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 |
20080293947 | Method of Preparation for Imidazolepyridines - The present invention relates to an improved process for preparing imidazo[1,2-a]pyridine-3-acetamides and more particularly, 6-methyl-2-p-tolylH-imidazo[1,2-a]pyridine. | 11-27-2008 |
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 |
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 |
20100048905 | Novel Opiate Reduction Utilizing Catalytic Hydrogen Transfer Reaction - An improved opiate synthesis scheme is provided. An improvement to the oxidation of oripavine and oripavine derivatives comprises the in-situ formation of the peroxacids required to oxidize the oripavine and oripavine derivatives to form an intermediate. An improvement to the reduction of the intermediate to form oxycodone and oxycodone derivatives comprises reduction utilizing a hydrogen transfer reagent. These improvements allow the production of oxycodone and oxycodone derivatives without isolation of the intermediate, providing a one-pot synthesis method. | 02-25-2010 |
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 |
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 |
20100113787 | Preparation of Oxymorphone from Oripavine - An improved method for the preparation of oxymorphone from oripavine is provided. Oripavine is oxidized to form 14-hydroxymorphinone after which the oxidation reaction is quenched to prevent the formation of 1-1′-dimer side products. The 14-hydroxymorphinone is then reduced, typically by catalytic hydrogenation to form oxymorphone. The inventive method disclosed is further applicable to the production of morphinan derivatives. | 05-06-2010 |
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 |