专利号:US-9024030-B2 优先权日:2012-01-13 标题 :Process for the synthesis of etoricoxib 发明人:MAO ZHENMIN; LAN TIAN; LIU LANFANG; YAN LONG; BECKER STEFAN 权利人:TIEFENBACHER ALFRED E GMBH & CO KG; SHANGHAI GOLDEN PHARMATECH CO LTD; SHANGHAI GOLDEN PHARMATECH CO LTD 摘要:The present invention relates to a process for the synthesis of the anti-inflammatory agent 5-chloro-3-(4-methanesulfonylphenyl)-6′-methyl-[2,3′]bipyridine, referred to as compound of formula (1) or etoricoxib, which is a pharmaceutically active ingredient inhibiting cyclooxygenase-2. In particular, the application concerns a novel process of making the compound of formula (1) by oxidizing a compound of formula (4).
专利号:US-5712407-A 优先权日:1997-01-14 标题 :Method for the preparation of alpha-chlorinated chloroformates 发明人:KREUTZBERGER CHARLES B; ESWARAKRISHNAN SEETHA; DAMLE SURESH B 权利人:PPG INDUSTRIES INC 摘要:Novel catalysts for the synthesis of a alpha-chlorinated chloroformate from an aldehyde and phosgene are described. The catalysts include alkyl substituted guanidines, hexasubstituted guanidinium chlorides, substituted biguanidinium chloride, phenyldialkyliminiumtetraalkylguanidinium chloride, dialkylimidazolinium tetraalkylguanidinium chloride, phenyltetraalkylamidinium chloride and N,N-dialkyl-N'-alkylpyrrolidinium chloride.
专利号:US-6891069-B1 优先权日:2004-01-30 标 题:Synthesis of 4-substituted phthalaldehyde 发明人:ZHU PETER C; WANG DER-HAW 权利人:ETHICON INC 摘要:Disclosed herein are methods of synthesizing a 4-substituted-benzene-1,2-carbaldehyde. In one aspect, a method may include reacting a 4-substituted-1,2-bis(dibromomethyl) benzene with sulfuric acid to form a reaction product, introducing a solid sodium bicarbonate into the reaction product, and hydrolyzing the reaction product to form a 4-substituted-benzene-1,2-carbaldehyde, after introducing the bicarbonate.
专利号:US-7476767-B2 优先权日:2004-01-30 标题:Alpha-hydroxy sulfonate aldehydes, germicidal compositions containing the alpha-hydroxy sulfonate aldehydes, or mixtures of alpha-hydroxy sulfonate aldehydes and phthalaldehydes, and methods of using the compounds or compositions for disinfection or sterilization 发明人:ZHU PETER C; ROBERTS CHARLES G; TRAN YVONNE 权利人:ETHICON INC 摘要:Disclosed herein are α-Hydroxy sulfonate aldehydes and synthesis methods therefor. Germicidal compositions including the α-hydroxy sulfonate aldehydes, are also disclosed. In one aspect, a germicidal composition may include a diluent, and a germicidally effective amount of a water-soluble germicidal compound including an aldehyde group and an α-hydroxy sulfonate group. The water-soluble compound may have a solubility of at least 5 (w/v) % in water. In a further aspect, the compound may include 1-hydroxy-3-oxo-2-phenyl-propane-1-sulfonic acid salt, (2-formyl-phenyl)-hydroxy-methane sulfonic acid salt, 1-hydroxy-2-(4-methanesulfonyl-2-nitro-phenyl)-3-oxo-propane-1-sulfonic acid salt, 2-bromo-1-hydroxy-3-oxo-propane-1-sulfonic acid salt, 2-chloro-1-hydroxy-3-oxo-propane-1-sulfonic acid salt, 2-(1-formyl-2-hydroxy-2-sulfo-ethyl)-isonicotinic acid salt, 2-benzooxazol-2-yl-1-hydroxy-3-oxo-propane-1-sulfonic acid salt, or 1-hydroxy-2-(4-methoxy-phenyl)-3-oxo-propane-1-sulfonic acid salt. Germicidal compositions including a mixture of an α-hydroxy sulfonate aldehyde and one or more phthalaldehydes, such as phthalaldehyde, isophthalaldehyde, terephthalaldehyde, or a combination thereof, are also disclosed. Methods of using the compounds or compositions for killing bacteria, disinfection, or sterilization, are also disclosed.
专利号:US-8624035-B2 优先权日:2008-10-22 标题 :Functionalized cyanine having a silane linker arm, a method of preparing thereof and uses thereof 发明人:CAPUTO GIUSEPPE; MILETTO IVANA; BERTOLINO CHIARA ALESSANDRA; MARTRA GIANMARIO; COLUCCIA SALVATORE 权利人:CAPUTO GIUSEPPE; MILETTO IVANA; BERTOLINO CHIARA ALESSANDRA; MARTRA GIANMARIO; COLUCCIA SALVATORE; UNIV DEGLI STUDI TORINO 摘要:A silane-modified cyanine of Formula (I) includes the valence tautomers thereof: wherein R 1 is a linear, saturated or unsaturated alkyl chain, having 1 to 30 carbon atoms, wherein one or more carbon atoms are optionally substituted by a 4-, 5- or 6-membered aromatic or non aromatic cyclic grouping of carbon atoms; R 8 and R 9 are independently selected from the group consisting of —OCH 3 , —OCH 2 CH 3 , —OCH 2 CH 2 CH 3 , —OCH(CH 3 ) 2 , —OCH 2 CH 2 OCH 3 , —Cl, —Br, —I, Formula (II), Formula (III), —N(CH 3 ) 2 , Formula (IV), Formula (V), methyl, ethyl, propyl, isopropyl. The synthesis method and the use as a fluorescent marker are for inorganic solid supports, for example silica nanoparticles, and/or for biomolecules such as peptides, antibodies, DNA, RNA, etc.
专利号:US-7892297-B2 优先权日:2003-08-12 标题 :Cyanin-type compounds having an alkynyl linker arm 发明人:CAPUTO GIUSEPPE 权利人:CYANINE TECHNOLOGIES S P A 摘要:Cyanine-type fluorescent dyes modified with an alkynyl linker arm of formula (I), suitable for the conjugation of biomolecules, such as for example nucleosides, nucleotides, oligonucleotides, nucleic acids, proteins, peptides, vitamins and hormones. A method and intermediates for the synthesis of the alkynyl cyanines of the invention are also described, as well as alkynyl cyanine-biomolecule conjugates and methods for preparing thereof. The alkynyl cyanines can be advantageously used as markers for biomolecules or as quenchers.
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 30. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 288. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 187.