专利号:US-8586765-B2 优先权日:2007-12-21 标题 :Process for the synthesis of 3-amino-3-cyclobuthylmethyl-2-hydroxypropionamide or salts thereof 发明人:DONG SHUAN; PARK JEONGHAN; VATER EUGENE JOHN 权利人:DONG SHUAN; PARK JEONGHAN; VATER EUGENE JOHN; MERCK SHARP & DOHME 摘要:A process for preparing 3-amino-3-cyclobutylmethyl-2-hydroxypropionamide of the Formula I: n nor a salt thereof involves providing a compound of the Formula VI described herein in a solution comprising predominately dimethylsulfoxide (DMSO) and converting this compound directly to the compound of the Formula VIII described herein without working up or isolating the intermediate compound of the Formula VII described herein.
专利号:US-4089855-A 优先权日:1976-04-23 标题:Process for the stereoselective reduction of 6- and 8-keto morphine and morphinan derivatives with formamidinesulfinic acid and compounds obtained thereby 发明人:CHATTERJIE NITHIANANDA; INTURRISI CHARLES E 权利人:CORNELL RES FOUNDATION INC 摘要:Process for the stereoselective synthesis of 6β-and 8β- hydroxy epimers by the chemical reduction of 6- and 8-keto derivatives in the morphine and morphinan series utilizing alkaline formamidinesulficic acid. The 6β- and 8β-hydroxy derivatives obtained according to the invention evidence narcotic antagonist and/or agonist activity and are also useful in the chemical and pharmacological standardization of various morphine and codeine derivatives and metabolites.
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-9346853-B2 优先权日:2012-06-20 标 题 :Synthesis of telaprevir and boceprevir, or pharmaceutically acceptable salts or solvates as well as intermediate products thereof including β-amino acids prepared via Mukaiyama aldol addition 发明人:HOEFERL-PRANTZ KATHRIN; FELZMANN WOLFGANG; WILHELM THORSTEN; BENITO-GARAGORRI DAVID 权利人:SANDOZ AG 摘要:The invention relates to synthetic routes for preparing telaprevir and boceprevir, and its intermediates as well as peptides other than telaprevir. The synthetic routes are based on a Mukaiyama aldol addition reaction of a silyl enol ether or an enolate with an imine. The invention also refers to novel intermediates for preparing telaprevir/boceprevir or other peptides.
专利号:US-9657030-B2 优先权日:2010-06-11 标 题 :Transition metal-catalyzed processes for the preparation of N-allyl compounds and use thereof 发明人:GIGUERE JOSHUA ROBERT; MCCARTHY KEITH EDWARD; REISCH HELGE ALFRED; SANDOVAL SERGIO; STYMIEST JAKE LARRY 权利人:RHODES TECH 摘要:The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
[参考文献]: Markus Nett, Et Al. Function-Oriented Biosynthesis Of Beta-Lactone Proteasome Inhibitors In Salinispora Tropica. J Med Chem. 2009 Oct 8;52(19):6163-7. [参考文献]: Michael Decker, Et Al. Synthesis And Opioid Receptor Binding Affinities Of 2-Substituted And 3-Aminomorphinans: Ligands For Mu, Kappa, And Delta Opioid Receptors. J Med Chem. 2010 Jan 14;53(1):402-18. [参考文献]: Usama M Hegazy, Et Al. Replacement Surgery With Unnatural Amino Acids In The Lock-And-Key Joint Of Glutathione Transferase Subunits. Chem Biol. 2006 Sep;13(9):929-36.
合成参考文献
摘要:Li, L.; Biscoe, M. R., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 797.