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US 2004/0176432 A1Published application
Intermediate halophenyl derivatives and their use in a process for preparing azole derivatives
AssigneeBasilea Pharmaceutica AG
InventorMilan Soukup
Life of this patent
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Abstract
Novel halophenyl derivatives of the general formula (I), wherein R1 is halogen, a leaving group or 1H-1,2,4-tria-zol-1-yl and R2 is ethynyl or carboxy, X1 is halogen and X2 and X3 are each independently hydrogen or halogen, and their manufacture are described. They are intermediates for manufacturing azole derivatives of the general formula (V) which are valuable medicaments useful for treating systemic mycoses. 1
Claims36
Halophenyl derivatives of the general formula
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- wherein R1 is halogen, a leaving group or 1H-1,2,4-triazol-1-yl and R2 is ethynyl or carboxy, X1 is halogen and X2 and X3 are each independently hydrogen or halogen.
Process for the manufacture of halophenyl derivatives of the general formula
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- wherein R11 is halogen or a leaving group, X1 is halogen and X2 and X3 are each independently hydrogen or halogen,
- which is characterized in that it comprises reacting a halophenyl derivative of the general formula
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- wherein R11, X1, X2 and X3 are as above,
- with an alkyne of the general formula
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- wherein L is halogen or a leaving group,
- in the presence of a palladium catalyst and an organometallic reagent in an apolar organic solvent.
6 more elements
Dependencies are inferred from the claim text.