专利号:US-11717498-B2 优先权日:2013-12-31 标题 :Methods of treatment using amphetamine controlled release, prodrug, and abuse deterrent dosage forms 发明人:POPP KARL; MECKLER HAROLD 权利人:Chemapotheca LLC; PHARMAPOTHECA A INC 摘要:The invention also relates to pharmaceutical compositions comprising highly pure amphetamine and amphetamine-class compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds, and to methods of manufacturing, delivering, and using the amphetamine compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds.
专利号:US-9802952-B2 优先权日:2013-07-15 标 题:Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives 发明人:KOPETZKI DANIEL; MCQUADE DAVID TYLER; SEEBERGER PETER H; GILMORE KERRY 权利人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V; MAX-PLANK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V 摘要:The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C 1 -C 5 alcohol.
专利号:WO-2013121018-A1 优先权日:2012-02-17 标题 :Synthesis of cyanocarboxylic acid alkyl esters 发明人:FRANZKE CONSTANZE; OTT LOTHAR; GRUETZNER THOMAS; LITZMANN OLIVER; REPKE JENS-UWE; HAMMANN MARKUS; LORENZ HILKE-MARIE; MEEMKEN FABIAN CARL INGOLD 权利人:LONZA AG 摘要:Provided is a process for obtaining a compound of formula (I): N≡C-CH 2 -A-C(O)-OR, wherein Hal is halogen selected from F, Cl, Br or I, A denotes a bond or a divalent spacer selected from alkylene and arylene groups, and R is a C 1-4 alkyl group, by reacting a compound of formula (II): Hal-CH 2 -A-C(O)-OR, wherein Hal is a halogen atom selected from F, Cl, Br and I, and wherein A and R are as defined above, with hydrogen cyanide in the presence of a first base, wherein the molar ratio between hydrogen cyanide and said first base is from 1:0.3 to 1:0.95 and the molar ratio between hydrogen cyanide to the compound of formula (II) is at least 1:1.
专利号:US-6444460-B1 优先权日:1998-08-19 标 题:Microbial production of actinol 发明人:SHIMIZU SAKAYU; WADA MASARU 权利人:ROCHE VITAMINS INC 摘要:A process for making (4R, 6R)-4-hydroxy-2,2,6-trimethylcyclohexanone by contacting (6R)-2,2,6-trimethylcyclohexanedione with a microorganism which is selected from microorganisms of the genera Cellulomonas, Corynebacterium, Planococcus and Arthrobacter and which is capable of the selective asymmetric reduction of (6R)-2,2,6-trimethylcyclohexanedione to (4R, 6R)-4-hydroxy-2,2,6-trimethylcyclohexanone, and recovering the resulting (4R, 6R)-4-hydroxy-2,2,6-trimethylcyclohexanone from the reaction mixture. The selective asymmetric reduction can be effected in the presence of a co-factor, such as, nicotinamide adenine dinucleotide (NAD), nicotinamide adenine dinucleotide phosphate (NADP), or said co-factor with glucose and glucose dehydrogenase (GDH), and/or in the presence of a surfactant. The product is useful for the synthesis of carotenoids, such as, zeaxanthin.
专利号:US-6281245-B1 优先权日:1996-10-28 标 题:Methods for solid-phase synthesis of hydroxylamine compounds and derivatives, and combinatorial libraries thereof 发明人:PATEL DINESH V; NGU KHEHYONG 权利人:VERSICOR INC 摘要:A novel method for generating hydroxylamine, hydroxamic acid, hydroxyurea, and hydroxylsulfonamide compounds is disclosed. The method involves the nucleophilic attack of an alkoxyamine on a suitable solid phase support. Techniques of combinatorial chemistry can then be applied to the immobilized alkoxyamine to generate a diverse set of compounds. Cleavage of the compounds from the support yields a library of hydroxylamine or hydroxylamine derivative compounds, which can be screened for biological activity (e.g., inhibition of metalloproteinases).
专利号:US-8344168-B2 优先权日:2006-06-14 标题 :Process for the preparation of fluticasone propionate 发明人:GORE VINAYAK G; GADAKAR MAHESH; POKHARKAR K; WAKCHURE V 权利人:GENERICS UK LTD; GORE VINAYAK G; GADAKAR MAHESH; POKHARKAR K; WAKCHURE V 摘要:The present invention relates to a process for the preparation of steroidal 17β-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17β-carboxylic thioates, such as fluticasone propionate I, using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds II resulting in selective and controlled fluorination. The present invention also relates to intermediates II and their preparation.
[参考文献]: C J Reid, Et Al. Aspartate Transport By The Dct System In Rhizobium Leguminosarum Negatively Affects Nitrogen-Regulated Operons. Microbiology (Reading). 1996 Sep:142 ( Pt 9):2603-12. [参考文献]: Caroline Wardrope, Et Al. Fumarate Reductase: Structural And Mechanistic Insights From The Catalytic Reduction Of 2-Methylfumarate. Febs Lett. 2006 Mar 6;580(6):1677-80. [参考文献]: Emma Heart, Et Al. Ca2+, Nad(P)H And Membrane Potential Changes In Pancreatic Beta-Cells By Methyl Succinate: Comparison With Glucose. Biochem J. 2007 Apr 1;403(1):197-205. [参考文献]: I Valverde, Et Al. Stimulation Of Insulin Release In Vivo By The Methyl Esters Of Succinic Acid And Glutamic Acid. Adv Exp Med Biol. 1997:426:231-4. [参考文献]: Ismail Syed, Et Al. Phagocyte-Like Nadph Oxidase Generates Ros In Ins 832/13 Cells And Rat Islets: Role Of Protein Prenylation. Am J Physiol Regul Integr Comp Physiol. 2011 Mar;300(3):R756-62.
合成参考文献
参考文献:10.1107/s160053681004585x 摘要:Matulková I, Císařová I, Němec I. 2-Phenyl-biguanidinium hydrogen succinate methanol monosolvate. Acta Crystallogr Sect E Struct Rep Online. 2010 Nov 17;66(Pt 12):o3187–8. 参考文献:10.1186/s40793-017-0220-z|10.1186/s40793-017-0283-x 摘要:Aserse AA, Woyke T, Kyrpides NC, Whitman WB, Lindström K. Draft genome sequences of Bradyrhizobium shewense sp. nov. ERR11T and Bradyrhizobium yuanmingense CCBAU 10071T. Environmental Microbiome. 2017 Dec 05;12(1):74. doi: 10.1186/s40793-017-0283-x. 参考文献:10.1152/ajpendo.00041.2002 摘要:MacDonald MJ. Differences between mouse and rat pancreatic islets: succinate responsiveness, malic enzyme, and anaplerosis. American Journal of Physiology-Endocrinology and Metabolism. 2002 Aug 01;283(2):E302–10. doi: 10.1152/ajpendo.00041.2002.