Abstract: Novel polymorphic forms of tavaborole, Form A and Form B, and methods of making same are disclosed. Methods are disclosed for the manufacture of the novel polymorphic Forms A and B. Methods include dissolving tavaborole in a pharmaceutically acceptable solvent to obtain a mixture, heating the mixture until a clear solution is obtained, cooling the clear solution, stirring the clear solution to obtain a crystalline product, filtering the crystalline product, and drying the crystalline product to obtain the pharmaceutically acceptable crystalline form of tavaborole. Pharmaceutical composition are disclosed including a pharmaceutically acceptable crystalline form of tavaborole Form A and/or Form B.

Abstract: Novel processes are disclosed for the preparation of eribulin mesylate. Novel intermediate compounds used in the processes for making eribulin mesylate as well as processes for making the intermediates are disclosed.

Abstract: Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.

Abstract: Processes are disclosed for making pomalidomide which involve reducing 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione using a catalyst and at least one solvent. The process may include reacting 3-nitrophthalic anhydride with ?-amino glutarimide hydrochloride to obtain the 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione. The process may further include, prior to the reducing step, subjecting the 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione to a purification process comprising heating a mixture of 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione and 1,4-dioxane to obtain a solution, treating the obtained solution with carbon, removing the carbon from the solution to obtain a purified 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione solution and using the purified 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione solution for the reducing step.

Abstract: Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.

Abstract: Novel synthetic approaches to make 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide, intermediates and pharmaceutically acceptable salts thereof are provided.

Abstract: Novel processes for making the N-pyrrazole substituted 2-adenosine derivative regadenoson and a novel polymorph thereof. The novel polymorph of regadenoson designated form H and drug substances and pharmaceutical compositions including the novel polymorph H are disclosed.

Abstract: Isosulfan blue and processes for the preparation thereof are provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.

Abstract: A process for the preparation of isosulfan blue (Active Pharmaceutical Ingredient) is provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon mild oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.

Abstract: Novel synthetic approaches to make 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide, intermediates and pharmaceutically acceptable salts thereof are provided.

Abstract: Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.

Abstract: A process for the preparation of isosulfan blue (Active Pharmaceutical Ingredient) is provided. A process is also provided for preparation of the intermediate, 2-chlorobenzaldehyde-5-sulfonic acid, sodium salt of formula (2), used in the preparation thereof and a procedure for the isolation of benzaldehyde-2,5-disulfonic acid, di-sodium salt of the formula (3). Also provided is a process for the preparation of an isoleuco acid of formula (4), which upon mild oxidation gives rise to isosulfan blue of pharmaceutical grade which can be used for preparation of pharmaceutical formulations. The isolation and purification procedures provided in the process provide substantially pure isosulfan blue with HPLC purity 99.5% or greater.

Abstract: Processes are disclosed for the synthesis of the Factor Xa anticoagulant fondaparinux and related compounds. Protected pentasaccharide intermediates and efficient and scalable processes for the industrial scale production of fondaparinux sodium by conversion of the protected pentasaccharide intermediates via a sequence of deprotection and sulfonation reactions are provided.