A method of recovering a highly pure hydrocodone base from an impure hydrocodone preparation includes contacting the impure hydrocodone preparation with a weak acid in water to form a solution and adding a strong base to the solution in an amount sufficient to precipitate the pure hydrocodone base product. A highly pure hydrocodone base comprises less than 0.0025 wt% codeinone.

本发明涉及阿片样受体拮抗剂类衍生物、其制备方法及其在医药上的应用。具体而言，本发明涉及一种通式(I)所示的纳洛酮类衍生物、其可药用盐，及其制备方法，以及它们作为治疗剂治疗因长期使用吗啡等阿片样受体激动剂而引起的便秘等疾病的用途，该药物作用于外周神经。其中通式(I)中的各取代基的定义与说明书中的定义相同。

An abuse deterrent pharmaceutical composition including an acid soluble salt of a pharmaceutically active ingredient and a buffering ingredient; wherein the acid soluble salt of the pharmaceutically active ingredient and the buffering ingredient retard release of the pharmaceutically active ingredient when the composition is ingested in excess of an intended dosage.

Pharmaceutically active homo-dimers of opioid and other pharmaceutically active agents characterized by a single phenolic hydroxyl group wherein the respective monomers are ether-linked through such groups by an ethylene residue. The dimers share the receptor pharmacology of the corresponding monomer, in particular cases are non-absorbed, and the ether link of the dimers is particularly resistant to metabolism when administered to a subject, all conferring divers advantages relative to the corresponding monomers. Exemplary of the dimers are those of buprenorphine, naloxone, naltrexone, des-venlafaxine, albuterol and acetaminophen.

The present invention concerns prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing more consistent pain relief by increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are provided. The invention also provides for decreasing the adverse GI side effects of opioid analgesics.

The present invention provides methods of N-demethylating, N-methylated heterocycles and N-methyl, N-oxide heterocycles using a transition metal with an oxidation state of zero, ferrocene or substituted derivatives thereof, or Cr ³⁺ .N-demethylated heterocycles prepared by the methods of the present invention are also provided.

The present invention provides processes for the stereoselective synthesis of 6-alpha-amino morphinans. In particular, the invention provides processes for the reductive amination of 6-keto normorphinans by catalytic transfer hydrogenation.

The present invention provides processes for the synthesis of five and six membered rings. In particular, the present invention provides processes for the synthesis of five and six membered rings in alkaloids.

Described herein are fluorinated organic compounds and methods of making fluorinated organic compounds, for example, using palladium complexes. Also described herein are compositions and kits containing compounds and palladium complexes described herein.

The present invention relates generally to analgesic compounds having a mu opioid receptor agonist linked to a delta opioid receptor antagonist, and to methods for producing analgesia using such compounds. As compared to opioids such as morphine, these compounds can cause less tolerance, physical dependence, and/or constitpation. These compounds are also more potent than morphine and are able to cross the blood brain barrier, thereby allowing for peripheral (e.g., IV) administration.

An improved process for the preparation of codeine from morphine comprises the steps of: a) reacting morphine with a methylating agent in the presence of a hydrocarbon solvent at a temperature of 100 to 215 °C under reflux conditions such that approximately 50 % or more of the hydrocarbon solvent is returned to the reaction mixture to substantially avoid the formation of codeine methyl ether; and b) recovering codeine from the reaction mixture. The process may include step a) above followed by b) cooling the reaction mixture to approximately 85 °C and adding water to terminate the reaction; c) raising the pH of the reaction mixture to approximately 11; d) separating the hydrocarbon solvent phase containing codeine and dimethylaniline; and e) adding a dilute mineral or organic acid and approximately 6 to 7 times the volume of water for each volume of hydrocarbon solvent to separate dimethylaniline and codeine.