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    • 4. 发明授权
    • 2-Oxoazetidines, methods for their preparation, and their use
    • 2-氧杂氮杂,其制备方法及其用途
    • US4855421A
    • 1989-08-08
    • US180200
    • 1988-04-20
    • Hans FliriChing Pong Mak
    • Hans FliriChing Pong Mak
    • C07D205/08C07D205/09C07D499/00C07F7/18
    • C07D205/08C07D205/09C07D499/00C07F7/186Y02P20/55
    • The invention relates to new 2-oxoazetidines having the formulas ##STR1## where R.sub.1 stands for a lower fluoroalkyl or an optionally protected lower hydroxyalkyl group; R.sub.2 for chlorine, bromine, iodine, fluorine, an ##STR2## group in which n is 0, 1 or 2 and R.sub.5 is a lower alkyl, lower alkenyl, an optionally substituted benzyl group, optionally substituted phenyl group, a --CH.sub.2 COX group in which X means a lower alkyl, lower alkoxy or the amino group, or a ##STR3## group in which Y and Z are the same or different and in each case stand for oxygen, nitrogen or sulphur and R.sub.6 stands for a lower alkyl, lower alkoxy, lower alkylthio, lower dialkylamino, an aryl, aryloxy or arylthio group, or for a group having the formula ##STR4## where W stands for --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or C.sub.6 H.sub.4 ; R.sub.3 stands for bromine, chlorine, iodine, SeC.sub.6 H.sub.5 or SC.sub.6 H.sub.5 ; and R.sub.4 stands for hydrogen, a group having the formula ##STR5## in which R.sub.7 is a lower alkyl, an optionally substituted benzyl or an optionally substituted benzohydryl group; or they represent a protecting group, with the proviso that in compounds of formula Ia R.sub.2 does not stand for SCH.sub.3 when R.sub.1 means hydroxyethyl, R.sub.3 means bromine and R.sub.4 means the group of formula IIa, as well as to methods for their preparation and to their use.
    • 本发明涉及具有式“IMAGE”的新的2-氧代氮杂环丁烷,其中R1代表低级氟烷基或任意保护的低级羟烷基; R2为氯,溴,碘,氟,其中n为0,1或2,R5为低级烷基,低级烯基,任选取代的苄基,任选取代的苯基,-CH 2 COX基团 其中X表示低级烷基,低级烷氧基或氨基,或其中Y和Z相同或不同且在各种情况下代表氧,氮或硫的基团,R 6代表低级烷基,低级烷基 烷氧基,低级烷硫基,低级二烷基氨基,芳基,芳氧基或芳硫基,或具有式II的基团,其中W代表-CH 2 CH 2 - , - CH = CH-或C 6 H 4; R3代表溴,氯,碘,SeC6H5或SC6H5; R4代表氢,具有式IIa的基团,其中R7是低级烷基,任意取代的苄基或任意取代的苯甲酰基; 或者它们表示保护基团,条件是当R 1表示羟乙基时,式Ia 2化合物不代表SCH 3,R 3表示溴,R 4表示式IIa基团,以及其制备方法及其制备方法 使用。