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    • 8. 发明公开
    • PROCESS FOR THE MANUFACTURE OF BRIDGED MONOBACTAM INTERMEDIATES
    • 制造桥联中间体的方法
    • EP2197881A1
    • 2010-06-23
    • EP08804217.1
    • 2008-09-15
    • Basilea Pharmaceutica AG
    • MULLER, MarcWU, XiaopingXU, Lin
    • C07D487/04C07C237/20
    • C07C271/54C07C271/22C07D487/04
    • A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0°C or less in a liquid aprotic solvent for a time period sufficient to obtain the compound of formula (I).
    • 制备具有顺式构象并且其中R 1代表1-苯基-C 1 -C 4烷基或1-萘基-C 1 -C 4烷基的式(I)化合物的方法,其中R 1的苯基或萘基部分未被取代或被取代 与一个或多个C1-C4烷氧基和R1的烷基部分的2-,3-和/或4-位上的碳原子独立地为R1的苯基或萘基部分且彼此独立地为未取代的或 被C 1 -C 4烷氧基和/或甲硅烷氧基取代,或者优选未取代或每个碳原子被一个C 1 -C 4烷氧基和/或甲硅烷氧基取代,并且R 2代表C 1 -C 6烷基或未取代或取代的苄基,其中 处理其中R3表示C1-C6烷基或未取代或取代的苄基,且R1和R2具有与式(I)中相同的含义的式(II)化合物; 在0℃或更低的温度下,在液体非质子传递溶剂中用碱处理足以获得式(I)化合物的时间。