| Patent application number | Description | Published |
|---|
| 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 |
| 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 |
| 20100081817 | Processes for the selective amination of ketomorphinans - The present invention is generally directed to a process for the preparation of a ketomorphinan comprising maintaining a ketone group as unprotected and performing reductive amination using a hydrogen source and a catalyst. | 04-01-2010 |
| 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 |
| 20100197921 | Preparation of N-Alkylated Opiates by Reductive Amination - The present invention is directed to the reduction of an N-imine moiety or a hemiaminal moiety of a morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source. | 08-05-2010 |
| 20100216995 | (+)-6-Hydroxy-Morphinan or (+)-6-Amino-Morphinan Derivatives - The present invention provides (+)-morphinanium compounds comprising substituted 6-hydroxy or 6-amine groups. The invention also provides methods for inhibiting microglial activation by administering the compounds of the invention. | 08-26-2010 |
| 20100216996 | (+)-Morphinanium Quaternary Salts and Processes for their Production - The present invention provides (+)-morphinanium quaternary salts. The invention also provides processes for producing (+)-morphinanium quaternary salts from tertiary N-substituted (+)-morphinan compounds. | 08-26-2010 |
| 20100216997 | (+)-Morphinanium N-Oxides and Processes for their Production - The present invention provides (+)-morphinanium N-oxide compounds or pharmaceutically acceptable salts thereof. The invention also provides processes for producing (+)-morphinanium N-oxides or pharmaceutically acceptable salts thereof from the corresponding tertiary N-substituted (+)-morphinan compound or pharmaceutically acceptable salt thereof. | 08-26-2010 |
| 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 |
| 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 |
| 20110136845 | (+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof - The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat pain. Also provided are pharmaceutical combination compositions comprising a (+)-morphinan and an opioid agonist/monoamine reuptake inhibitor, as well as methods for using the combination compositions to treat pain. | 06-09-2011 |
| 20120316343 | Reductive Amination of 6-Keto Morphinans by Catalytic Hydrogen Transfer - The present invention provides compositions of 6-amino morphinan compounds and process for their synthesis. In particular, the processes provide for the reductive amination of 6-keto morphinans by catalytic transfer hydrogenation, to produce 6-amino morphinan compounds, which are epimerically and/or diastereomerically enriched. | 12-13-2012 |
| 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 |
| 20140031543 | (+)-6-Hydroxy-Morphinan or (+)-6-Amino-Morphinan Derivatives - The present invention provides (+)-morphinanium compounds comprising substituted 6-hydroxy or 6-amine groups. The invention also provides methods for inhibiting microglial activation by administering the compounds of the invention. | 01-30-2014 |
