Albemarle Corporation

Calithera Biosciences, Inc.

Wyckoff Chemical Company, Inc.

James J Springer

Timothy Friend Stanton

Jacqueline N Williams

Eric Lee Williams

Anthony Frank Skufca

Andrew George Zeiler

Mario Emilov Lozanov

Bryce Kelly Assink

James M VanderRoest

Krishnamurthy Nacharaju

Andrew G Zeiler

Richard S Olsen

Amit Thakkar

James D Sunderhaus

Anthony F Skufca

Mario E Lozanov

Bryce K Assink

Eric L Williams

The invention relates to crystalline salts of a compound having the structure of formula (I), methods for their preparation, and related pharmaceutical compositions comprising the crystalline salt. The invention further relates to methods of treating or preventing cancer or an immunological or neurological disease comprising administering a crystalline salt of the invention.

Crystal forms of glutaminase inhibitors

The invention relates to crystalline salts of a heterocyclic compound, methods of their preparation, and related pharmaceutical preparations thereof. The invention further relates to methods of treatment using the crystalline salts of the invention.

Process for preparing metyrapone type compounds are generally described herein. In particular, one step process for preparing metyrapone type compounds are described herein. Such processes generally include an alpha-carbon arylation coupling reaction between 3-isobutyrylpyridine and 3-halopyridine compounds in the presence of a palladium catalyst and a phosphine ligand to form the metyrapone-type compounds. 

Process for the synthesis of metyrapone and alkylated metyrapone analogs

This invention provides a method for the synthesis of a 2-amino-4,6-dimethoxybenzamide and other benzamides of Compound I: wherein R, R, R, and Reach independently represent a hydrogen, a C-Calkyl, or a C-Calkoxy; and wherein Rand Reach independently represent a hydrogen, a C-Calkyl, a protecting group, or a directing group. 

Processes for the synthesis of 2-amino-4,6-dimethoxybenzamide and other benzamide compounds

The present invention comprises a process for preparing essentially pure 1,2-dihydro-6-alkyl-2-oxo-5-(pyridinyl)-nicotinonitriles from a crude reaction mixture containing the corresponding amide as an impurity. By 'essentially pure' is meant a level of purity acceptable for orally administered pharmaceutical products, usually less than 0.1% of any single impurity. At least a stoichiometric amount of an acylating agent is reacted with the crude reaction mixture, and thereafter recovering essentially pure 1,2-dihydro-6-alkyl-2-oxo 5-(pyridinyl)-nicotinonitrile.

Purification of 1,2-dihydro-6-alkyl-2-oxo-5-(pyridinyl)-nicotinonitriles

A process for preparing 4-aryl-1,2,4-triazol-3-ones and 4-aryl-5-alkoxy-1,2,4-triazol-3-ones. A reaction mixture includes a primary aromatic amine, an alkyl carbazate and a trialkyl orthoformate. The reactants are heated in a reaction vessel in the presence of an acid catalyst and a polar solvent. After the reaction is complete, the solvent is removed, water is added, and the slurry is filtered to isolate 4-aryl-5-alkoxy-1,2,4-triazol-3-one. Alternatively, after the reaction is complete, an alkali metal alkoxide is added to the reaction mixture in the vessel, and the new mixture is again heated until the reaction is complete. The solvent is distilled from the mixture, and the remaining mixture is diluted with water. The slurry is separated from mixture, washed and dried to obtain 4-aryl-1,2,4-triazol-3-one in near 100% yield.

Process for preparation of 4-aryl-1,2,4-triazol-3-ones

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Saugatuck, MI, United States of America

James J Springer