COMPOUNDS USEFUL FOR PRODUCING AN OPTICALLY ACTIVE DIAZABICYCLOOCTANE COMPOUND
    5.
    发明申请
    COMPOUNDS USEFUL FOR PRODUCING AN OPTICALLY ACTIVE DIAZABICYCLOOCTANE COMPOUND 有权
    用于生产光学活性二氮杂环戊烷化合物的化合物

    公开(公告)号:US20160137645A1

    公开(公告)日:2016-05-19

    申请号:US15007906

    申请日:2016-01-27

    IPC分类号: C07D471/08

    摘要: An optically active (2S,5R)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxylic acid compound defined by the following formula (F): wherein R1 represents CO2R, CO2M, or CONH2, wherein R represents an allyl group or a benzyl group, and M represents a hydrogen atom, an inorganic cation, or an organic cation; and R2 represents a benzyl group or an allyl group.

    摘要翻译: 由下式(F)定义的光学活性(2S,5R)-7-氧代-1,6-二氮杂双环[3.2.1]辛烷-2-羧酸化合物:其中R1表示CO 2 R,CO 2 M或CONH 2,其中 R表示烯丙基或苄基,M表示氢原子,无机阳离子或有机阳离子; 并且R 2表示苄基或烯丙基。

    PROCESS FOR PRODUCING DIAZABICYCLOOCTANE DERIVATIVE AND INTERMEDIATE THEREOF
    6.
    发明申请
    PROCESS FOR PRODUCING DIAZABICYCLOOCTANE DERIVATIVE AND INTERMEDIATE THEREOF 有权
    生产二氮杂环戊烷衍生物及其中间体的方法

    公开(公告)号:US20160264573A1

    公开(公告)日:2016-09-15

    申请号:US15023976

    申请日:2014-09-24

    摘要: A process for producing a diazabicyclooctane derivative represented by Formula (IV) and intermediates thereof by carrying out the following steps: wherein P is an NH protecting group capable of being removed with acid; R1 is 2,5-dioxopyrrolidin-1-yl, 1,3-dioxo-3a,4,7,7a-tetrahydro-1H-isoindol-2(3H)-yl, 1,3-dioxohexahydro-1H-isoindol-2(3H)-yl, or 3,5-dioxo-4-azatricyclo[5.2.1.02.6]dec-8-en-4-yl; R2 is hydrogen, ClCO— or Cl3COCO—; R3 is C1-6 alkyl or heterocyclyl, or forms a 3- to 7-membered heterocyclic ring together with the —O—NH— to which it is attached; and OBn is benzyloxy.

    摘要翻译: 其中P是能够被酸去除的NH保护基; R1是2,5-二氧代吡咯烷-1-基,1,3-二氧代-3a,4,7,7a-四氢-1H-异吲哚-2(3H) - 基,1,3-二氧代六氢-1H-异吲哚-2 (3H) - 基或3,5-二氧代-4-氮杂三环[5.2.1.02.6]癸-8-烯-4-基; R2是氢,ClCO-或Cl3COCO-; R 3是C 1-6烷基或杂环基,或与其连接的-O-NH-一起形成3至7元杂环; 而OBn是苄氧基。

    BETA-LACTAMASE INHIBITOR AND PROCESS FOR PREPARING THE SAME
    7.
    发明申请
    BETA-LACTAMASE INHIBITOR AND PROCESS FOR PREPARING THE SAME 有权
    BETA-LACTAMASE抑制剂及其制备方法

    公开(公告)号:US20160024090A1

    公开(公告)日:2016-01-28

    申请号:US14872988

    申请日:2015-10-01

    摘要: A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I): wherein A represents Ra(Rb)N— or RcO—; B represents NH or NC1-6 alkyl; C represents benzyl, H or SO3M, wherein M represents H, an inorganic or an organic cation; Ra and Rb represent H, C1-6 alkyl or acyl; Rc represents C1-6 alkyl or a heterocyclyl; A is unsubstituted or substituted with 0 to 4 substituents Fn1, wherein Fn1 represents C1-6 alkyl, O═, or Rg-(CH2)0-3—, wherein Rg represents a heterocyclyl, phenyl, heteroaryl, acyl, RdO2S—, Re(Rf)N—, Re(Rf)NCO—, ReO—, ReOCO— or a protective group, wherein Rd represents C1-6 alkyl or MO—; Re and Rf represent H or C1-6 alkyl, and a heterocycle having at least one nitrogen atom may be formed between Ra and Rb, between Rc and B, or between Re and Rf.

    摘要翻译: 由下式(I)表示的β-内酰胺抑制剂的二氮杂双环辛烷化合物:其中A表示Ra(Rb)N-或RcO-; B表示NH或NC1-6烷基; C表示苄基,H或SO 3 M,其中M表示H,无机或有机阳离子; R a和R b表示H,C 1-6烷基或酰基; Rc表示C 1-6烷基或杂环基; A是未取代的或被0至4个取代基Fn1取代,其中Fn1表示C1-6烷基,或为 - (CH2)O3-,其中Rg表示杂环基,苯基,杂芳基,酰基,RdO2S-,Re (Rf)N,Re(Rf)NCO-,ReO-,ReOCO-或保护基,其中Rd表示C1-6烷基或MO-; R f和R f表示H或C 1-6烷基,并且可以在R a和R b之间,R c和B之间,或者在Re和R f之间形成具有至少一个氮原子的杂环。