专利号:US-6355826-B1 优先权日:1997-09-17 标题:Synthesis of stable nitrile oxide compounds 发明人:PARKER DANE KENTON 权利人:GOODYEAR TIRE & RUBBER 摘要:This invention discloses a process for the synthesis of stable aryl nitrile oxides which comprises the sequential steps of (1) halomethylating a halomethyl group onto a substituted aromatic compounds wherein said halomethyl group is halomethylated onto a position that is ortho to at least one of the substituent groups on the substituted aromatic compound; (2) converting the ortho halomethylated-substituted aromatic compound into an ortho-substituted aromatic aldehyde by reacting the ortho halomethylated-substituted aromatic compound with a salt selected from the group consisting of sodium 2-nitropropane and potassium 2-nitropropane in a lower alcohol solvent; (3) converting the ortho-substituted aromatic aldehyde into an ortho-substituted aromatic; and (4) converting the ortho-substituted aromatic oxime into the ortho-substituted aryl nitrile oxide by reacting the ortho-substituted aromatic oxime with an aqueous sodium hypochlorite solution.
专利号:US-8106031-B2 优先权日:2006-05-02 标题:Hydrolytically-resistant boron-containing therapeutics and methods of use 发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A 权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:US-7884128-B2 优先权日:2005-10-13 标题:Process for total synthesis of pladienolide B and pladienolide D 发明人:KANADA REGINA MIKIE; ITO DAISUKE; SAKAI TAKASHI; ASAI NAOKI; KOTAKE YOSHIHIKO; NIIJIMA JUN 权利人:EISAI R&D MAN CO LTD 摘要:Process for producing compound of Formula: n nwherein P 2 , P 3 and R 2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7):n n nwherein P 3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8):n n nwherein P 2 means a protecting group for hydroxy group; and R 2 means a phenyl group which may be substituted, in the presence of a base.
专利号:US-7803955-B2 优先权日:2005-06-16 标 题:Method for preparing 2,5,7,8-tetramethyl-2-(2′-carboxyethyl)-6-acetoxychroman-precursor- α-CEHC precursor 发明人:SPIVAK ANNA YULIEVNA; ODINOKOV VIKTOR NIKOLAEVICH; KNYSHENKO OXANA VALERIEVNA 权利人:INST NEFTEKHIMII I KATALIZA RA 摘要:The contemplated invention relates to the field of synthesis of biologically active substances, namely to the synthesis of an acetate derivative of the main water-soluble α-tocopherol metabolite known under the name of α-CEHC, which is prepared by the acid-catalyzed reaction of condensation of trimethyl hydroquinone with linalool in boiling octane, using n-toluenesulfonic acid or (+)-camphor-10-sulfonic acid as the catalyst. The reaction is carried out for 3 hours at the trimethyl hydroquinone:linalool:catalyst mole ratio of 1:1:0.1. The forming product is acetylated with acetic anhydride in pyridine at room temperature for 0.5 hour, and then ozonized in acetone in the presence of Ba(OH) 2 , oxidized with Jones' reagent in acetone, and isolated on silica gel column chromatography. n Said compound is an acetate derivative of the main α-tocopherol metabolite—α-CEHC, for which high efficiency has been noted in treating disorders of the central nervous system.
专利号:US-7612064-B2 优先权日:2003-05-26 标题:Sulfopyrroles 发明人:EBERLE MARTIN; ERMERT PHILIPP; OBRECHT DANIEL; LACH FRANK; LUTHER ANATOL; BACHMANN FELIX; STREBEL ALLESSANDRO 权利人:TAKEDA PHARMACEUTICAL 摘要:The invention relates to compounds of formula (I) wherein R 1 represents aryl, aralkyl or heteroaryl, R 2 is aryl or heteroaryl and R 3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.
专利号:CN-114940668-A 优先权日:2022-03-23 标题 :Preparation of a catalyst and its application in the synthesis of vitamin E acetate
[参考文献]: S B Matin, Et Al. Stereochemical Aspects And Metabolite Formation In The In Vivo Metabolism Of The Psychotomimetic Amine, 1-(2,5-Dimethoxy-4-Methylphenyl)-2-Aminopropane. J Med Chem. 1974 Aug;17(8):877-82.
合成参考文献
摘要:Krohn, K.; Böker, N., Science of Synthesis, (2006) 28, 381. 摘要:Kim, S. H.; Theodorakis, E. A., Science of Synthesis, (2006) 28, 57. 摘要:Balci, M.; Gültekin, M. S.; Çelik, M., Science of Synthesis, (2006) 28, 116. 摘要:von Angerer, S.; Warriner, S. L., Science of Synthesis, (2007) 29, 368.