| Patent application number | Description | Published |
|---|
| 20080207906 | Synthetic Route to 14-Hydroxyl Opiates Through 1-Halo-Thebaine or Analogs - Novel methods of synthesis of known and novel 14-hydroxyl opiates through 1-halothebaine and derivatives are described. | 08-28-2008 |
| 20080262231 | Processes for Preparing Morphinans and Intermediates Thereof - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a β,γ-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a β,γ-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting α,β-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to β,γ-bicyclic ketone compounds, wherein the β,γ-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product. | 10-23-2008 |
| 20090156818 | Process and compounds for the production of (+)opiates - The invention generally provides processes and intermediate compounds useful for the production of (+)-opiates. Non-limiting examples of (+) opiates that may be derived from one or more compounds of the invention include (+)-noroxymorphone, (+)-naltrexone, (+)-naloxone, (+)-N-cyclopropylmethylnorhydrocodone, (+)-N-cycloproylmethylnorhydromorphone, (+)-N-allylnorhydrocodone, (+)-N-allylnorhydromorphone, (+)-noroxycodone, (+)-naltrexol, (+)-naloxol, and (+)-3-O-methyl-naltrexone. | 06-18-2009 |
| 20090221825 | Process for the Preparation of 3-Hydroxymorphinan Derivatives - Processes are described for the synthesis of 3-hydroxymorphinan derivatives by hydrolysis of side products from the O-demethylation of 3-methoxymorphinan derivatives. | 09-03-2009 |
| 20090247756 | Process for the Preparation of Hexahydroisoquinolines from 1,2,3,4-Tetrahydroisoquinolines - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate. | 10-01-2009 |
| 20090247760 | Preparation of Amides from an Acid and Amine for Intermediates in the Synthesis of Morphinans - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl | 10-01-2009 |
| 20090247761 | Preparation of 3,4-Dihydroisoquinolines in the Synthesis of Morphinans - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl | 10-01-2009 |
| 20090258843 | Compositions Containing Antiviral Compounds and Methods of Using the Same - The present invention is directed to compositions and methods for the treatment of various diseases, pathological disorders, and medical conditions such as viral infections and cancer. The compositions include (A) an antiviral compound or a pharmaceutically acceptable salt thereof; and (B) an agent selected from the group consisting of a substituted or unsubstituted imidazole or a pharmaceutically acceptable salt thereof; a non-steroidal anti-inflammatory agent or a pharmaceutically acceptable salt thereof; an amino acid or a pharmaceutically acceptable salt thereof; a carboxylic acid or a pharmaceutically acceptable salt thereof; a sulfonic acid or a pharmaceutically acceptable salt thereof; and a combination thereof. | 10-15-2009 |
| 20090299069 | Processes and Compounds for the Preparation of Normorphinans - The invention generally provides processes and intermediate compounds useful for the production of normorphinans and derivatives of normorphinans. | 12-03-2009 |
| 20100022776 | Preparation of Hexahydroisoquinolines from Dihydroisoquinolines - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate. | 01-28-2010 |
| 20100041888 | Process for the Preparation of 6-Alpha-Hydroxy-N-Alkylated Opiates - The present invention is directed to the conversion of a 6-keto morphinan to a 6-alpha-hydroxy morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source. | 02-18-2010 |
| 20100048906 | Preparation of Substituted Morphinan-6-Ones and Salts and Intermediates Thereof - The present invention is directed to processes for the synthesis of morphinan-6-ones and salts, intermediates, and analogs thereof. | 02-25-2010 |
| 20100056789 | Substituted Berbines and Processes for their Synthesis - The present invention provides processes for the synthesis of substituted berbine compounds. Also provided are intermediates used in the synthesis of substituted berbine compounds. | 03-04-2010 |
| 20100063290 | Preparation of 3,4-Dihydroisoquinolines from an Acid and an Amine - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl | 03-11-2010 |
| 20100081818 | Process for the Preparation of 6-Alpha-Hydroxy-N-Alkylated Opiates - The present invention is directed to the preparation of 6-hydroxy morphinans having formula (II) or N-alkylated 6-hydroxy morphinans having formula (III). | 04-01-2010 |
| 20100081821 | Berberine compounds and processes for the preparation of berberine compounds - The invention is directed to berberine compounds and processes for the preparation of berberine compounds through an intramolecular Bischler-Napieralski cyclization. | 04-01-2010 |
| 20100113788 | Process for the Preparation of 6-Alpha-Hydroxy-N-Alkylated Opiates - The present invention is directed to the preparation of 6-keto morphinans. | 05-06-2010 |
| 20100317683 | Preparation of 6-Alpha-Amino N-Substituted Morphinans by Catalytic Hydrogen Transfer - The present invention provides processes for the stereoselective synthesis of 6-alpha-amino N-substituted morphinans. In particular, the invention provides processes for the reductive amination of 6-keto N-substituted morphinans by catalytic hydrogen transfer. | 12-16-2010 |
| 20100317861 | Remove Amination of 6-Keto Normorphinans by Catalytic Hydrogen Transfer - 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. | 12-16-2010 |
| 20110015398 | 3-Oxy-Hydromorphone Derivatives - The present invention provides 3-oxy-hydromorphone derivatives, and in particular, 3-ester, 3-carbonate, and 3-sulfonate derivatives of hydromorphone. | 01-20-2011 |
| 20110071299 | One-Pot Preparation of Hexahydroisoquinolines from Amides - The present invention provides an efficient process for the preparation of hexahydroisoquinolines from amides. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines. | 03-24-2011 |
| 20110071300 | One-Pot Preparation of Hexahydroisoquinolines from Dihydroisoquinolines - The present invention provides an efficient process for the preparation of hexahydroisoquinolines from dihydroisoquinolines. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines. | 03-24-2011 |
| 20130137874 | One-Pot Preparation of Hexahydroisoquinolines from Amides - The present invention provides an efficient process for the preparation of hexahydroisoquinolines from amides. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines. | 05-30-2013 |
| 20130144053 | Process for the Production of Seven-Membered Lactam Morphinans - The present invention relates to improved processes for preparing lactam morphinans. The processes generally transform keto-morphinans to seven-membered lactam morphinans using a hydroxyamine sulfonic acid reagent and proceed in high yield and with good selectivity. | 06-06-2013 |
