专利号:US-10968174-B2 优先权日:2016-12-21 标题:Synthesis of a thiosulfonic acid by a step of periodate mediated oxidative coupling of a thiosulfonic acid with an aniline 发明人:SINCLAIR JAMES PETER; NICOLL SARAH LOUISE; STOREY JOHN MERVYN DAVID; LARCH CHRISTOPHER PAUL 权利人:WISTA LAB LTD 摘要:The present invention pertains generally to the field of chemical synthesis, and more particularly to methods for the chemical synthesis of a thiosulfonic acid of Formula (1) by a step of periodate mediated oxidative coupling of a thiosulfonic acid of Formula (2) with an aniline of Formula (3), as described herein. The present invention also relates to such methods which incorporate one or more additional (subsequent and/or preceding) steps, for example, to prepare compounds of Formula (5) from compounds of Formula (1); to prepare compounds of Formula (6) from compounds of Formula (5); and to prepare compounds of Formula (2) from compounds of Formula (4), as described herein.
专利号:US-8691979-B2 优先权日:2009-05-12 标题 :Methods of chemical synthesis of diaminophenothiazinium compounds involving the use of persulfate oxidants 发明人:LARCH CHRISTOPHER PAUL; STOREY JOHN MERVYN DAVID; WILLIAMSON CRAIG; MARSHALL COLIN; KEMP STEVEN JOHN 权利人:LARCH CHRISTOPHER PAUL; STOREY JOHN MERVYN DAVID; WILLIAMSON CRAIG; MARSHALL COLIN; KEMP STEVEN JOHN; WISTA LAB LTD 摘要:Described are methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compoundsâ€?) including Methylhioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: a thiosulfonic acid formation (TSAF); an oxidative coupling (OC); and a ring closure (RC). Also described are resulting compounds and compositions comprising them (e.g., tablets, capsules) for use in methods of medical treatment and diagnosis, etc., for example, for tauopathies, or Alzheimer's disease (AD).
专利号:US-9574189-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries 发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK 权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS 摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
专利号:US-8143423-B2 优先权日:2007-03-22 标 题 :N-heterocyclic carbene (NHC) catalyzed synthesis of hydroxamic acids 发明人:ZHANG YUGEN; YING JACKIE Y; SEAYAD JAYASREE; WONG FONG TIAN; PATRA PRANAB K 权利人:ZHANG YUGEN; YING JACKIE Y; SEAYAD JAYASREE; WONG FONG TIAN; PATRA PRANAB K; AGENCY SCIENCE TECH & RES 摘要:A process for preparing hydroxamic acids is provided. The process comprises reacting an aldehyde with a nitroso compound in the presence of a N-heterocyclic carbene (NHC) catalyst.
专利号:US-9765042-B2 优先权日:2013-10-07 标题 :Methods of chemical synthesis of diaminophenothiazinium compounds including methylthioninium chloride (MTC) 发明人:SINCLAIR JAMES PETER; NICOLL SARAH LOUISE; STOREY JOHN MERVYN DAVID 权利人:WISTA LAB LTD 摘要:Methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compoundsâ€?) including Methythioninium Chloride (MTC) (also known as Methylene Blue) are provided.
专利号:US-9980971-B2 优先权日:2006-07-11 标 题:Methods of synthesis and/or purification of diaminophenothiazinium compounds 发明人:WISCHIK CLAUDE MICHEL; STOREY JOHN MERVYN DAVID; MARSHALL COLIN; SINCLAIR JAMES PETER; BADDELEY THOMAS CRAVEN 权利人:WISTA LAB LTD 摘要:Disclosed are methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (“diaminophenothiazinium compoundsâ€?) including Methylthioninium Chloride (MTC) (Methylene Blue), and the resulting high purity characterized by a purity greater than 98%, and very low levels of heavy metals and organic impurities Azure A, B, C and MVB. Also disclosed are methods of treatment of a tauopathy or methemoglobinemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of the high-purity diaminophenothiazinium compound.
摘要:Sainsbury, M., Science of Synthesis Knowledge Updates, (2010) 1, 262. 摘要:International Labour Office. Encyclopedia of Occupational Health and Safety. Volumes I and II. New York: McGraw-Hill Book Co., 1971., p. 96 摘要:International Labour Office. Encyclopedia of Occupational Health and Safety. Volumes I and II. New York: McGraw-Hill Book Co., 1971., p. 93 摘要:Clayton, G. D. and F. E. Clayton (eds.). Patty's Industrial Hygiene and Toxicology: Volume 2A, 2B, 2C: Toxicology. 3rd ed. New York: John Wiley Sons, 1981-1982., p. 2476 摘要:Weast, R.C. (ed.). Handbook of Chemistry and Physics. 60th ed. Boca Raton, Florida: CRC Press Inc., 1979., p. C-115