专利号:US-2023286918-A1 优先权日:2020-07-02 标 题:Manufacturing process for 3,5-dichloropicolinonitrile for synthesis of vadadustat 发明人:JURKAUSKAS VALDAS; JUNG YOUNG CHUN; KWON TAESOO; KANNAN ARUNACHALAM; GONDI VIJAYA BHASKER 权利人:AKEBIA THERAPEUTICS INC 摘要:Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the synthesis of vadadustat.
专利号:US-2013338369-A1 优先权日:2011-03-07 标 题 :Process for the Synthesis of Aminobiphenylene 发明人:HEINRICH MARKUS; PRATSCH GERALD 权利人:HEINRICH MARKUS; PRATSCH GERALD; BASF SE 摘要:The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.
专利号:US-12037623-B2 优先权日:2018-07-09 标 题 :Enzymatic synthesis of 4′-ethynyl nucleoside analogs 发明人:HUFFMAN MARK A; FRYSZKOWSKA ANNA; KOLEV JOSHUA N; DEVINE PAUL N; CAMPOS KEVIN R; TRUPPO MATTHEW; NAWRAT CHRISTOPHER C 权利人:MERCK SHARP & DOHME; MERCK SHARP & DOHME LLC 摘要:The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.
专利号:US-4365094-A 优先权日:1979-12-28 标 题 :Process for the synthesis of tertiary phosphine oxides, and new tertiary phosphine oxides 发明人:BOILEAU SYLVIE L; N GUYEN THANH-DUNG; GAUTIER JEAN-CLAUDE C 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The invention relates to the synthesis of tertiary phosphine oxides and also to certain tertiary phosphine oxides. According to the invention, an organic phase containing a halogenomethyl derivative, a secondary phosphine oxide and a phase transfer catalyst in an organic medium is reacted with an aqueous phase containing an inorganic base. The halogenomethyl derivative can be a micromolecule or a macromolecule. The tertiary phosphine oxides are substances which are useful, in particular, in fireproofing, in hydrometallurgy and in the field of plant health.
专利号:US-2024199658-A1 优先权日:2022-12-01 标 题:Direct synthesis of organotin alkoxides 发明人:JILEK ROBERT E; REED CHRISTOPHER J; NOVAS BRYAN 权利人:INPRIA CORP 摘要:Synthesis techniques are described for forming organotin trialkoxide compounds via direct alkylation of tin alkoxides. A first method involves reacting an alkali metal tin trialkoxide with an organohalide compound (RXn, where X is a halide atom and n≥1) to form a monoorgano tin trialkoxide represented by the formula R[Sn(OR′)3]n. The method can be used to form polytin trialkoxide compounds with a plurality of radiation sensitive C—Sn bonds. R and R′ include organo groups and can optionally comprise hetero-atoms and/or unsaturated bonds. A second method involves the ultraviolet light-driven reaction of a di-tin tetraalkoxide with an organohalide compound (RX) to form a monoorgano trialkoxide represented by the formula RSn(OR′)3. A third method involves the visible or ultraviolet light-driven reaction of a di-tin tetraalkoxide or an alkali metal tin trialkoxide with an fluorinated organohalide compound (RFX) to form a fluorinated monoorgano trialkoxide represented by the formula RFSn(OR′)3. The disclosed methods provide for high mono-organo specificity. Corresponding organotin trialkoxide compositions are also described. The compositions are useful for radiation patterning, especially with EUV radiation. The organotin trialkoxide compositions may be formed as radiation-patternable coatings on substrates.
专利号:US-6051704-A 优先权日:1996-07-22 标题:Synthesis of macrocyclic tetraamido-N ligands 发明人:GORDON-WYLIE SCOTT W; COLLINS TERRENCE J 权利人:UNIV CARNEGIE MELLON 摘要:New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an α or β amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the α or β amino carboxylic acid, the malonate, and the aryl diamine may all be selectively varied so that the resulting tetraamido macrocycle can be tailored to specific desired end uses. The macrocyclic tetraamide ligand may then be complexed with a metal, such as a transition metal, and preferably the middle and later transition metals, to form a robust chelate complex suitable for catalyzing oxidation reactions.
参考标题:Process For The Synthesis Of Aminobiphenylene 摘要:The Present Invention Relates To A Process For The Synthesis Of 2-Aminobiphenylene And Derivatives Thereof By Reacting A Benzene Diazonium Salt With An Aniline Compound Under Basic Reaction Conditions.
合成参考文献
摘要:Pajkert, R.; Röschenthaler, G.-V., Science of Synthesis Knowledge Updates, (2022) 1, 402. 摘要:Pajkert, R.; Röschenthaler, G.-V., Science of Synthesis Knowledge Updates, (2022) 1, 397. 摘要:Wu, S.; Song, H.; Hu, M., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 2.