专利号:US-2019127389-A1 优先权日:2016-04-22 标题 :Processes And Oxazolidine-Containing Intermediates For The Preparation Of Morphine Analogs And Derivatives 发明人:KAPPE CHRISTOPHER OLIVER; GUTMANN BERNHARD; WEIGL ULRICH; EGLI PATRICK; COX DOUGLAS PHILLIP; CANTILLO DAVID 权利人:NORAMCO INC 摘要:The present invention relates to processes useful in the preparation of morphine analogs and derivatives, such as naltrexone, naloxone and nalbuphine and intermediates in the synthesis of said morphine analogs and derivatives. In a particular example, the process begins with for example oxymorphone, oxycodone, 14-hydroxycodeinone or 14-hydroxymorphinone, and includes the formation of an oxazolidine-containing intermediate using catalytic oxidation.
专利号:US-9045497-B1 优先权日:2011-05-02 标 题:Processes and intermediates in the preparation of morphine analogs via N-demethylation of N-oxides using cyclodehydration reagents 发明人:HUDLICKY TOMAS; WERNER LUKAS; MACHARA ALES; WERNEROVA MARTINA; ENDOMA-ARIAS MARY ANN 权利人:UNIV BROCK 摘要:A high-yielding method for the N-demethylation of oxycodone- and oxymorphone-N-oxides by the reaction of these compounds with cyclodehydration reagents has been performed. This method has been utilized to improve the synthesis of various morphine analogs, such as naltrexone, nalbuphone and naloxone.
专利号:US-8981098-B2 优先权日:2012-02-03 标题 :Process for the preparation of morphine analogs via the reaction of organometallic reagents with an oxazolidine derived from morphinans 发明人:HUDLICKY TOMAS; ENDOMA-ARIAS MARY ANN 权利人:HUDLICKY TOMAS; ENDOMA-ARIAS MARY ANN; UNIV BROCK 摘要:The oxazolidine derived from the reaction of oxymorphone with the Burgess reagent, temporarily protected at O-3 and C-6, reacts with Grignard or other suitable metallic or organometallic reagents to directly provide, for example, A/-allyl, A/-methylcyclopropyl and /V-methylcyclobutyl derivatives that are further converted into naltrexone, naloxone, nalbuphone and nalbuphine in excellent yields. These morphine analogs can be prepared from the oxazolidine in a one-pot synthesis.
专利号:CN-101535336-A 优先权日:2006-11-10 标题 :Synthesis of Phthalamide and Its Dimer
专利号:CN-101627049-B 优先权日:2006-11-10 标题 :Synthesis of phthalamides
专利号:US-2014315720-A1 优先权日:2012-10-24 标 题 :Polysaccharide ester microspheres and methods and articles relating thereto 发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY 权利人:CELANESE ACETATE LLC 摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.