B-lactam-like chaperone inhibitors
    11.
    发明授权
    B-lactam-like chaperone inhibitors 有权
    β-内酰胺样分子伴侣抑制剂

    公开(公告)号:US06495539B1

    公开(公告)日:2002-12-17

    申请号:US09252792

    申请日:1999-02-19

    IPC分类号: C07D50100

    CPC分类号: C07D499/00 C07D277/12

    摘要: Compounds of the formula and the salts, esters and amides thereof wherein Z is S, SO, SO2 or O; each of R1, R2 and R3 is independently H or substituted or unsubstituted alkyl (1-10C), substituted or unsubstituted alkenyl, substituted or unsubstituted acyl (2-11C), substituted or unsubstituted aryl (6-14C), substituted or unsubstituted arylcarbonyl (7-15C), substituted or unsubstituted arylalkyl (7-15C), substituted or unsubstituted pyridyl wherein substituents on any alkyl, alkenyl, or acyl moiety are selected from the group consisting of halo, and RO, wherein R is H or alkyl (1-6C), and substituents on any aryl or pyridyl moiety are selected from the group consisting of halo, and RO, where R is H or alkyl (1-6C), —CN and —CF3; with the proviso that R1 is not H and R1 and R3 are not identical and with the proviso that in formula (1), the B ring may contain one double bond that is located between positions 2 and 3, and in formula (2), the B ring may contain one double bond that can be located between positions 2 and 3 or positions 3 and 4 are useful as antibacterial agents.

    摘要翻译: 式中的化合物及其盐,酯和酰胺,其中Z为S,SO,SO 2或O; R 1,R 2和R 3各自独立地为H或取代或未取代的烷基(1-10C),取代或未取代的烯基,取代或未取代的酰基 (2-11C),取代或未取代的芳基(6-14C),取代或未取代的芳基羰基(7-15C),取代或未取代的芳基烷基(7-15C),取代或未取代的吡啶基,其中任何烷基,链烯基或酰基 部分选自卤素和RO,其中R是H或烷基(1-6C),任何芳基或吡啶基部分上的取代基选自卤素和RO,其中R是H或 烷基(1-6C),-CN和-CF3; 条件是R1不是H,R1和R3不相同,条件是在式(1)中,B环可以含有位于2和3之间的一个双键,而在式(2)中, B环可以含有一个可以位于2和3位之间的双键,或3或4位可用作抗菌剂。

    CATALYST
    17.
    发明申请
    CATALYST 审中-公开
    催化剂

    公开(公告)号:US20120321533A1

    公开(公告)日:2012-12-20

    申请号:US13439232

    申请日:2012-04-04

    IPC分类号: B01J31/04 B01J19/00 B01J31/08

    摘要: The present invention relates to a method of producing a heterogeneous catalyst suitable for catalyzing Heck, Suzuki-Miyaura Sonogashira coupling and Buchwald-Hartwig reactions, comprising the steps of: a) providing a macroporous carrier, said macroporous carrier consisting of a core and a plurality of ion exchange groups covalently bonded to the surface of said core, where at least 90% of the ions bound to said carrier are formate ions; b) swelling said carrier in a polar solvent; c) providing a palladium (II) salt; d) suspending said carrier in an organic solvent thereby obtaining a suspension; e) adding said palladium salt to said suspension and allowing the resulting mixture to react at a temperature within the range of 0-70° C. until said carrier has turned black; f) washing said carrier in water; g) drying said carrier under vacuum.

    摘要翻译: 本发明涉及适用于催化Heck,Suzuki-Miyaura Sonogashira偶联剂和Buchwald-Hartwig反应的多相催化剂的制备方法,包括以下步骤:a)提供大孔载体,所述大孔载体由核和多个 共价结合到所述芯的表面上的离子交换基团,其中与所述载体结合的至少90%的离子是甲酸根离子; b)在极性溶剂中溶胀载体; c)提供钯(II)盐; d)将所述载体悬浮在有机溶剂中,从而获得悬浮液; e)将所述钯盐加入到所述悬浮液中,并使得到的混合物在0-70℃的温度下反应,直到所述载体变黑; f)在水中清洗载体; g)在真空下干燥所述载体。