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-2006178357-A1 优先权日:2005-02-10 标题 :Chphalosporin-derived mercaptans as inhibitors of serine and metallo-beta-lactamases 发明人:BUYNAK JOHN D; CHEN HANSONG 权利人:BUYNAK JOHN D; CHEN HANSONG 摘要:Compounds of formula I: See Formula I in Figures Section n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting simultaneously serine and metallo-β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
专利号:US-7125986-B2 优先权日:1997-12-29 标题:Penicillanic acid derivative compounds and methods of making 发明人:BUYNAK JOHN D; RAO AKIREDDY SRINIVASA; DOPPALAPUDI VENKATA RAMANA 权利人:UNIV SOUTHERN METHODIST 摘要:Compounds of formula I: n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
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.
专利号:RU-1589598-C 优先权日:1987-12-01 标题 :4-hydroxy-2,6-dihydroxyiminocyclohexanone as a parent product for synthesis of 4-hydroxybenzofurazan, and a method of 4-hydroxybenzofurazan synthesis
摘要:Toxicometric Parameters of Industrial Toxic Chemicals Under Single Exposure, Izmerov, N.F., et al., Moscow, Centre of International Projects, GKNT, 1982, -(79), 1982