Bristol-myers Squibb Pharma Company

Bristol-myers Squibb Compnay

Dupont Pharmaceuticals Company

Lynette May Oh

Jiacheng Zhou

Philip Ma

Hui-Yin Li

Pasquale N Confalone

Rajagopal Bakthavatchalam

Charles G Clark

Lucius T Rossano

Chris Teleha

A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.

Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones

The present invention relates to processes for the production of &#x3b1;-aryl-&#x3b2;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.

Convergent synthesis of &#x3b1;-aryl-&#x3b2;-ketonitriles

A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described.These compounds are useful as factor Xa inhibitors.

Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones

The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.

Convergent synthesis of &agr;-aryl-&bgr;-ketonitriles

The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.

Efficient ligand-mediated Ullmann coupling of anilines and azoles

Synthesis of 1,3,5-trisubstituted pyrazoles

A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described.

The present invention relates to processes for the production of .alpha.-aryl-.beta.-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.

Convergent synthesis of .alpha.-aryl-.beta.-ketonitriles

Method for making 4-arylamino-1-alkyl-�1,2,3!triazolo�4,5-c!pyridines by base-promoted isomerization of 7-alkylamino-3-aryl-�1,2,3!triazolo�4,5-b!pyridines.

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West Chester, PA, United States of America

Lynette May Oh