专利号:US-9840468-B1 优先权日:2016-12-30 标 题:Methods for the preparation of 6-aminoisoquinoline 发明人:CHAMBOURNIER GILLES; DELONG MITCHELL A 权利人:AERIE PHARMACEUTICALS INC 摘要:Described are methods for the preparation of 6-aminoisoquinoline, a useful intermediate compound in the synthesis of kinase inhibitors.
专利号:WO-2013035102-A1 优先权日:2011-09-05 标 题 :Processes for the preparation of imatinib base and intermediates thereof 发明人:KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD; KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 摘要:The invention relates to an improved process for the preparation of highly pure imatinib base (99.99% HPLC purity) of formula (I) and the pharmaceutically acceptable acid addition salts thereof. This invention also relates to processes for the preparation of the intermediates in the synthesis of imatinib base.
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-7718598-B1 优先权日:1998-09-25 标 题:Auxiliary for amide bond formation 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programmes. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganizing peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-11884714-B2 优先权日:2019-03-01 标 题:Cyclic peptide analogs of melanocortin and amanitin and methods of making such 发明人:PERRIN DAVID; TODOROVIC MIHAJLO; BÉNARD FRANÇOIS; ZHANG CHENGCHENG 权利人:UNIV BRITISH COLUMBIA; PROVINCIAL HEALTH SERVICES AUTHORITY 摘要:The invention described herein is based in part on the discovery of a protein/peptide crosslink, which introduces fluorescent properties, and which has been applied to synthesize analogues of melanocortin and amanitin as choice peptides to be explored in the context of isoindole peptides. Without limitation, it is expected that those trained in the art of peptide synthesis and stapling would appreciate the consequences of this invention such that other peptides of varied length can be similarly constrained by isoindole staples as featured herein.
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.
摘要:Weast, R.C. (ed.). Handbook of Chemistry and Physics. 60th ed. Boca Raton, Florida: CRC Press Inc., 1979., p. C-163 摘要:Weast, R.C. and M.J. Astle. CRC Handbook of Data on Organic Compounds. Volumes I and II. Boca Raton, FL: CRC Press Inc. 1985., p. V2 439 摘要:Hawley, G.G. The Condensed Chemical Dictionary. 9th ed. New York: Van Nostrand Reinhold Co., 1977., p. 620 摘要:SHUTOVA ET AL; GAS-CHROMATOGRAPHIC DETERMINATION OF NITROXYLENE ISOMERS IN WASTE WATERS FROM NITROXYLENE PRODUCTION, KHIM PROM-ST, SER: METODY ANAL KONTROLYA KACH PROD KHIM PROM-STI 8: 7 (1979) 摘要:2024 Emergency Response Guidebook, https://www.phmsa.dot.gov/training/hazmat/erg/emergency-response-guidebook-erg