. to give the compound of formula (I).
Claims3
A process for the manufacture of a compound of formula (IV-a)
- wherein PrG represents a hydroxyl-protecting group,
- in which process 1,4-difluorobenzene is reacted in the presence of a base with a compound of formula (III-a)
- wherein
- PrG has the same meaning as in Formula (IV-a),
- R3 represents methyl or ethyl, and
- R4 represents methyl, ethyl or methoxy, or
- R3 and R4 taken together with the nitrogen atom to which they are bound represent a 4- to 6-membered heterocyclic group having from 0 to 2 additional heteroatoms selected from nitrogen or oxygen.
A process according to 2, wherein PrG represents a 2-tetrahydropyranyl residue.
Dependencies are inferred from the claim text.