Process for the Synthesis of a CPLA2 Inhibitor
OwnerChristoph M. Dehnhardt, Sreenivasulu Megati +2inventors
InventorsChristoph M. Dehnhardt, Sreenivasulu Megati, Ronald S. Michalak, Panolil Raveendranath
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Abstract
A process for making a substituted indole compound, including the steps of: reacting the compounds in a non-protic polar solvent in the presence of a catalyst to form the intermediate compound wherein Ph and X are as defined herein; and then, heating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compound The invention also includes compounds formed by this process.
Claims9
1-12. (canceled)
A process for making the compound
- comprising the reaction step
- wherein Ar represents phenyl optionally substituted with one to three halogen atoms;
- R represents C1-C6-alkyl, phenyl, —CH2O-phenyl, —CH2O-(C1-C6-alkyl), —CH2-phenyl, —CH2CH2-phenyl, or —CH2-phenyl—COOZ;
- Z represents H or C1-C6-alkyl;
- Ph represents phenyl;
- and
- X represents a moiety selected from the group consisting of H, F, Cl, Br, C1-C10-alkyl, C3-C10-cycloalkyl, and C6-C10-aryl, the alkyl moiety being optionally substituted with one or more atoms selected from F, Cl and Br, and the cycloalkyl and aryl moieties being optionally substituted with from one to three substituents selected from F, Cl, Br and C1-C6-alkyl.
A process for making the compound
- comprising the step of reacting the compound
- in N,N-dimethylformamide in the presence of copper iodide to form the substituted indole compound
- wherein Ar represents phenyl optionally substituted with one to three halogen atoms;
- R represents C1-C6-alkyl, phenyl, —CH2O-phenyl, —CH2O-(C1-C6-alkyl), —CH2-phenyl, —CH2CH2-phenyl, or —CH2-phenyl—COOZ;
- Z represents H or C1-C6-alkyl;
- Ph represents phenyl;
- and
- X represents a moiety selected from the group consisting of H, F, Cl, Br, C1-C10-alkyl, C3-C10-cycloalkyl, and C6-C10-aryl, the alkyl moiety being optionally substituted with one or more atoms selected from F, Cl and Br, and the cycloalkyl and aryl moieties being optionally substituted with from one to three substituents selected from F, Cl, Br and C1-C6-alkyl.
A process for making the compound
- comprising the reaction steps
20-22. (canceled)
Dependencies are inferred from the claim text.