New n-cyclopropylmethyl azetidine compounds and process for their production
    2.
    发明授权
    New n-cyclopropylmethyl azetidine compounds and process for their production 失效
    新的N-环丙基甲基吗啉化合物及其生产方法

    公开(公告)号:US3817985A

    公开(公告)日:1974-06-18

    申请号:US29618172

    申请日:1972-10-10

    申请人: PARKE DAVIS & CO

    发明人: LOCKHART I

    IPC分类号: C07D205/04 C07D25/00

    CPC分类号: C07D205/04

    摘要: m-(1-(Cyclopropylmethyl)-3-isopentyl-3-azetidinyl)-phenol, and its acid-addition salts and phenolate salts. The compounds have pharmacological activity and exhibit a selective pattern of analgesic action. They can be produced by reducing the carbonyl group of m-(1-(cyclopropylcarbonyl)-3-isopentyl-3azetidinyl)phenol. The starting material can be obtained by a sequence of steps beginning with the reaction of diethyl carbonate, m-methoxyphenylacetonitrile, sodium ethoxide, and 1bromo-3-methylbutane, followed by operations to form the azetidine ring and introduce the N-cyclopropylcarbonyl group.

    摘要翻译: 间 - [1-(环丙基甲基)-3-异戊基-3-氮杂环丁基] - 苯酚及其酸加成盐和酚盐。 这些化合物具有药理活性并表现出选择性的止痛作用。 它们可以通过还原m- [1-(环丙基羰基)-3-异戊基-3-氮杂环丁烷基]苯酚的羰基来制备。 原料可以通过从碳酸二乙酯,间甲氧基苯基乙腈,乙醇钠和1-溴-3-甲基丁烷的反应开始的步骤顺序获得,然后进行氮杂环丁烷环的形成和引入N-环丙基羰基 。

    3-azetidinols
    4.
    发明授权
    3-azetidinols 失效
    3-AZETIDINOLS

    公开(公告)号:US3668196A

    公开(公告)日:1972-06-06

    申请号:US3668196D

    申请日:1969-01-13

    申请人: LILLY CO ELI

    IPC分类号: C07D205/06 C07D25/00

    CPC分类号: C07D205/06

    摘要: 2,2-Disubstituted-azetidines, optionally substituted in addition at the 1,3, and 4 positions, useful as CNS stimulants and as blood pressure-lowering agents.

    摘要翻译: 2,2-二取代 - 氮杂环丁烷,在1,3和4位任选被另外取代,可用作CNS兴奋剂和降血压剂。

    Certain disulfide derivatives of 2-azetidinones
    5.
    发明授权
    Certain disulfide derivatives of 2-azetidinones 失效
    2-AZETIDINONES的某些衍生物衍生物

    公开(公告)号:US3872086A

    公开(公告)日:1975-03-18

    申请号:US16784871

    申请日:1971-07-30

    申请人: GLAXO LAB LTD

    CPC分类号: C07D205/095

    摘要: Compounds of the general formula

    (WHEREIN R1 is an amino group or a blocked amino group; and R2 is an aliphatic, araliphatic or aromatic group while R3 is the residue of a thiophilic sulphur nucleophile or is a group of formula

    OR R2 is a hydrogen atom while R3 is the residue of a thiophilic sulphur nucleophile or may, when R1 is a phenylacetamido or phenoxyacetamido group, be a group of formula II in which R2 is hydrogen) are provided. The new compounds are useful as intermediates in the production of cephalosporins, penicillins and related Beta -lactam antibiotic compounds. The new compounds may be obtained from penicillin 1-oxides by cleavage of the 1,2sulphur-carbon bond thereof and attachment of the group -SR3 to the sulphur atom in one or more stages.

    摘要翻译: 通式(WHEREIN R1是氨基或封端氨基; R 2是脂族,芳脂族或芳族基团)的化合物,而R 3是亲硫性硫亲核试剂的残基,或者是式OR的基团,其中R2是氢原子 而R3是亲硫性亲核试剂的残基,或者当R1是苯乙酰氨基或苯氧基乙酰胺基时,可以是其中R 2是氢的式II基团)。 新化合物可用作生产头孢菌素,青霉素和相关的β-内酰胺抗生素化合物的中间体。 新化合物可以通过其1,2-硫 - 碳键的切割和基团-SR3在一个或多个阶段中与硫原子的连接而从青霉素1-氧化物获得。