专利号:US-2023339906-A1 优先权日:2020-09-26 标 题 :A process for the synthesis of anthranilic acid/amide compounds and intermediates thereof 发明人:SYTHANA SURESH KUMAR; NAGLE PRAMOD; KUMAR VIJAY KUMAR; KANAWADE SHRIKANT BHAUSAHEB; CHANDRE TUKARAM NIVRUTTI; THUBE VINAYAK KISAN; PATIL PRADEEP PRAKASH; SHUKLA SHALINI; SHENDE KANTILAL BALU; PATRA PRANAB KUMAR; KLAUSENER ALEXANDER G M 权利人:PI INDUSTRIES LTD; PI INDUSTRIES LTD 摘要:The present invention discloses a process for the synthesis of compound of formula (VII) or a salt thereof,wherein, R, R1, R2, R3, R4a and R4b are as defined in the detailed description. The process further comprises the synthesis of an anthranilic diamide compound of formula (I).
专利号:US-7452994-B2 优先权日:2001-09-12 标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 发明人:MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN 权利人:ANORMED INC 摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.
专利号:US-11649213-B2 优先权日:2018-09-26 标题 :Synthetic method for the preparation of a 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol compound 发明人:MEISENBACH MARK; MARTIN BENJAMIN; RONDE NIEK JOHANNES; RUIZ CARMEN 权利人:MEREO BIOPHARMA 1 LTD 摘要:Provided is a process for preparing a compound, comprising the steps of a) Reacting a compound of Formula A (Formula A) with the compound 3 (3) to provide the compound 5 (5) or a salt or solvate thereof, wherein R is a linear or branched C1-C5 alkyl. Further provided is the compound 5 or a salt or solvate thereof. (5) The use of these compounds in the synthesis of 3-[5-Amino-4-(3-Cyanobenzoyl)-Pyrazol-1-yl]-N-Cyclopropyl-4-Methylbenzamide is also provided.
专利号:US-4304934-A 优先权日:1980-12-30 标题 :Synthesis of amino hydroxy cyclopentenones 发明人:BARTELS-KEITH JAMES R; KARGER EVA R; ROGERS JEAN B 权利人:POLAROID CORP 摘要:This invention relates to a method of synthesizing 3-amino-2-hydroxy-2-cyclopentenones possessing an aliphatic substituent in the 4-position which comprises reacting cyanoacetamide with an aliphatic aldehyde to yield the corresponding β-substituted-α,α'-dicyanoglutaramide, hydrolyzing the amide to the corresponding β-substituted glutaric acid, esterifying the acid to the corresponding dialkyl diester, converting the diester to a 1,2-bis(trimethylsiloxy)-4-substituted cyclopentene by reductive cyclization using chlorotrimethylsilane in the presence of sodium, hydrolyzing and oxidizing the bis(trimethylsiloxy) compound to the 2-hydroxy-4-substituted-2-cyclopentenone in the presence of a cupric salt, nitrosating the 2-cyclopentenone to the 2-hydroxy-4-substituted-5-oximino-2-cyclopentenone, converting the oxime to the 2-acetoxy-3-amino-4-substituted-2-cyclopentenone by reductive acetylation and removing the acetyl group by alkanolysis to yield the 3-amino-2-hydroxy-4-substituted-2-cyclopentenone product.
专利号:US-3697597-A 优先权日:1968-09-21 标 题:Process for the preparation of alpha-oximinoalkyl ketones 发明人:DORLARS ALFONS 权利人:BAYER AG 摘要:Alpha -Oximino ketones, for example, oximinodipropyl ketone, are prepared by reacting a ketone in an inert organic solvent immiscible with water in the presence of a hydrogen halide with an amount of alkyl nitrite that is insufficient for complete nitrosation followed by extracting the ketone formed with an aqueous alkali solution, removing the alkaline extract formed and isolating the Alpha -oximino ketone. The ketones formed are useful as intermediates in the synthesis of pharmaceutical compounds, dyes, analytical reagents, plant protection agents, and optical brighteners.
专利号:US-9181203-B2 优先权日:2010-11-12 标题:Substituted pyrazino[2,3-d]isooxazoles as intermediates for the synthesis of substituted pyrazinecarbonitriles and substituted pyrazinecarboxamides 发明人:NAKAMURA KOUKI; MURAKAMI TAKESHI; NAITOU HIROYUKI; HANAKI NAOYUKI; WATANABE KATSUYUKI 权利人:FUJIFILM CORP; TOYAMA CHEMICAL CO LTD 摘要:The object of the present invention is to provide a compound which is useful as a production intermediate of pyrazine carboxamide derivative such as 6-fluoro-3-hydroxy-2-pyrazine carboxamide. The present invention provides a pyrazino[2,3-d]isoxazole derivative represented by the formula (I): n nwherein X represents a halogen atom, a hydroxyl group or a sulfamoyloxy group, and Y represents —C(â•?O)R or —CN; wherein R represents a hydrogen atom, an alkoxy group an aryloxy group, an alkyl group, an aryl group or an amino group.
摘要:Zimmer, R.; Trawny, D., Science of Synthesis Knowledge Updates, (2013) 4, 170. 摘要:Bronstein, A.C., P.L. Currance; Emergency Care for Hazardous Materials Exposure. 2nd ed. St. Louis, MO. Mosby Lifeline. 1994., p. 252 摘要:Association of American Railroads. Emergency Handling of Hazardous Materials in Surface Transportation. Washington, DC: Association of American Railroads, Bureau of Explosives, 1994., p. 455 摘要:Franke C et al; Chemosphere 29: 1501-14 (1994) 摘要:CHILCOTE RR ET AL; PEDIATRICS 59 (2): 280-2 (1977)