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    Ferrocenyl diphosphines as ligands for homogeneous catalysts
    91.
    发明授权
    Ferrocenyl diphosphines as ligands for homogeneous catalysts 失效
    二茂铁基二膦作为均相催化剂的配体

    公开(公告)号：US5371256A

    公开(公告)日：1994-12-06

    申请号：US037783

    申请日：1993-03-26

    Applicant: Antonio Togni ,  Felix Spindler ,  Nadia Zanetti ,  Amina Tijani

    Inventor： Antonio Togni ,  Felix Spindler ,  Nadia Zanetti ,  Amina Tijani

    IPC: B01J31/22 ,  B01J31/24 ,  C07B35/02 ,  C07B41/02 ,  C07B43/04 ,  C07B53/00 ,  C07B61/00 ,  C07C45/41 ,  C07C45/64 ,  C07C49/245 ,  C07C67/303 ,  C07C67/31 ,  C07C209/52 ,  C07C217/08 ,  C07C231/18 ,  C07C235/16 ,  C07F17/02 ,  C07F19/00

    CPC classification number: C07F17/02 ,  B01J31/2291 ,  B01J31/2295 ,  B01J31/2409 ,  B01J31/2471 ,  C07C209/52 ,  C07C231/18 ,  C07C67/303 ,  C07C67/31 ,  B01J2231/643 ,  B01J2231/645 ,  B01J2531/0205 ,  B01J2531/0286 ,  B01J2531/822 ,  B01J2531/827 ,  B01J2531/842 ,  Y10S526/943

    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.8 alkyl, phenyl or phenyl which is substituted by 1 to 3 C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy groups; R.sub.2 and R.sub.3 are identical and are C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.12 cycloalkyl or C.sub.1 -C.sub.4 alkyl- or C.sub.1 -C.sub.4 alkoxy-substituted C.sub.5 -C.sub.12 cycloalkyl, or phenyl which is substituted by one to three identical or different members selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --SiR.sub.4 R.sub.5 R.sub.6, halogen, --SO.sub.3 M, --CO.sub.2 M, --PO.sub.3 M,--NR.sub.7 R.sub.8 and --[.sup..sym. NR.sub.7 R.sub.8 R.sub.9 ]X.sup..crclbar. ; or R.sub.2 and R.sub.3 are different and are C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.1 -C.sub.4 alkyl- or C.sub.1 -C.sub.4 alkoxy-substituted C.sub.5 -C.sub.12 cycloalkyl, phenyl or phenyl which is substituted by one to three identical or different members selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --SiR.sub.4 R.sub.5 R.sub.6, halogen, --SO.sub.3 M, --CO.sub.2 M, --PO.sub.3 M.sub.2, --NR.sub.7 R.sub.8 and --[.sup..sym.NR.sub.7 R.sub.8 R.sub.9 ]X.sup..crclbar. ; or the group --PR.sub.2 R.sub.3 is a radical of formula II ##STR2## and R.sub.4, R.sub.5 and R.sub.6 are each independently of one another C.sub.1 -C.sub.12 alkyl or phenyl, R.sub.7 and R.sub.8 are H, C.sub.1 -C.sub.2 alkyl, phenyl or R.sub.7 and R.sub.8, taken together, are tetramethylene, pentamethylene or 3-oxa-1,5-pentylene, R.sub.9 is H or C.sub.1 -C.sub.4 alkyl, M is H or an alkali metal, X.sup..crclbar. is the anion of a monobasic acid, and * is a stereogenic carbon atom, in the form of their racemates and diastereoisomers or mixtures of diastereoisomers. Rhodium and iridium complexes with these ligands are suitable for use as homogeneous enantioselective catalysts for the hydrogenation of prochiral compounds containing carbon double bonds or carbon/hetero atom double bonds.

    Abstract translation: 式I的化合物其中R 1是C 1 -C 8烷基，苯基或被1至3个C 1 -C 4烷基或C 1 -C 4烷氧基取代的苯基; R 2和R 3相同，为C 1 -C 12烷基，C 5 -C 12环烷基或C 1 -C 4烷基 - 或C 1 -C 4烷氧基取代的C 5 -C 12环烷基或被一至三个相同或不同的选自C1- C 1-4烷基，C 1 -C 4烷氧基，-SiR 4 R 5 R 6，卤素，-SO 3 M，-CO 2 M，-PO 3 M，-NR 7 R 8和 - [（+）NR 7 R 8 R 9] X（ - ）。 或R 2和R 3不同，为C 1 -C 12烷基，C 5 -C 12环烷基，C 1 -C 4烷基 - 或C 1 -C 4烷氧基取代的C 5 -C 12环烷基，被一至三个相同或不同的成员所取代的苯基或苯基，所述相同或不同的成员选自 C 1 -C 4烷基，C 1 -C 4烷氧基，-SiR 4 R 5 R 6，卤素，-SO 3 M，-CO 2 M，-PO 3 M 2，-NR 7 R 8和 - [（+）NR 7 R 8 R 9] X（ - ）。 或基团-PR 2 R 3是式II的基团（II），且R 4，R 5和R 6彼此独立地为C 1 -C 12烷基或苯基，R 7和R 8为H，C 1 -C 2烷基，苯基或R 7和R 8 一起是四亚甲基，五亚甲基或3-氧杂-1,5-亚戊基，R9是H或C1-C4烷基，M是H或碱金属，X（ - ）是一元酸的阴离子，*是 其外消旋体和非对映异构体形式的立体碳原子或非对映异构体的混合物。 与这些配体的铑和铱配合物适合用作含碳双键或碳/杂原子双键的前手性化合物氢化的均匀对映选择性催化剂。

    Active compounds
    95.
    发明授权
    Active compounds 失效
    活性化合物

    公开(公告)号：US4987138A

    公开(公告)日：1991-01-22

    申请号：US231183

    申请日：1988-08-11

    Applicant: Frederick Cassidy ,  Geoffrey Stemp

    Inventor： Frederick Cassidy ,  Geoffrey Stemp

    IPC: C07C49/245 ,  A61K31/165 ,  A61K31/215 ,  A61K31/22 ,  A61K31/265 ,  A61K31/275 ,  A61K31/35 ,  A61K31/352 ,  A61K31/443 ,  A61K31/445 ,  A61K31/47 ,  A61P1/00 ,  A61P9/00 ,  A61P9/12 ,  A61P11/00 ,  A61P25/02 ,  C07C45/00 ,  C07C49/252 ,  C07C49/255 ,  C07C49/83 ,  C07C49/84 ,  C07C67/00 ,  C07C201/00 ,  C07C239/00 ,  C07C301/00 ,  C07C303/26 ,  C07C303/30 ,  C07C303/36 ,  C07C303/40 ,  C07C309/28 ,  C07C313/00 ,  C07C313/04 ,  C07C313/06 ,  C07C317/24 ,  C07C317/46 ,  C07C323/25 ,  C07D215/20 ,  C07D215/48 ,  C07D311/58 ,  C07D405/04

    CPC classification number: C07D405/04 ,  C07D215/48 ,  C07D311/58

    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl(NOH) or --C(C.sub.1-6 alkyl)NNH.sub.2 or, when Y is oxygen, one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by C.sub.2-7 alkanoyl;one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.2 and R.sub.3 together are C.sub.2-5 polymethylene;R.sub.5 is hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy;R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.7 is NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are independently C.sub.1-6 alkyl, R.sub.8 is hydrogen and R.sub.9 is C.sub.1-6 alkyl or R.sub.8 and R.sub.9 together are C.sub.4-5 polymethylene; or R.sub.6 and R.sub.8 together are --(CH.sub.2).sub.n --wherein n is 2 or 3, and R.sub.9 is hydrogen or C.sub.1-6 alkyl; or R.sub.7 is CH.sub.2 R.sub.10 wherein R.sub.10 is hydrogen or C.sub.1-5 alkyl optionally substituted by halo, hydroxy or C.sub.1-6 alkoxy; or R.sub.6 and R.sub.10 are ---(CH.sub.2).sub.m -- wherein m is 2 or 3;X is oxygen or sulphur; andY is oxygen, CH.sub.2 or NH;the R.sub.6 --CH--CX--R.sub.7 group being trans to the R.sub.5 group; having blood pressure lowering activity, a process for their preparation and their use as pharmaceuticals.

    Abstract translation: 式（I）化合物及其药学上可接受的盐：其中：R 1和R 2中的任一个是氢，另一个选自C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6 烷基羰氧基，C 1-6烷基羟甲基，硝基，氰基，氯，三氟甲基，C 1-6烷基亚磺酰基，C 1-6烷基磺酰基，C 1-6烷氧基亚磺酰基，C 1-6烷氧基磺酰基，C 1-6烷基羰基氨基，C 1-6烷氧基羰基氨基，C 1-6烷基 - 硫代羰基，C 1-6烷氧基 - 硫代羰基，C 1-6烷基 - 硫代羰基氧基，1-巯基C 2-7烷基，甲酰基或氨基亚磺酰基，氨基磺酰基或氨基羰基，氨基部分任选被一个或两个C 1-6烷基取代，或C 1 -6烷基亚磺酰氨基，C 1-6烷基磺酰基氨基C 1-6烷氧基亚磺酰基氨基或被C 1-6烷基羰基，硝基或氰基末端取代的C 1-6烷氧基磺酰基氨基或乙烯基，或-C（C 1-6烷基（NOH）或-C ）NNH 2，或者当Y为氧时，R 1和R 2中的一个为硝基，氰基或C 1-3烷基羰基，另一个为I 任选被C 2-7烷酰基取代的羟基或氨基; R3和R4之一是氢或C1-4烷基，另一个是C1-4烷基或R2和R3一起是C2-5聚亚甲基; R5是羟基，C1-6烷氧基或C1-7酰氧基; R6是氢或C1-6烷基; R7是NR8R9，其中R8和R9独立地是C1-6烷基，R8是氢，R9是C1-6烷基或R8和R9一起是C4-5聚亚甲基; 或R 6和R 8一起为 - （CH 2）n - ，其中n为2或3，并且R 9为氢或C 1-6烷基; 或R 7为CH 2 R 10，其中R 10为氢或任选被卤素，羟基或C 1-6烷氧基取代的C 1-5烷基; 或R 6和R 10为 - （CH 2）m - ，其中m为2或3; X是氧或硫; Y是氧，CH 2或NH; R6-CH-CX-R7基团反应到R5基团; 具有降血压活性，其制备方法及其作为药物的用途。

    Fluorine-containing carbonyl compounds and method for preparing the same
    96.
    发明授权
    Fluorine-containing carbonyl compounds and method for preparing the same 失效
    含氟羰基化合物及其制备方法

    公开(公告)号：US4929760A

    公开(公告)日：1990-05-29

    申请号：US221371

    申请日：1988-07-19

    Applicant: Tomoya Kitazume ,  Takashi Yamazaki ,  Seiten Rin

    Inventor： Tomoya Kitazume ,  Takashi Yamazaki ,  Seiten Rin

    IPC: C07C45/67 ,  C07C45/72 ,  C07C49/173 ,  C07C49/245 ,  C07C49/82 ,  C12P7/26 ,  C12P41/00

    CPC classification number: C07C49/173 ,  C07C45/673 ,  C07C45/72 ,  C07C49/245 ,  C07C49/82 ,  C12P41/004 ,  C12P7/26

    Abstract: Fluorine-containing carbonyl compounds of the formula ##STR1## and its optically active isomers, which are useful for liquid crystal, bioactive substances, medicines, agricultural medicines such as fungicides, herbicides and hormones, organic functional materials and LB membranes, prepared by the reaction with trifluoro acetoaldehyde and RCOCH.sub.3, wherein R is a substituted or not-substituted lower alkyl group, preferably a lower alkyl having not more than 10 carbon atoms, a substituted or not-substituted aromatic group or a substituted or not-substituted arylalkyl group.

    Abstract translation: 制备式（Ⅰ）的含氟羰基化合物及其旋光异构体，其可用于液晶，生物活性物质，药物，农药如杀真菌剂，除草剂和激素，有机功能材料和LB膜，其制备 通过与三氟乙醛和RCOCH 3的反应，其中R是取代或未取代的低级烷基，优选具有不超过10个碳原子的低级烷基，取代或未取代的芳族基团或取代或未取代的芳基烷基 组。

    Preparation of 1-(4-hydroxy-phenyl)-butan-3-one and novel intermediates
    97.
    发明授权
    Preparation of 1-(4-hydroxy-phenyl)-butan-3-one and novel intermediates 失效
    1-（4-羟基 - 苯基） - 丁-3-酮和新型中间体的制备

    公开(公告)号：US4908481A

    公开(公告)日：1990-03-13

    申请号：US798361

    申请日：1985-11-18

    Applicant: Werner Hoffmann ,  Dieter Degner

    Inventor： Werner Hoffmann ,  Dieter Degner

    IPC: C07C49/245 ,  B01J23/00 ,  B01J27/02 ,  C07B61/00 ,  C07C45/00 ,  C07C45/62 ,  C07C45/65 ,  C07C45/67 ,  C07C45/73 ,  C07C45/74 ,  C07C49/255 ,  C07C67/00

    CPC classification number: C07C49/255 ,  C07C45/62 ,  C07C45/673 ,  C07C45/73 ,  C07C45/74

    Abstract: A simple process for preparing 1-(4-hydroxy-phenyl)-butan-3-one, a sought-after natural aromatic, in a pure form and in good yield from easily accessible starting materials, wherein a 4-tert-alkoxy-benzaldehyde is condensed, under alkaline conditions, to give a novel 1-(4-tert.-alkoxy-phenyl)-but-1-en-3-one, the latter is hydrogenated, during or after this condensation, to give a novel 1-(4-tert.-alkoxy-phenyl)-butan-3-one, and isobutene or 2-methyl-but-1(2)-ene is eliminated from this compound in the presence of a catalytic amount of an acid. The novel intermediates have the general formula ##STR1## where R is H or CH.sub.3 and the broken line may or may not be an additional carbon-carbon bond.

    Abstract translation: 一种简单的制备1-（4-羟基 - 苯基）丁烷-3-酮的方法，一种被追求的天然芳族化合物，纯的形式和从容易获得的原料得到良好的产率，其中4-叔 - 烷氧基 - 苯甲醛在碱性条件下冷凝，得到新的1-（4-叔 - 烷氧基 - 苯基） - 丁-1-烯-3-酮，后者在该缩合之间或之后被氢化，得到一种新颖的 在催化量的酸的存在下，从该化合物中除去1-（4-叔 - 烷氧基 - 苯基） - 丁-3-酮和异丁烯或2-甲基 - 丁-1（2） - 烯。 新型中间体具有通式“IMAGE”，其中R是H或CH 3，虚线可以是或不是另外的碳 - 碳键。

    4-(1,1-Dimethylethyl)-4'-methoxydibenzoylmethane
    99.
    发明授权
    4-(1,1-Dimethylethyl)-4'-methoxydibenzoylmethane 失效
    4-（1,1-二甲基乙基）-4'-甲氧基二苯甲酰甲烷

    公开(公告)号：US4387089A

    公开(公告)日：1983-06-07

    申请号：US264774

    申请日：1981-05-18

    Applicant: Karl-Fred De Polo

    Inventor： Karl-Fred De Polo

    IPC: A61K8/35 ,  A61K8/37 ,  A61Q17/04 ,  C07C45/00 ,  C07C45/45 ,  C07C49/213 ,  C07C49/225 ,  C07C49/84 ,  C07C49/245 ,  A61K7/42

    CPC classification number: A61Q17/04 ,  A61K8/35 ,  A61K8/37 ,  C07C45/455 ,  C07C49/84

    Abstract: The novel 4-(1,1-Dimethylethyl)-4'-methoxydibenzoylmethane is useful as a sunscreen agent. It exhibits outstanding UV-A absorbing qualities in that it brings about a considerable retardation in the ageing of the skin with excellent skin tolerance and stability (light, heat and moisture).4-(1,1-Dimethylethyl)-4'-methoxydibenzoylmethane furthermore improves the protective action of UV B-filters, i.e. of substances which absorb the erythema-producing UV B-radiation in the range of about 290 to 320 mm.

    Abstract translation: 新型4-（1,1-二甲基乙基）-4'-甲氧基二苯甲酰甲烷可用作防晒剂。 它表现出优异的UV-A吸收性能，因为它在皮肤老化中带来显着的延迟，具有优异的皮肤耐受性和稳定性（光，热和湿气）。 4-（1,1-二甲基乙基）-4'-甲氧基二苯甲酰甲烷进一步改善了紫外线B过滤器，即吸收产生紫外线B辐射的物质在约290至320mm范围内的保护作用。

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