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    • 6. 发明授权
    • Process for the preparation of quinolonecarboxylic acid esters
    • 制备喹喔啉羧酸酯的方法
    • US5095112A
    • 1992-03-10
    • US121502
    • 1987-11-17
    • Michael Preiss
    • Michael Preiss
    • A61K31/47A61P31/04C07D215/56C07D455/04C07D471/04C07D471/06C07D498/04C07D498/06
    • C07D215/56C07D455/04C07D471/04C07D471/06
    • A process for the preparation of quinolone-carboxylic acid esters of the formulae I and II ##STR1## in which A represents nitrogen or .dbd.C--R.sup.4,R.sup.4 represents hydrogen, fluorine, chlorine, nitro or methyl,B represents halogen, nitro, alkoxy, alkylsulphonyloxy or the radical ##STR2## and B additionally represents ##STR3## if R1 does not denote cyclopropyl, and R.sup.5 represents a branched or unbranched alkyl group which has 1 to 4 carbon atoms and which can optionally be substituted by a hydroxyl or methoxy group,R.sup.6 represents hydrogen, methyl or phenyl,R.sup.7 represents hydrogen or methyl,R.sup.8 represents dialkylamino having 1 or 2 carbon atoms in the alkyl group or dialkylaminomethyl having 1 or 2 carbon atoms in the alkyl group, or aminomethylR.sup.1 represents hydrogen, optionally substituted alkyl having 1 to 3 carbon atoms, optionally substituted cycloalkyl, 2-fluoroethyl, vinyl, methoxy or 4-fluorophenyl,R.sup.2 represents optionally substituted alkyl having 1 to 6 carbon atoms and also cyclohexyl and benzyl,R.sup.3 represents hydrogen, methyl or ethyl, andZ represents oxygen, nitrogen which is substituted by methyl or phenyl, and .dbd.CH.sub.2,characterized in that quinolonecarboxylic acids of the formulae III and IV ##STR4## in which A, B, Z, R.sup.1 and R.sup.3 have the meanings indicated above, are reacted with chloroformic acid esters of the formula VCl--COOR.sup.2 (V)in which R.sup.2 has the meaning indicated above.
    • 一种制备式I和II的喹诺酮 - 羧酸酯的方法,其中A表示氮或= C-R 4,R 4表示氢,氟,氯,硝基或 甲基,B表示卤素,硝基,烷氧基,烷基磺酰氧基或基团,且如果R1不表示环丙基,则B另外表示“IMAGE”,R 5表示具有1至4个碳原子的支链或非支链烷基, 任选被羟基或甲氧基取代,R 6表示氢,甲基或苯基,R 7表示氢或甲基,R 8表示烷基中具有1或2个碳原子的二烷基氨基或烷基中具有1或2个碳原子的二烷基氨基甲基, 或氨基甲基R 1表示氢,任选取代的具有1至3个碳原子的烷基,任选取代的环烷基,2-氟乙基,乙烯基,甲氧基或4-氟苯基,R 2表示任选取代的具有1至6个碳原子的烷基和 因此环己基和苄基,R 3表示氢,甲基或乙基,Z表示氧,被甲基或苯基取代的氮和= CH 2,其特征在于式III和IV的喹诺酮羧酸(图III) 其中A,B,Z,R 1和R 3具有上述含义的式(Ⅳ)与式ⅤCl-COOR2(Ⅴ)的氯甲酸酯反应,其中R2具有上述含义。
    • 9. 发明授权
    • Dioxopiperazine derivatives suitable for use as medicaments and
.beta.-lactam antibiotic intermediates
    • 适用于药物和β-内酰胺抗生素中间体的二氧代哌嗪衍生物
    • US4182762A
    • 1980-01-08
    • US861473
    • 1977-12-16
    • Michael Preiss
    • Michael Preiss
    • C07D241/08C07D405/12C07D499/00C07D499/68C07D241/02C07D405/02C07D409/02
    • C07D499/00C07D241/08
    • New dioxo-piperazine derivatives suitable for use as medicaments and .beta.-lactam antibiotic intermediates of the formula ##STR1## in which Z is ##STR2## and, R.sup.1 and R.sup.2 each independently is hydrogen or various optionally substituted aliphatic, aromatic or heterocyclic radicals or together form an optionally substituted ring,are formed by reacting(a) 1-amino-2,3-dioxo-piperazine of the formula ##STR3## with a compound of the formula ##STR4## or a hydrate, acetal, ketal, sulphite, hydrogen halide or hydrocyanic acid addition product thereof or, ##STR5## with an oxalic acid ester in the presence of a diluent, thereby to effect cyclization. The new derivatives are anti-virally active and can also be chlorocarbonated with phosgene to form a reactive derivative which can be condensed with the amino group of .alpha.-amino penicillins to form antibiotics.
    • 适合用作药物的新二氧代哌嗪衍生物和其中Z为的式“IMAGE”的β-内酰胺抗生素中间体,R1和R2各自独立地为氢或各种任选取代的脂族,芳族或杂环基或一起 形成任选取代的环,通过使(a)式(Ⅰa)的1-氨基-2,3-二氧代 - 哌嗪与下式化合物或水合物,缩醛,缩酮,亚硫酸盐,氢气 卤化物或氢氰酸加成产物,或b)与草酸酯在稀释剂存在下进行环化反应。 新衍生物具有抗病毒活性,也可用光气进行氯碳化,形成可与α-氨基青霉素氨基缩合形成抗生素的活性衍生物。