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    Thiolsilanes, method of their production and of their use
    31.
    发明授权
    Thiolsilanes, method of their production and of their use 失效
    硫代硅烷，其生产方法及其用途

    公开(公告)号：US5792881A

    公开(公告)日：1998-08-11

    申请号：US793270

    申请日：1997-03-05

    Applicant: Herbert Wolter ,  Werner Storch

    Inventor： Herbert Wolter ,  Werner Storch

    IPC: C07F7/18 ,  C08G77/20 ,  C08G77/26 ,  C08G77/28 ,  C08K5/54 ,  C07F7/10 ,  C07F7/08

    CPC classification number: C07F7/184 ,  C07F7/182 ,  C07F7/1836 ,  C08G77/20 ,  C08G77/26 ,  C08G77/28 ,  C08K5/5406

    Abstract: The invention relates to hydrolyzable and polyadditive silanes, a method ofheir production and of their use in the production of (hetero) silicic acid polycondensates and of polyadducts. The silanes in accordance with the invention have the general formula �(HS--R.sup.5).sub.n R.sup.6 --S--E--R.sup.5 !.sub.a SiX.sub.x R.sup.3.sub.4-a-x (I) in which the groups and indices are equal or different and have the following meaning: E=--CO--NH--, CS--NH--, --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 --CH(OH)--; R.sup.3 =alkyl, alkenyl, aryl, alkylaryl or arylalkyl each with 1 to 15 carbon atoms, whereby these groups may be interrupted by oxygen or sulfur atoms, by ester, carbonyl, amide or amino groups; R.sup.5 =Alkene, arylene, arylenealkene or arylenealkene each with 1 to 15 carbon atoms, whereby these groups may be interrupted by oxygen or sulfur atoms, by ester, carbonyl, amide or amino groups; R.sup.6 =alkene, arylene, arylenealkene or arylenealkene each with 1 to 15 carbon atoms, whereby these groups may be interrupted by oxygen or sulfur atoms, by ester, carbonyl, amide or amino groups; X=hydrogen, halogen, hydroxy, alkoxy, acyloxy, alkylcarbonyl, alkoxycarbonyl or NR".sub.2 ; a=1, 2 or 3; n=2, 3, 4 or 5; x=1, 2 or 3.

    Abstract translation: PCT No.PCT / DE96 / 01217 Sec。 371日期1997年3月5日 102（e）1997年3月5日PCT PCT 1996年7月5日PCT公布。 出版物WO97 / 02270 日期1997年1月23日本发明涉及可水解和多加成硅烷，其生产方法及其在（异）硅酸缩聚物和多加合物的制备中的应用。 根据本发明的硅烷具有通式[（HS-R5）nR6-SE-R5] aSiXxR34-ax（I），其中基团和指数相同或不同，具有以下含义：E = -CO- NH-，CS-NH-，-CH 2 -CH 2 - 或-CH 2 -CH（OH） - ; R3 =烷基，烯基，芳基，烷基芳基或芳烷基，各自具有1至15个碳原子，由此这些基团可被酯，羰基，酰胺或氨基的氧或硫原子间隔; R5 =烯烃，亚芳基，亚芳基烯或亚芳基烯烃，各自具有1至15个碳原子，由此这些基团可被酯，羰基，酰胺或氨基的氧或硫原子间隔; R6 =烯烃，亚芳基，亚芳基烯烃或亚芳基烯烃，各自具有1至15个碳原子，由此这些基团可被酯，羰基，酰胺或氨基的氧或硫原子间隔; X =氢，卤素，羟基，烷氧基，酰氧基，烷基羰基，烷氧基羰基或NR'2; a = 1,2或3; n = 2,3,4或5; x = 1,2或3。

    Retro-.alpha.-retinol (4,14-retro-retinol) derivatives and uses of retro-.alpha.-retinol
    35.
    发明授权
    Retro-.alpha.-retinol (4,14-retro-retinol) derivatives and uses of retro-.alpha.-retinol 失效
    复方α-吗啉醇（4,14-反 - 视黄醇）衍生物及其用途

    公开(公告)号：US5521221A

    公开(公告)日：1996-05-28

    申请号：US682909

    申请日：1991-04-09

    Applicant: Jochen Buck ,  Ulrich Hammerling ,  Fadila Derguini ,  Koji Nakanishi

    Inventor： Jochen Buck ,  Ulrich Hammerling ,  Fadila Derguini ,  Koji Nakanishi

    IPC: A01N37/18 ,  A01N37/34 ,  A61K31/07 ,  A61K31/23 ,  A61K31/70 ,  C07C403/08 ,  C07D303/14 ,  C07D317/20 ,  C07F7/18 ,  C12N1/38 ,  C12N5/078 ,  C12N5/0783 ,  C12N15/67 ,  C12P17/02 ,  C12P23/00 ,  C07C35/18 ,  C07C37/68

    CPC classification number: C12P23/00 ,  C07C403/08 ,  C07C403/10 ,  C07C403/12 ,  C07D303/14 ,  C07F7/184 ,  C12N15/67 ,  C12N5/065 ,  C07B2200/09 ,  C07C2101/14 ,  C07C2101/16 ,  C12N2501/385

    Abstract: This invention provides a purified retro-retinoid compound characterized by a molecular mass of about 302 daltons. Also provided by this invention is a method of enhancing the growth of a cell in a vitamin A reduced environment which comprises contacting the cell with an effective growth enhancing amount of a compound having a structure: ##STR1## wherein the configuration of the C6, C8, C10 and C12 double bond independently is Z or E and the absolute configuration at C-14 is independently R or S; wherein R.sub.1 is alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acid halide, amide, nitrile, or amine; and wherein R.sub.2 is hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R.sub.1 and R.sub.2 are replaced by a 14, 15-oxirane group; and wherein the retro structure is alpha or gamma. Further provided are a method for enhancing transcription of a gene regulated by retinoid in a cell, or a method for enhancing an immune response in a subject.

    Abstract translation: 本发明提供了一种以分子质量为约302道尔顿为特征的纯化的后视色素化合物。 本发明还提供了增强维生素A还原环境中细胞生长的方法，其包括使细胞与有效生长增加量的具有以下结构的化合物接触：其中C6，C8的构型 ，C10和C12双键独立地为Z或E，C-14的绝对构型独立地为R或S; 其中R1是烷基，烷基卤，醇，酯，醚，醛，酮，羧酸，羧酸酯，酰卤，酰胺，腈或胺; 烷基，醇，醚，醛，酮，羧酸，羧酸酯，腈，胺，叠氮化物，烷基卤，酰卤，叠氮化物或酰胺; 或其中R 1和R 2被14,15-环氧乙烷基团取代; 并且其中所述复古结构是α或γ。 还提供了增强细胞中类视黄醇调节基因转录的方法，或增强受试者的免疫应答的方法。

    (2-arylpropyl)alkylsilanes and their preparation methods
    37.
    发明授权
    (2-arylpropyl)alkylsilanes and their preparation methods 失效
    （2-芳基丙基）烷基硅烷及其制备方法

    公开(公告)号：US5386050A

    公开(公告)日：1995-01-31

    申请号：US176433

    申请日：1994-01-03

    Applicant: Il N. Jung ,  Bok R. Yoo ,  Bong W. Lee ,  Seung H. Yeon

    Inventor： Il N. Jung ,  Bok R. Yoo ,  Bong W. Lee ,  Seung H. Yeon

    IPC: C07F7/08 ,  C07F7/12 ,  C07F7/18

    CPC classification number: C07F7/184 ,  C07F7/0896 ,  C07F7/12 ,  C07F7/1836

    Abstract: The present invention relates to a process for preparing (2-arylpropyl)alkylsilanes represented by the formula III by reacting (2-arylpropyl)silanes represented by the formula I with olefin compounds represented by the formula II in the presence of hydrosilation catalysts such as chloroplatanic acid, platinum on silica, tributylamine and Pd, Rh, Ni metals. ##STR1## Olefin compounds(cyclohexene or CH.sub.2 =CH--R.sup.3) (II) ##STR2## In the formulas (I) and (III), R.sup.1 and R.sup.2 represent independently hydrogen, alkyl(C.sub.1 -C.sub.4), fluoro, chloro or bromo; and Ar represents phenyl ring, naphthalene ring, or biphenyl ring. X represents hydrogen or chloro group. In the formula (III), R represents --(CH.sub.2 CH.sub.2)--R.sup.3, sec-butyl, or cyclohexyl wherein R.sup.3 =Ph, CH.sub.2 Cl, C.sub.n H.sub.2n CH.sub.3 (n=0-15), CH.sub.2 Si(Me).sub.m Cl.sub.3-m (m=O-3), (CH.sub.2).sub.2 Si(Me).sub.m (OMe).sub.3-m (m=O-3), (CH.sub.2).sub.3 Si(Me).sub.m (OMe).sub.3-m (m=O-3), Si(Me).sub.m Cl.sub.3-m (m=0-3), CF.sub.3, CN, CH.sub.2 CN, ##STR3## CH.dbd.CH.sub.2, (CH.sub.2 ).sub.4 CH.dbd.CH.sub.2, ##STR4## or Ph--CH.sub.2 Cl.

    Abstract translation: 本发明涉及通过使式I表示的（2-芳基丙基）硅烷与式II表示的烯烃化合物在氢化硅烷化催化剂如氯铂酸存在下反应来制备由式III表示的（2-芳基丙基）烷基硅烷的方法 酸，二氧化硅上的铂，三丁胺和Pd，Rh，Ni金属。 （I）烯烃化合物（环己烯或CH 2 = CH-R 3）（II）（III）在式（I）和（III）中，R 1和R 2分别独立地表示氢，烷基（C 1 -C 4） ，氟，氯或溴; Ar表示苯环，萘环或联苯环。 X表示氢或氯基。 在式（III）中，R表示 - （CH2CH2）-R3，仲丁基或环己基，其中R3 = Ph，CH2Cl，CnH2nCH3（n = 0-15），CH2Si（Me）mCl3-m（m = 3），（CH 2）2 Si（Me）m（OMe）3-m（m = O-3），（CH 2）3 Si（Me）m（OMe）3-m ）mCl3-m（m = 0-3），CF3，CN，CH2CN，CH = CH2，（CH2）4CH = CH2，IMA或Ph-CH2Cl。

    Asymmetric synthesis of taxol side chain
    39.
    发明授权
    Asymmetric synthesis of taxol side chain 失效
    紫杉醇侧链的不对称合成

    公开(公告)号：US5300638A

    公开(公告)日：1994-04-05

    申请号：US914909

    申请日：1992-07-16

    Applicant: Vittorio Farina ,  Sheila I. Hauck

    Inventor： Vittorio Farina ,  Sheila I. Hauck

    IPC: C07D305/14 ,  A61K31/355 ,  C07B53/00 ,  C07D205/08 ,  C07F7/18

    CPC classification number: C07D205/08 ,  C07F7/184 ,  C07F7/186 ,  C07F7/1896 ,  Y02P20/55

    Abstract: The present invention relates to a process for the preparation of (3R, 4S)-3-hydroxy-4-phenyl-2-azetidinone derivatives which are useful intermediates in the synthesis of taxol from baccatin III, said process comprises reacting an acyloxyacetyl halide with an imine derived from L-threonine; and to compounds of formula (III) which are produced in said process: ##STR1## wherein Ar is phenyl; R.sup.1 is hydrogen, an acyl radical of a carboxylic acid, or a carbonic acid ester radical; R.sup.2 is hydrogen or a carboxy protecting group; and R.sup.3 is hydrogen or a hydroxy protecting group.

    Abstract translation: 本发明涉及一种制备（3R，4S）-3-羟基-4-苯基-2-氮杂环丁酮衍生物的方法，它们是从浆果赤霉素Ⅲ合成紫杉醇中的有用中间体，所述方法包括使酰氧基乙酰卤与 衍生自L-苏氨酸的亚胺; 和在所述方法中制备的式（III）化合物：（*化学结构*）其中Ar是苯基; R1是氢，羧酸的酰基或碳酸酯基; R2是氢或羧基保护基; 并且R 3是氢或羟基保护基。

    Protected formylpentanediols, hydroxymethylpentanediols, process for their preparation and intermediates
    40.
    发明授权
    Protected formylpentanediols, hydroxymethylpentanediols, process for their preparation and intermediates 失效
    受保护的甲酰戊二醇，羟甲基戊二醇，其制备方法和中间体

    公开(公告)号：US5274157A

    公开(公告)日：1993-12-28

    申请号：US969632

    申请日：1992-10-30

    Applicant: Heinz Moser

    Inventor： Heinz Moser

    IPC: C07C43/178 ,  C07C47/47 ,  C07D319/08 ,  C07D321/10 ,  C07D321/12 ,  C07D327/10 ,  C07D473/34 ,  C07F7/08 ,  C07F7/18 ,  C07D321/00 ,  C07D319/00

    CPC classification number: C07D319/08 ,  C07C43/1788 ,  C07D327/10 ,  C07D473/34 ,  C07F7/0841 ,  C07F7/184 ,  C07F7/1856 ,  C07C2101/06

    Abstract: Compounds of the formula Ib ##STR1## in which R.sub.1 and R.sub.2 independently of one another are linear or branched C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 8 ring carbon atoms, phenylalkyl having 1 to 4 C atoms in the alkylene group, the cyclic radicals being unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, or R.sub.1 and R.sub.2 independently of one another are --SiR.sub.4 R.sub.5 R.sub.6 in which R.sub.4, R.sub.5 and R.sub.6 independently of one another are C.sub.1 -C.sub.12 alkyl, phenyl, benzyl, or phenyl or benzyl, each of which is substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and R.sub.3 is a bridging member which, together with the radical --OCH--CH.sub.2 --CHO-- to which it is bonded, forms a 6- to 8-membered ring. These compounds are valuable intermediates for the preparation of carbacyclic nucleosides of the natural and unnatural series and of the racemates.

    Abstract translation: 其中R 1和R 2彼此独立地为直链或支链C 1 -C 12烷基，具有5至8个环碳原子的环烷基，亚烷基中具有1至4个C原子的苯基烷基的式Ib化合物 未取代或被C1-C4烷基或C1-C4烷氧基或R1和R2彼此独立取代的环基是-SiR4R5R6，其中R4，R5和R6彼此独立地是C1-C12烷基，苯基，苄基或苯基或苄基 ，其各自被C 1 -C 4烷基或C 1 -C 4烷氧基取代，并且R 3是与其键合的基团-OCH-CH 2 -CH 2 - 一起形成6-至8-元环的桥连构件。 这些化合物是制备天然和非天然系列和外消旋体的碳环核苷的有价值的中间体。

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