专利号:US-11905296-B2 优先权日:2020-01-27 标题:Process for the synthesis of buprenorphine 发明人:ZINSER HARTMUT; DANIELYAN TAMAR; GRIGORYAN MERI; GHARIBYAN MARIAM; MOVSISYAN MIKAYEL; NERKARARYAN KRISTINE 权利人:AZAD PHARMA AG 摘要:The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of thebaine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolic-oxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.
专利号:US-8236877-B2 优先权日:2003-03-13 标 题 :Method of producing hybrid polymer-inorganic materials 发明人:KUMACHEVA EUGENIA 权利人:KUMACHEVA EUGENIA 摘要:Hybrid composite materials with multiscale morphologies are formed by doping polymer submicrometer spheres with semiconductor or metal (e.g. CdS or Ag, respectively) nanoparticles and using these doped microspheres as functional building blocks in production of hybrid periodically structured materials. The preparation of hybrid polymer particles include the following stages: (i) synthesis of monodisperse polymer microspheres, (ii) in-situ synthesis of the inorganic nanoparticles either on the surface, or in the bulk with polymer beads, and (iii) encapsulation of hybrid microspheres with a hydrophobic shell.
专利号:US-2021163438-A1 优先权日:2017-08-16 标题 :Synthesis of phytocannabinoids including a demethylation step 发明人:REEKIE TRISTAN; SCOTT MICHAEL; KASSIOU MICHAEL 权利人:UNIV SYDNEY 摘要:A method for demethylating a methylated phytocannabinoid compound of Formula I to form a phytocannabinoid compound of Formula II: Formula I Formula II wherein: R1 is selected from the group consisting of: substituted or unsubstituted C1-C5 alkyl; R2 is selected from the group consisting of: OH or O, and R3 is selected from the group consisting of: a substituted or unsubstituted cyclohexene, a substituted or unsubstituted C2-C8 alkene, or a substituted or unsubstituted C2-C8 dialkene; or R2 is O, and R2 and R3 together form a ring structure in which R2 is an internal ring atom; wherein the method includes: heating a reaction mixture comprising the methylated phytocannabinoid compounds and a polar aprotic solvent in the presence of a dissolved inorganic alkaline salt for a time sufficient to demethylate at least a portion of the methylated phytocannabinoid compounds and form the phytocannabinoid compound.
专利号:US-7902383-B2 优先权日:2006-05-29 标 题 :Production method of heterocyclic mercapto compound 发明人:YOROZUYA SHINICHI; AOKI HIDEMASA 权利人:SHOWA DENKO KK 摘要:A method of the invention industrially produces heterocyclic mercapto compounds useful as raw materials or intermediates in the synthesis of medicaments or pesticides, or as permanent wave agent, with a high yield and high productivity using easily available starting materials. A heterocyclic mercapto compound represented by Formula (1) (wherein X represents any structure of —O—, —S—, —NH—, and —NR 1 —; R 1 represents any of an alkyl group, alkoxy group and alkoxyalkyl group each having 1 to 6 carbon atoms; Y represents an oxygen atom, a sulfur atom or —NR 2 —; R 2 represents a hydrogen atom or alkyl group having 1 to 6 carbon atoms; and Z 1 represents a divalent organic residue having at least one mercapto group) is produced by reacting a metal sulfide or a metal hydrosulfide with a compound represented by Formula (2) (wherein X and Y are as defined in Formula (1); and Z 2 represents a divalent organic residue having at least one halogen group) in the presence of a solvent at a pH of 7.0 to 11.0.
专利号:US-10377729-B2 优先权日:2015-06-15 标题 :Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (FAP) 发明人:VIEIRA SIMÕES CARLOS JOSÉ; LOURENÇO DE ALMEIDA ZAIDA CATARINA; VASCONCELOS DIAS DE PINHO E MELO TERESA MARGARIDA; PONTES MEIRELES FERREIRA DE BRITO RUI MANUEL; SILVA COSTA DORA CRISTINA; CABRAL CARDOSO LOPES ANA LÚCIA 权利人:BSIM THERAPEUTICS S A 摘要:The design and synthesis of a novel bis-furan scaffold tailored for high efficiency at inhibiting transthyretin amyloid formation is reported. In vitro results show that the discovered compounds are more efficient inhibitors of amyloid formation than tafamidis, a drug currently used in the treatment of familial amyloid polyneuropathy (FAP), despite their lower molecular weight and lipophilicity. Moreover, ex vivo experiments with the strongest inhibitor in the series, conducted in human blood plasma from normal and FAP Val30Met-transthyretin carriers, disclose remarkable affinity and selectivity profiles. The promises and challenges facing further development of this compound are discussed under the light of increasing evidence implicating transthyretin stability as a key factor not only in transthyretin amyloidoses and several associated co-morbidities, but also in Alzheimer's disease.
专利号:US-11834470-B2 优先权日:2018-10-05 标题:4-thioribose NAD analogues and methods of synthesizing and using the same 发明人:ZHANG YONG; DAI ZHEFU; Zhang xiao-nan 权利人:UNIV SOUTHERN CALIFORNIA 摘要:This disclosure provides a method of synthesis of 4′-thioribose NAD+ and analogues thereof, using an efficient chemoenzymatic approach. Also provided are methods of inhibiting the CD38 enzyme and compounds including 4′-thioribose NAD+ and compounds related thereto.
摘要:Merck Index - O'Neil MJ, Heckelman PE, Dobbelaar PH, Roman KJ (eds). The Merck Index, An Encyclopedia of Chemicals, Drugs, and Biologicals, 15th Ed. Cambridge, UK: The Royal Society of Chemistry, 2013.