Abstract: The present invention provides enantiomerically pure (R)-(?)-tomoxetine (S)-(+)-mandelate and atomoxetine HCl. The present invention further provides enantiomerically pure (R)-(?)-tomoxetine (S)-(+)-mandelate prepared from racemic tomoxetine. The present invention also provides enantiomerically pure atomoxetine HCl prepared from (R)-(?)-tomoxetine (S)-(+)-mandelate.

Abstract: Provided are processes for preparing tomoxetine comprising reacting N-methyl-3-hydroxy-3-phenylpropylamine with dimethylsulfoxide (DMSO) and 2-fluorotoluene in the presence of an alkali base to form tomoxetine. Also provided is the conversion of said tomoxetine into atomoxetine or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(?)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water.

Abstract: The present invention provides a process for the optical resolution of racemic tomoxetine under reaction conditions that improve reaction yields and optical purity. The invention also provides an epimerization process for the (S)-(+) enantiomer. The invention further provides the conversion of the enantiomer obtained from the optical resolution into atomoxetine or a pharmaceutically acceptable salt thereof.

Abstract: The invention is directed to processes for making levalbuterol HCl Polymorph A from by suspending or forming a first slurry of (R)-SLB(D)-DBTA in at least a first organic solvent, adding HCl to the suspension or slurry of the solid (R)-SLB.D-DBTA until the (R)-SLB.D-DBTA forms levalbuterol HCl Polymorph A, and isolating the levalbuterol HCl Polymorph A.

Abstract: The invention is directed to levalbuterol HCl Form B and methods of making the same.

Abstract: Provided are processes for the preparation of (R)-SLB.D-DBTA salt and levalbuterol hydrochloride. Also provided are levalbuterol hydrochloride degradation products and processes for preparing them. Pharmaceutical compositions comprising at least one levalbuterol hydrochloride of the invention and at least one pharmaceutically-acceptable excipient are also provided.

Abstract: The invention relates to a process for the synthesis of 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo[4,5-C]quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C]quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C]quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-carboxamide, and to the said intermediates.

Abstract: The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imidazo(4,5-C)quinoline-4-amines via the intermediates.

Abstract: The invention relates to a process for the synthesis of 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo [4,5-C]quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C]quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C]quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-carboxamide, and to the said intermediates.

Abstract: The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imidazo(4,5-C)quinoline-4-amines via the intermediates.

Abstract: The invention relates to a process for the synthesis of 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo[4,5-C] quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C] quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C] quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-carboxamide, and to the said intermediates.

Abstract: The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imidazo(4,5-C)quinoline-4-amines via the intermediates.

Abstract: The invention relates to a process for the synthesis of 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo[4,5-C] quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C] quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C] quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-carboxamide, and to the said intermediates.