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US 7,459,563 B2Granted
Process for the preparation of isonicotinic acid derivatives
AssigneeHoffmann-La Roche Inc.
InventorPaul Spurr
Life of this patent
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Abstract
The present invention relates to a process for the manufacture of compounds of formula Ia or Ib and pharmaceutically acceptable additional salts thereof, wherein R is lower alkyl. The compounds of formula Ia or Ib are valuable intermediate products for the manufacture of compounds that are pharmaceutically active as adenosine A2a receptor antagonist or metabotropic Glutamate receptor 2 antagonist. Such compounds are important in the regulation of many aspects of cellular metabolism and in the modulation of different central nervous system activities.
Claims15
A process for the manufacture of a compound of formula Ia or Ib
- or a pharmaceutically acceptable additional salt thereof,
- wherein R is lower alkyl;
- comprising
- a) lithiating a compound of formula II
- with a lithiating agent to produce a lithiated compound of formula III
- b) reacting of the compound of formula III with DMF to produce the compound of formula IV
- c) oxidizing the compound of formula IV with O3 and H2O2 to produce compound of formula Ia;
- d) optionally, esterifying a compound of formula Ia with an alcohol of formula ROH to produce compound of formula Ib;
- wherein R is as defined above.
6 more elements
Dependencies are inferred from the claim text.