Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.

Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.

Abstract: The present disclosure generally related to an improved process for the preparation of various piperidine derivatives. More particularly, the present disclosure related to an improved process for preparing sufentanil base (1) and related compounds, which advantageously utilizes more cost effective and/or less hazardous reagents, including a dispersion comprising between about 50% and about 70% by weight (based on the total weight of the dispersion) of an alkali metal hydride, such as sodium hydride, as well as eliminates the need for expensive and/or time consuming purification techniques.

Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.

Abstract: The present invention relates to novel crystalline forms of naltrexone methobromide including hydrated and solvated forms. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline forms of naltrexone methobromide, as well as methods of treating or preventing opioid induced side effects by administering the pharmaceutical compositions.

Abstract: The present invention provides to an improved process for preparing alkaloid salts. In particular, the process comprises a stepwise addition of an acid to an alkaloid chosen from hydrocodone, codeine, and dihydrocodeine to form a flowable mixture of the alkaloid salt.

Abstract: A synthetic process for the preparation of amino acid esters such as methylphenidate and analogs thereof is disclosed. The process involves reacting an amino acid such as ?-phenyl-?-(2-piperidinyl)acetic acid or an analog thereof with an alcohol such as methanol in the presence of an acid and a water sequestrant such as trimethyl orthoacetate. In some embodiments, the water sequestrant is added to the reaction mixture after an initial period of esterification and then the reaction is allowed to continue. The ?-phenyl-?-(2-piperidinyl)acetic acid methyl ester or analog thereof is then isolated from the reaction mixture. In one variation of the process, the supernatant liquid may be recycled in subsequent runs to increase yield and product purity.

Abstract: The present disclosure generally related to an improved process for the preparation of various piperidine derivatives. More particularly, the present disclosure related to an improved process for preparing sufentanil base (1) and related compounds, which advantageously utilizes more cost effective and/or less hazardous reagents, including a dispersion comprising between about 50% and about 70% by weight (based on the total weight of the dispersion) of an alkali metal hydride, such as sodium hydride, as well as eliminates the need for expensive and/or time consuming purification techniques.

Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.

Abstract: The present invention relates to novel crystalline forms of naltrexone methobromide including hydrated and solvated forms. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline forms of naltrexone methobromide, as well as methods of treating or preventing opioid induced side effects by administering the pharmaceutical compositions.

Abstract: The present invention provides processes for the preparation of saturated 6-keto, 3-alkoxy morphinans from unsaturated 6-hydroxy, 3-hydroxy morphinans, In particular, the invention provides processes that utilize catalytic isomerization and alkylation reactions for the preparation of saturated 6-keto, 3-alkoxy morphinans.

Abstract: A synthetic process for the preparation of amino acid esters such as methylphenidate and analogs thereof is disclosed. The process involves reacting an amino acid such as ?-phenyl-?-(2-piperidinyl)acetic acid or an analog thereof with an alcohol such as methanol in the presence of an acid and a water sequestrant such as trimethyl orthoacetate. In some embodiments, the water sequestrant is added to the reaction mixture after an initial period of esterification and then the reaction is allowed to continue. The ?-phenyl-?-(2-piperidinyl)acetic acid methyl ester or analog thereof is then isolated from the reaction mixture. In one variation of the process, the supernatant liquid may be recycled in subsequent runs to increase yield and product purity.

Abstract: A process for purifying Narcotine to remove color and impurities to form Noscapine. The process includes forming an aqueous isopropanol solution with the Narcotine product wherein the isopropanol concentration of the solution is about 20% to about 70% by volume; and adjusting the pH of the solution with a strong base to a pH of about 10 to about 14, wherein impurities are removed from the Narcotine product.

Abstract: This invention relates to the purification of N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester by resolving a mixture of the alpha- and beta-isomers of N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester using metal ions.

Abstract: Disclosed are methods of producing super-absorbing polymeric networks of polyaspartates from crosslinked polysuccinimide. In one preferred aspect, polysuccinimide is first reacted with an organic crosslinking agent, preferably an organic base containing at least two primary amine groups, to form a gelled crosslinked polysuccinimide. The gelled crosslinked polysuccinimide is then base hydrolyzed to a gelled polymeric network of polyaspartate and deswollen with at least one liquid alcohol to a polymeric network of polyaspartate which demonstrates super-absorbing capability in water and in electrolyte solution. Super-absorbing polymeric networks of polyaspartates can also be produced in a single reaction vessel by sequentially crosslinking a polysuccinimide with an organic crosslinking agent in an aqueous reaction medium, optionally containing a mineral acid, and then hydrolyzing the crosslinked polysuccinimide to produce a polymeric network of polyaspartate.

Abstract: Super-absorbing polymeric networks of crosslinked polyaspartates are produced from crosslinked polysuccinimide. Super-absorbing polymeric networks are produced in a single reaction vessel by crosslinking polysuccinimide with at least one organic polyamine crosslinking agent in the presence of at least one nitrogenous base. The reaction is carried out in an aqueous reaction mixture to produce a polymeric network of crosslinked polyaspartate.