Polycyclic gamma-pyrone-3-carboxaldehyde derivatives
    94.
    发明授权
    Polycyclic gamma-pyrone-3-carboxaldehyde derivatives 失效
    多环γ-吡喃酮-3-甲醛衍生物

    公开(公告)号:US3959480A

    公开(公告)日:1976-05-25

    申请号:US546587

    申请日:1975-02-03

    IPC分类号: C07D311/92 C07F5/02 A61K31/35

    CPC分类号: C07F5/022 C07D311/92

    摘要: Novel polycyclic gamma-pyrone derivatives having a carboxaldehyde group on the 3-position and optionally substituted on the 5, 6, 7, 8, 9 or 10 positions with a hydroxy, lower alkyl or lower alkoxy group are disclosed, as well as the corresponding N-substituted, formyl imine derivatives thereof. These compounds, and pharmaceutical compositions containing these compounds, are useful for the treatment of allergic conditions and for the treatment of hyperacidity.

    摘要翻译: 公开了具有羟基,低级烷基或低级烷氧基的3-位上具有羧醛基并任选在5,6,7,8,9或10位上被取代的新型多环γ-吡喃酮衍生物,以及相应的 N-取代的甲酰基亚胺衍生物。 这些化合物和含有这些化合物的药物组合物可用于治疗过敏性疾病和治疗胃酸过多。

    Protonated indole phthalides and naphthalides
    95.
    发明授权
    Protonated indole phthalides and naphthalides 失效
    质子化吲哚酞和萘

    公开(公告)号:US3954799A

    公开(公告)日:1976-05-04

    申请号:US393798

    申请日:1973-09-04

    申请人: Alan L. Borror

    发明人: Alan L. Borror

    摘要: This invention relates to protonated compounds of the formula: ##SPC1##Wherein A is a radical selected from ##SPC2##X represents the atoms necessary to complete a ring-closing moiety selected from phthalide and naphthalide; and Z is an anion derived from a protic acid. These compounds are useful as intermediates in the preparation of phthalide and naphthalide indicator dyes.

    摘要翻译: 本发明涉及下式的质子化化合物:

    Polycyclic dioxaborin complexes
    96.
    发明授权
    Polycyclic dioxaborin complexes 失效
    多环二氧杂环硼配合物

    公开(公告)号:US3936488A

    公开(公告)日:1976-02-03

    申请号:US515765

    申请日:1974-10-17

    申请人: Daniel Kaminsky

    发明人: Daniel Kaminsky

    IPC分类号: C07D311/92 C07F5/02 C07F5/04

    CPC分类号: C07D311/92 C07F5/022

    摘要: A process for the production of partially saturated gamma-pyrones of the general formula I: ##SPC1##wherein R represents hydrogen, hydroxy, lower alkyl, or lower alkoxy and n represents 1 or 2, by reacting a suitably substituted tetralone (IIa) or indanone (IIb) with a boron trifluoride compound and acetic anhydride to obtain intermediate boron complexes III, which are reacted with a Vilsmeier reagent prepared from phosphorus oxychloride and dimethylformamide to obtain the partially saturated gamma-pyrones of formula I. The gamma-pyrones I have anti-allergy and anti-secretory activity.

    摘要翻译: 制备通式I的部分饱和γ-吡喃酮的方法:

    Process for preparing phthalide and naphthalide indicator dyes
    97.
    发明授权
    Process for preparing phthalide and naphthalide indicator dyes 失效
    制备苯酞和萘指示剂染料的方法

    公开(公告)号:US3931228A

    公开(公告)日:1976-01-06

    申请号:US446716

    申请日:1974-02-28

    申请人: Alan L. Borror

    发明人: Alan L. Borror

    摘要: This invention relates to a process of preparing phthalein indicator dyes including phthalides and naphthalides derived from certain hydroxy-substituted carbocyclic aryl compounds, such as phenols, and from certain N-heterocyclic aryl compounds, such as indoles, and to a process of preparing novel intermediates useful therein. According to the present invention, the selected carbocyclic compound or the selected N-heterocyclic compound is reacted with phthalaldehydic or naphthalaldehydic acid to form the corresponding (na)phthalidyl adduct which is treated with an oxidizing agent to yield the subject intermediates. To prepare the indicator dye, the intermediate, i.e., the oxidation product thus obtained is then reacted with a carbocyclic or heterocyclic aryl compound to yield the corresponding indicator dye. The oxidation products comprising the novel intermediates of the present invention may be dehydro or hydrated (na)phthalidyl adducts.

    摘要翻译: 本发明涉及一种制备酞菁指示剂染料的方法,所述染料包括衍生自某些羟基取代的碳环芳基化合物如酚类的苯酞和萘衍生物,以及某些N-杂环芳基化合物如吲哚,以及制备新型中间体的方法 在其中有用。 根据本发明,选择的碳环化合物或所选择的N-杂环化合物与邻苯二甲醛或萘醛酸反应形成相应的(na)酞基加合物,其用氧化剂处理以产生主题中间体。 为了制备指示剂染料,中间体即所得氧化产物然后与碳环或杂环芳基化合物反应,得到相应的指示剂染料。 包含本发明新型中间体的氧化产物可以是脱水或水合(na)的苯酞基加合物。

    Process for production of isochromans

    公开(公告)号:US3910964A

    公开(公告)日:1975-10-07

    申请号:US46606874

    申请日:1974-05-01

    摘要: Process for producing isochromans having the structure:

    WHEREIN R1 and R2 are each (i) separately selected from the group consisting of hydrogen, lower alkoxyl, lower alkyl, and, (ii) taken together, selected from the group consisting of benzo, cyclopentano, cyclohexano, naphtho, monoalkyl cyclopentano, polyalkyl cyclopentano, monoalkyl cyclohexano and polyalkyl cyclohexano, and R3 and R4 are the same or different and are selected from the group consisting of hydrogen and lower alkyl comprising the steps of intimately admixing: A. An alkanol having the structure:

    B. An acetal having the structure:

    (wherein R5 and R6 are the same or different alkyl); and C. A protonic acid selected from the group consisting of ptoluene sulfonic acid and phosphoric acid. AND HEATING THE RESULTING MIXTURE FOR A PERIOD OF TIME WHEREBY A SUBSTANTIAL AMOUNT OF THE ISOCHROMAN HAVING THE ABOVE STRUCTURE IS FORMED.

    Steroidal intermediates
    99.
    发明授权
    Steroidal intermediates 失效
    类固醇中间体

    公开(公告)号:US3892779A

    公开(公告)日:1975-07-01

    申请号:US45069274

    申请日:1974-03-13

    申请人: HOFFMANN LA ROCHE

    发明人: SAUCY GABRIEL

    摘要: Stereo-specific total synthesis of steroidal materials. 7Substituted 3-oxo-1-heptenes or variants thereof are reacted with 2-alkylcycloalkane-1,3-diones yielding 3-substituted 6a Beta alkyl-cyclopenta (f) (l) benzopyrans or naphtho (2,1-b) pyrans. These are then subjected to a selective catalytic hydrogenation followed by an introduction of a hydroxy, alkoxy or acyloxy group at the 4a-position to produce a 3-substituted 6a, Beta , 4ahydroxy, alkoxy or acyloxy perhydrocyclopenta (f) (1) benzopyran or perhydro-naphtho (2,1-b) pyran. These latter compounds are then converted into 4- or 5-(3-oxoalkyl)perhydroindene-5-ones or perhydronaphthalene-6-ones which in turn can be converted to known steroidal materials by known methods.

    摘要翻译: 立体声特异性全合成甾体材料。 7-取代的3-氧代-1-庚烯或其变体与2-烷基环烷-1,3-二酮反应,得到3-取代的6aβ-烷基 - 环戊二烯并[f] [1]苯并吡喃或萘并[2,1-b ] pyrans。 然后将它们进行选择性催化氢化,然后在4a位引入羟基,烷氧基或酰氧基以产生3-取代的6a,β,4a-羟基,烷氧基或酰氧基全氢环戊二烯并[f] [1] 苯并吡喃或全氢 - 萘并[2,1-b]吡喃。 然后将这些后一种化合物转化为4-或5-(3-氧代烷基)全氢茚-5-酮或全氢萘-6-酮,其又可以通过已知方法转化为已知的甾族化合物。