Process for O-acylating phenol derivatives and acylating compositions
for this purpose
    2.
    发明授权
    Process for O-acylating phenol derivatives and acylating compositions for this purpose 失效
    用于此目的的O-酰化苯酚衍生物和酰化组合物的方法

    公开(公告)号:US4315861A

    公开(公告)日:1982-02-16

    申请号:US246412

    申请日:1981-03-23

    CPC分类号: C07D307/86

    摘要: A process is disclosed for preparing a carbamic acid phenyl ester of the formula (I) ##STR1## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, or aralkyl having 7 to 16 carbon atoms, wherein the aryl, cycloalkyl or aralkyl is unsubstituted or substituted by at least one alkyl group having 1 to 8 carbon atoms;R.sub.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, cyanomethyl, 1,3-dioxolan-2-yl, or carboalkoxyamino wherein the alkoxy group contains 1 to 4 carbon atoms;R.sub.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms; orR.sub.1 and R.sub.2 form together a carbocyclic ring or a heterocyclic ring fused to the phenyl ring wherein the carbocyclic ring of the heterocyclic ring is unsubstituted or substituted by at least one alkyl having 1 to 8 carbon atoms, which comprises acylating a phenol of the formula (II) ##STR2## with a compound of the formula (IV) ##STR3## in the presence of a base. The compounds obtained are valuable intermediates.

    摘要翻译: 公开了制备式(I)的氨基甲酸苯酯的方法,其中R是具有1至8个碳原子的烷基,具有5或6个碳原子的芳基,环烷基或具有7至16个碳原子的芳烷基, 其中芳基,环烷基或芳烷基是未取代的或被至少一个具有1至8个碳原子的烷基取代; R1是氢,具有1至4个碳原子的烷基,具有1至4个碳原子的烷氧基,氰基甲基,1,3-二氧戊环-2-基或烷氧基氨基,其中烷氧基含有1至4个碳原子; R2是氢,卤素,具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基; 或者R 1和R 2一起形成稠合到苯环的碳环或杂环,其中杂环的碳环是未取代的或被至少一个具有1至8个碳原子的烷基取代,其包括酰化式 (II)的化合物与式(IV)的化合物在碱的存在下反应。 所得化合物是有价值的中间体。

    Process for O-acylating phenol derivatives and acylating compositions
for this purpose
    3.
    发明授权
    Process for O-acylating phenol derivatives and acylating compositions for this purpose 失效
    用于此目的的O-酰化苯酚衍生物和酰化组合物的方法

    公开(公告)号:US4323469A

    公开(公告)日:1982-04-06

    申请号:US201508

    申请日:1980-10-28

    IPC分类号: C07D307/86 C09K3/00

    CPC分类号: C07D307/86

    摘要: The invention relates to a process for the preparation of carbamic acid phenyl esters of the formula (I) ##STR1## by acylating phenol derivatives of the formula (II) ##STR2## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, aralkyl having 7 to 16 carbon atoms which groups can be substituted by one or more alkyl groups,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms or acylamino,R.sup.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, or ifR.sup.1 and R.sup.2 represent alkyl and/or alkoxy, they can form together a carbocyclic ring.According to the invention the phenol derivatives of the general formula (II), wherein R.sup.1 and R.sup.2 are as defined above, are reacted with N-carbamoyl-saccharin derivatives of the formula (IV) ##STR3## wherein R has the same meaning as defined above, in the presence of a base.

    摘要翻译: 本发明涉及通过酰化式(II)的苯酚衍生物(II)制备式(I)的氨基甲酸苯酯的方法,其中R是具有1至8个碳原子的烷基 碳原子,芳基,具有5或6个碳原子的环烷基,具有7至16个碳原子的芳基,该基团可以被一个或多个烷基取代,R 1是氢,具有1至4个碳原子的烷基,具有1至4个碳原子的烷氧基 原子或酰氨基,R 2是氢,卤素,具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基,或者如果R 1和R 2表示烷基和/或烷氧基,则它们可以一起形成碳环。 根据本发明,其中R 1和R 2如上定义的通式(II)的酚衍生物与式(Ⅳ)的N-氨基甲酰基 - 糖精衍生物反应其中R具有相同的 意义如上所述,在碱的存在下。

    Combined compositions
    4.
    发明授权
    Combined compositions 失效
    组合成分

    公开(公告)号:US5389662A

    公开(公告)日:1995-02-14

    申请号:US687938

    申请日:1991-05-31

    CPC分类号: A01N53/00

    摘要: The invention relates to novel combined compositions for combatting plant, animal and sanitarian as well as forestry, horticultural and warehouse pests. These compositions contain a pyrethroid-type insecticide as an insecticidally active ingredient and at least one fungicide inhibiting the ergosterol biosynthesis as activity-strengthening agent as well as optionally piperonylbutoxide and other additives.The advantages of the compositions according to the invention consist therein that the activity-strengthening substances used are fungicidal agents widely used and have an advantageous toxicology. The activity-strengthening agent exerts a synergistic effect together with the pyrethroid-type insecticide.The combinations according to the invention bear an outstanding importance in the protection of stored crops.

    摘要翻译: PCT No.PCT / HU90 / 00055 Sec。 371日期1991年5月31日 102(e)日1991年5月31日PCT提交1990年7月30日PCT公布。 出版物WO91 / 01640 日期1991年2月21日。本发明涉及用于对抗植物,动物和卫生以及林业,园艺和仓库害虫的新型组合物。 这些组合物含有拟除虫菊酯型杀虫剂作为杀虫活性成分和至少一种抑制麦角甾醇生物合成作为活性增强剂以及任选的胡椒基丁醚和其它添加剂的杀真菌剂。 根据本发明的组合物的优点在于其中使用的活性增强物质是广泛使用的杀真菌剂并且具有有利的毒理学。 活性增强剂与拟除虫菊酯类杀虫剂一起发挥协同作用。 根据本发明的组合在保存作物方面具有突出的重要性。

    Method of treatment of learning deficiency
    7.
    发明授权
    Method of treatment of learning deficiency 失效
    治疗学习缺陷的方法

    公开(公告)号:US5075338A

    公开(公告)日:1991-12-24

    申请号:US420058

    申请日:1989-10-11

    CPC分类号: A61K31/135

    摘要: A method of treating a learning deficiency is disclosed wherein a patient in need of stimulating learning ability is treated with a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein R.sup.1 is C.sub.1 to C.sub.8 straight or branched chain alkyl, C.sub.7 to C.sub.10 phenylalkyl, phenyl, or C.sub.3 to C.sub.8 cycloalkyl; andR.sup.2 is C.sub.1 to C.sub.8 straight or branched chain alkyl, unsubstituted or substituted by halogen, hydroxy, C.sub.1 to C.sub.4 alkoxy or by 1 or 2 phenyl groups; or is C.sub.3 to C.sub.8 cycloalkyl;with the proviso that R.sup.1 and R.sup.2 together contain at least 3 carbon atoms; or a pharmaceutically acceptable salt thereof.

    摘要翻译: 公开了一种治疗学习缺陷的方法,其中需要刺激学习能力的患者用治疗有效量的式(I)化合物(I)治疗,其中R1为C1至C8直链或支链 烷基,C7至C10苯基烷基,苯基或C3至C8环烷基; R2为C1至C8直链或支链烷基,未取代或被卤素,羟基,C1至C4烷氧基取代或被1或2个苯基取代; 或为C3至C8环烷基; 条件是R1和R2一起含有至少3个碳原子; 或其药学上可接受的盐。

    Psychostimulant agent
    9.
    发明授权
    Psychostimulant agent 失效
    精神刺激剂

    公开(公告)号:US5220068A

    公开(公告)日:1993-06-15

    申请号:US649239

    申请日:1991-01-29

    IPC分类号: A61K31/135

    CPC分类号: A61K31/135

    摘要: The present invention relates to a pharmaceutical composition comprising as active ingredient a compound of the Formula I ##STR1## wherein R.sup.1 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; phenyl alkyl having 7 to 10 carbon atoms; phenyl; or cycloalkyl comprising 3 to 8 carbon atoms;R.sup.2 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; alkyl comprising 1 to 8 carbon atoms substituted by halogen, hydroxy, alkoxy having 1 to 4 carbon atoms or by one or two phenyl groups; phenyl; or cycloalkyl having 3 to 8 carbon atoms,with the proviso that groups R.sup.1 and R.sup.2 together contain at least three carbon atoms. The invention also relates to a process for the preparation of compounds of the Formula I by methods known per se. The compounds of the Formula I are phychostimulants having a new spectrum of effect which can be used in therapy for increasing psychical activity (learning and retention) and for treating clinical patterns of depression and deficiencies of learning and retention like in Alzheimer's disease, and are void of side effects (e.g. due to catecholamine release) of known stimulants.

    摘要翻译: 本发明涉及包含作为活性成分的式I化合物(I)的药物组合物,其中R1代表包含1至8个碳原子的直链或支链烷基; 具有7至10个碳原子的苯基烷基; 苯基; 或包含3至8个碳原子的环烷基; R2代表包含1至8个碳原子的直链或支链烷基; 被卤素,羟基,具有1至4个碳原子的烷氧基或一个或两个苯基取代的碳原子数为1〜8的烷基; 苯基; 或具有3至8个碳原子的环烷基,条件是基团R 1和R 2一起含有至少3个碳原子。 本发明还涉及通过本身已知的方法制备式I化合物的方法。 式I的化合物是具有新的效应谱的phychostimulants,其可用于增加心理活动(学习和保留)的治疗和用于治疗抑郁症的临床模式和学习和保留的缺陷,如阿尔茨海默病,并且是无效的 的已知兴奋剂的副作用(例如由于儿茶酚胺释放)。