专利号:US-8987503-B2 优先权日:2013-04-30 标 题 :Process for the synthesis of aminaphtone 发明人:BALDACCI MASSIMO; ROBERTI MARINELLA 权利人:BALDACCI LAB SPA 摘要:The present invention concerns a new process for the synthesis of aminaphtone, which makes use of non-toxic solvents and reagents, under mild reaction and temperature conditions. The aminaphtone obtained with the method of the present invention also has a purity of at least 98% in weight. The method comprises the following steps: a) epoxidating menadione 1 to provide epoxide 2, b) acidifying epoxide 2 to provide hydroxynaphthoquinone 3, c) esterifying between hydroxynaphthoquinone 3 and 4-aminobenzoyl chloride to obtain compound 4, and d) reducing compound 4 in the presence of a reducing agent in water to obtain aminaphtone.
专利号:US-9409879-B2 优先权日:2011-03-29 标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents 发明人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA 权利人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA; CENTRE NAT RECH SCIENT 摘要:Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.
专利号:US-4459227-A 优先权日:1981-03-02 标 题:Para-hydroxyphenylhydrazines as in situ precursors of iminoquinones and quinones 发明人:SAHMEL REINHARDT O; GRAHAM DOYLE G 权利人:UNIV DUKE 摘要:Iminoquinone precursors having the formula wherein R1 represents hydrogen or an enzymatically hydrolyzable group; R2 and R3 independently represent hydrogen, a non-electron-withdrawing organic substituent or an enzymatically hydrolyzable group except that when R1 is hydrogen, R2 must be an enzymatically hydrolyzable group and R3 must not inhibit the hydrolysis of R2; R4 represents hydrogen or an electron-withdrawing or non-electron-withdrawing organic substituent, except that if R1 is hydrogen, R4 may not inhibit the hydrolysis of R2; W, X, Y and Z independently represent hydrogen or an electron-withdrawing or non-electron-withdrawing organic substituent, or any one of X and W, Y and Z, or X and R4 taken together represents a cyclic or heterocyclic ring having 5 to 6 ring atoms; and wherein said enzymatically hydrolyzable group is selected so that a hydrolysis product is biologically benign for the biological system in which said precursor is present is produced by hydrolysis of the hydrolyzable group. Also disclosed are methods of synthesis and methods of use of these compounds.
专利号:SU-1763444-A1 优先权日:1990-05-08 标题 :Method for synthesis of sulfur-containing polymer
专利号:US-2014121238-A1 优先权日:2011-03-29 标 题:Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents
专利号:US-2014323747-A1 优先权日:2013-04-30 标 题:Process for the synthesis of aminaphtone
1: Moura-Alves P, Faé K, Houthuys E, Dorhoi A, Kreuchwig A, Furkert J, Barison N, Diehl A, Munder A, Constant P, Skrahina T, Guhlich-Bornhof U, Klemm M, Koehler AB, Bandermann S, Goosmann C, Mollenkopf HJ, Hurwitz R, Brinkmann V, Fillatreau S, Daffe M, Tümmler B, Kolbe M, Oschkinat H, Krause G, Kaufmann SH. AhR sensing of bacterial pigments regulates antibacterial defence. Nature. 2014 Aug 28;512(7515):387-92. doi: 10.1038/nature13684. Epub 2014 Aug 13. Epub 2014 Aug 5. 3: Gardner PR. Superoxide production by the mycobacterial and pseudomonad quinoid pigments phthiocol and pyocyanine in human lung cells. Arch Biochem Biophys. 1996 Sep 1;333(1):267-74. 8: QUAGLIARIELLO E, AURICCHIO S, SORDINO R, PIAZZA M. [Effects of phthiocol and menadione on the reaction of 3-hydroxyanthranilic acid to quinolinic acid; probable mechanism of action of their inhibiting effect]. Boll Soc Ital Biol Sper. 1957 Jan-Feb;33(1-2):159-62. Italian. Undetermined Language.
合成参考文献
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