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    Supports and their use
    1.
    发明授权
    Supports and their use 失效
    支持及其使用

    公开(公告)号：US4812512A

    公开(公告)日：1989-03-14

    申请号：US878611

    申请日：1986-06-26

    申请人： Jean Buendia ,  Jeanine Nierat

    发明人： Jean Buendia ,  Jeanine Nierat

    IPC分类号： C07H21/02 ,  C07H21/00 ,  C07H21/04

    CPC分类号： C07H21/00

    摘要： Novel supports useful in solid phase synthesis of oligonucleotides of the formula ##STR1## wherein .circle.P is a material selected from the group consisting of functionalized glass micropellets, silica functionalized by aminoalkyl trialkoxysilane capable of to obtain for ##STR2## Kieselguhr, polytetrafluoroethylene, cellulose and metallic oxides, m is an integer from 1 to 20, A is selected from the group consisting of alkyl of 1 to 20 carbon atoms, saturated cycloalkyl of 3 to 12 carbon atoms, phenyl and 5 to 6 member heterocycles, x and y are an integer from 0 to 20, x.sub.1 is an integer from 1 to 20 and y.sub.1 is an integer from 0 to 10, a process for the preparation of said supports, the use of said supports and intermediates.

    摘要翻译： 新颖的载体可用于固相合成下式的寡核苷酸，其中＆cir＆P是选自官能化的玻璃微丸，由能够获得 Kieselguhr的氨基烷基三烷氧基硅烷官能化的二氧化硅的材料， 聚四氟乙烯，纤维素和金属氧化物，m是1至20的整数，A选自1至20个碳原子的烷基，3至12个碳原子的饱和环烷基，苯基和5至6个成员杂环，x y为0〜20的整数，x1为1〜20的整数，y1为0〜10的整数，制备所述载体的方法，所述载体和中间体的使用。

    Supports useful in solid phase synthesis of oligonucleotides
    2.
    发明授权
    Supports useful in solid phase synthesis of oligonucleotides 失效
    支持寡核苷酸的固相合成

    公开(公告)号：US4780504A

    公开(公告)日：1988-10-25

    申请号：US871451

    申请日：1986-06-05

    申请人： Jean Buendia ,  Jeanine Nierat

    发明人： Jean Buendia ,  Jeanine Nierat

    IPC分类号： C07H21/04 ,  B01J31/02 ,  C07F7/18 ,  C07H21/00 ,  C12P19/34 ,  C12P19/38

    CPC分类号： C07H21/00

    摘要： Novel supports useful in solid phase synthesis of oligonucleotides of the formula ##STR1## wherein .circle. is micro pellets of a material selected from the group consisting of glass, silica, Kieselguhr, polytetrafluoroethylene, cellulose and metallic oxides, m is an integer from 1 to 20, A is selected from the group consisting of alkylene of 1 to 20 carbon atoms, saturated cycloalkylene of 3 to 12 carbon atoms, phenyl and 5 to 6 member heterocycles, x is an integer from 0 to 20, x.sub.1 is an integer from 0 to 10 and the amino group may be in the m-, p- or o-position, a process for the preparation of said supports, the use of said supports and intermediates.

    摘要翻译： 新颖的载体可用于下式的寡核苷酸的固相合成：其中＆cir是选自玻璃，二氧化硅，硅藻土，聚四氟乙烯，纤维素和金属氧化物的材料的微丸，m是 A为1至20的整数，A选自1至20个碳原子的亚烷基，3至12个碳原子的饱和环亚烷基，苯基和5至6个成员杂环，x为0至20的整数，x1 是0至10的整数，并且氨基可以在m-，p-或o-位，制备所述载体的方法，所述载体和中间体的用途。

    Epimerization of trans chrysanthemates
    3.
    发明授权
    Epimerization of trans chrysanthemates 失效
    反式菊花异构化

    公开(公告)号：US4447637A

    公开(公告)日：1984-05-08

    申请号：US347278

    申请日：1982-02-09

    申请人： Jacques Martel ,  Jean Buendia ,  Jeanine Nierat

    发明人： Jacques Martel ,  Jean Buendia ,  Jeanine Nierat

    IPC分类号： C07C69/747 ,  C07C51/353 ,  C07C51/487 ,  C07C61/04 ,  C07C61/37 ,  C07C67/333 ,  C07C69/74 ,  C07C61/18

    CPC分类号： C07C61/37 ,  C07C51/353 ,  C07C51/487

    摘要： A novel process for the epimerization of alkyl trans chrysanthemates comprising reacting at a low temperature in an anhydrous organic solvent an alkyl trans chrysanthemate of the formula ##STR1## of the 1S, trans or 1R, trans configuration wherein R is alkyl of 1 to 6 carbon atoms with a strong alkali metal base to obtain a compound of the formula ##STR2## wherein R has the above definition and M is an alkali metal, reacting the latter compound with a reactant of the formulaY--Awherein A is selected from the group consisting of chlorine, bromine, iodine and anion derived from a hydrogen acid and Y is an organic radical capable of forming a ketal of a ketene to obtain a compound of the formula ##STR3## reacting the latter at a low temperature in an anhydrous organic solvent with a proton donor to obtain a mixture of the corresponding alkyl cis chrysanthemate and alkyl trans chrysanthemate and recovering the cis chrysanthemic acid of the formula ##STR4## with the 1R, cis or 1S, cis configuration.

    摘要翻译： 一种用于烷基反式菊氨酸差向异构化的新方法，其包括在低温下在无水有机溶剂中反应1S，反式或1R，反式构型的式II的烷基反式菊酯，其中R是1至6的烷基 具有强碱金属碱的碳原子以得到式III的化合物，其中R具有上述定义，M是碱金属，使后一化合物与式YA的反应物反应，其中A选自 由氯，溴，碘和由氢酸衍生的阴离子组成，Y是能够形成乙烯酮缩酮的有机基团，得到下式的化合物，其中IV在低温下与无水有机物 溶剂与质子供体反应，得到相应的顺式菊酸菊酯和反式菊酸酯的混合物，并用1R，顺式或1S的方法回收式Ⅰ的顺式菊酸， 顺式配置。

    Intermediates for the preparation of .DELTA..sup.4,9(11),17(20) -pregnatriene-3-ones
    5.
    发明授权
    Intermediates for the preparation of .DELTA..sup.4,9(11),17(20) -pregnatriene-3-ones 失效
    制备DELTA 4,9（11），17（20） - 三烯-3-酮的中间体

    公开(公告)号：US5594127A

    公开(公告)日：1997-01-14

    申请号：US557594

    申请日：1995-11-14

    申请人： Francis Brion ,  Jean Buendia ,  Christian Diolez ,  Michel Vivat

    发明人： Francis Brion ,  Jean Buendia ,  Christian Diolez ,  Michel Vivat

    IPC分类号： C07J7/00 ,  C07J13/00 ,  C07J21/00 ,  C07J33/00 ,  C07J75/00

    CPC分类号： C07J13/005 ,  C07J13/007 ,  C07J21/006 ,  C07J33/007 ,  Y02P20/55 ,  Y02P20/582

    摘要： A compound having a formula ##STR1## in which K is defined as above, C--P being CH.sub.2 or --C.dbd.CH.sub.2 or ##STR2## and J is --SO.sub.2 R.sub.2, or C--P is C.dbd.O and J is --CH.sub.2 Hal.sub.2, or C--P is --CH SO.sub.2 R.sub.2 and J is CO.sub.2 R or Hal.sub.1, R.sub.2 is methyl, phenyl, tolyl or xylyl, R is alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 is carbon atoms or a silylated remainder selected from the group consisting of trimethylsilyl, tert.-butyldimethylsilyl, triphenylsilyl and diphenyltert.-butylsilyl, Hal.sub.1 is halogen, Hal.sub.2 is chlorine, bromine or iodine and the wavy lines symbolize any one of the isomer forms or their mixtures which are intermediates.

    摘要翻译： 具有式“IMAGE”G的化合物，其中K如上所定义，CP是CH 2或-C = CH 2或者，而J是-SO 2 R 2，或CP是C = O，J是-CH 2 Hal 2，或CP是 -CH + Z SO 2 R 2，J为+ Z CO 2 R或Hal 1，R 2为甲基，苯基，甲苯基或二甲苯基，R为1至6个碳原子的烷基，7至15的芳烷基为碳原子或选自 由三甲基甲硅烷基，叔丁基二甲基甲硅烷基，三苯基甲硅烷基和二苯基叔丁基甲硅烷基组成，Hal1是卤素，Hal2是氯，溴或碘，波浪线表示任何一种异构体形式或它们作为中间体的混合物。

    Perfumant cyclopropane-carboxylic acid derivatives
    8.
    发明授权
    Perfumant cyclopropane-carboxylic acid derivatives 失效
    香料环丙烷 - 羧酸衍生物

    公开(公告)号：US4431576A

    公开(公告)日：1984-02-14

    申请号：US343348

    申请日：1982-01-27

    申请人： Jacques Martel ,  Jean Buendia ,  Francois Nezot

    发明人： Jacques Martel ,  Jean Buendia ,  Francois Nezot

    IPC分类号： C07C69/747 ,  A01N53/06 ,  A01N53/10 ,  A61K8/37 ,  A61Q13/00 ,  C07D307/54 ,  C07D307/58 ,  C07D333/24 ,  C07D333/32 ,  C11B9/00 ,  A61K7/46

    CPC分类号： C11B9/0092 ,  C07D307/54 ,  C07D333/24 ,  C11B9/003 ,  C11B9/0076

    摘要： A compound in all its possible isomeric forms and mixtures thereof of the formula ##STR1## wherein R is selected from the group consisting of (a) alkyl of 1 to 12 carbon atoms optionally substituted with cycloalkyl or cycloalkenyl of 3 to 6 carbon atoms or a hydrocarbon chain of 2 to 8 carbon atoms optionally interrupted by an oxygen or ketone, (b) alkenyl and alkynyl of 3 to 8 carbon atoms, (c) cycloalkyl of 3 to 12 carbon atoms optionally containing at least one double bond and substituted with at least one alkyl and (d) aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen and --CF.sub.3 and R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, --CHO, --COAlK.sub.1, --COOAlK.sub.2 and --CN, at least one being hydrogen, AlK.sub.1 and AlK.sub.2 are alkyl of 1 to 8 carbon atoms and R.sub.1 and R.sub.2 taken together with the carbon atom to which they are attached form the group ##STR2## and X is selected from the group consisting of sulfur, oxygen and imino joined to the 1-carbon atom with a double bond with the proviso that the double bond has the E geometry when R.sub.1 or R.sub.2 are --CHO, --COAlK.sub.1, --COOAlK.sub.2 or ##STR3## and their preparation and odorant compositions containing at least one compound of formula I as a perfume agent.

    摘要翻译： 化合物，其全部可能的异构形式及其混合物，其中R选自（a）任选被3至6个碳原子的环烷基或环烯基取代的1至12个碳原子的烷基或 2至8个碳原子的烃链任选被氧或酮中断，（b）3至8个碳原子的烯基和炔基，（c）3至12个碳原子的环烷基，任选地含有至少一个双键并被 至少一个烷基和（d）7-12个碳原子的芳烷基，任选被至少一个1-4个碳原子的烷基，1-4个碳原子的烷氧基，卤素和-CF 3和R 1和 R2分别选自氢，-CHO，-COAlK1，-COOAlK2和-CN，至少一个为氢，AlK1和AlK2为1至8个碳原子的烷基，R1和R2与碳原子一起 它们所连接的组由和X选自硫，氧和亚氨基与具有双键的1-碳原子连接，条件是当R1或R2为-CHO，-COAlK1， - COOAlK2或及其制备和加味剂组合物，其含有至少一种式I化合物作为预浸剂。

    .beta.-Lactones of 2-hydroxy-cyclopentane-carboxylic acids
    9.
    发明授权
    .beta.-Lactones of 2-hydroxy-cyclopentane-carboxylic acids 失效
    β-内酯2-羟基 - 环戊烷 - 羧酸的内酯

    公开(公告)号：US4308209A

    公开(公告)日：1981-12-29

    申请号：US216124

    申请日：1980-12-15

    申请人： Jean Buendia ,  Michel Vivat ,  Laurent Taliani

    发明人： Jean Buendia ,  Michel Vivat ,  Laurent Taliani

    IPC分类号： A61K31/337 ,  A61K31/34 ,  A61K31/365 ,  A61K31/38 ,  A61P9/12 ,  C07D305/14 ,  C07D309/12 ,  C07D333/32 ,  C07D409/06 ,  C07D409/12

    CPC分类号： C07D333/32 ,  C07D305/14 ,  C07D309/12

    摘要： Novel .beta.-lactones of 2-hydroxy-cyclopentane-carboxylic acids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl and R.sub.2 is selected from the group consisting of --CH.sub.2 --O--CH.sub.2 --CH.sub.3 and --X--Ar, X is selected from the group consisting of --O-- and --CH.sub.2 --, Ar is an optionally substituted member selected from the group consisting of thienyl, thiazolyl, phenyl and thiadiazolyl, the optional substituents being at least one member selected from the group consisting of halogen and --CF.sub.3 and the wavy lines indicate that the groups may be in the .alpha.,.beta. or .beta.,.alpha.-positions or mixtures thereof having hypotensive activity and their preparation.

    摘要翻译： 式（I）的2-羟基 - 环戊烷 - 羧酸的新型β-内酯，其中R 1选自氢和甲基，R 2选自-CH 2 -O-CH 2 -CH 3和 -X-Ar，X选自-O-和-CH 2 - ，Ar是选自噻吩基，噻唑基，苯基和噻二唑基的任选取代的成员，任选的取代基是至少一个选自 由卤素和-CF 3组成的组和波浪线表示这些基团可以是具有低血压活性的α，β或β，α-位或其混合物及其制备。

    Process for the preparation of biphenyl derivatives
    10.
    发明授权
    Process for the preparation of biphenyl derivatives 失效
    联苯衍生物的制备方法

    公开(公告)号：US5618975A

    公开(公告)日：1997-04-08

    申请号：US449396

    申请日：1995-05-24

    申请人： Adalbert Wagner ,  Neerja Bhatnagar ,  Jean Buendia ,  Christine Griffoul

    发明人： Adalbert Wagner ,  Neerja Bhatnagar ,  Jean Buendia ,  Christine Griffoul

    IPC分类号： B01J23/44 ,  A61K31/235 ,  A61K31/41 ,  C07B37/04 ,  C07B61/00 ,  C07C41/48 ,  C07C45/61 ,  C07C45/71 ,  C07C47/546 ,  C07C67/30 ,  C07C67/343 ,  C07C69/76 ,  C07C69/767 ,  C07C253/30 ,  C07C255/37 ,  C07C255/40 ,  C07C255/56 ,  C07C303/40 ,  C07C311/09 ,  C07C311/48 ,  C07C311/51 ,  C07C311/52 ,  C07C311/53 ,  C07C311/54 ,  C07C311/57 ,  C07C311/58 ,  C07D257/04 ,  C07C311/21

    CPC分类号： C07D257/04 ,  C07B37/04 ,  C07C253/30 ,  C07C303/40 ,  C07C311/09 ,  C07C311/51 ,  C07C311/58 ,  C07C67/343

    摘要： Biphenyl derivatives and processes for the preparation of biphenyl derivatives are described. A compound of formula (I) is disclosed ##STR1## in which the substituent X is --CHO or --CH(OR.sup.1)OR.sup.2, where R.sup.1 and R.sup.2 independently of one another are (C.sub.1 -C.sub.6)-alkyl or R.sup.1 and R.sup.2 together are an alkylene group (--CH.sub.2).sub.n --, where n is 2, 3 4 or 5 and R is --F, --Cl, --NO.sub.2, --(CH.sub.2).sub.m --COOR.sup.3, --(CH.sub.2).sub.m --CONHR.sup.3, --(CH.sub.2).sub.m --CN, --SO.sub.2 NH--COOR.sup.3, --SO.sub.2 NH--CO--NHR.sup.3, --SO.sub.2 NH--SO.sub.2 --R.sup.3, --NHSO.sub.2 R.sup.3, ##STR2## --PO.sub.3 R.sup.3, --NH--SO.sub.2 --CF.sub.3, --SO.sub.2 NR.sup.4 where R.sup.3 is hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.3 -C.sub.6)cycloalkyl, or (C.sub.1 -C.sub.6)-alkyl-(C.sub.3 -C.sub.6)cycloalkyl and R.sup.4 is a group .dbd.C--N(CH.sub.3).sub.2, and m is 0, 1, 2, 3, or 4. The invention also relates to a process for the preparation of a compound of the formula (I) in which X is an optionally protected formyl group and R is a group which is itself inert to the reaction conditions of the synthesis, which comprises reacting a compound of the formula (II) ##STR3## with a substituted phenyl-halogen compound of the formula (III) ##STR4## wherein the substituent Hal is a halogen group.

    摘要翻译： 描述了联苯衍生物和制备联苯衍生物的方法。 公开了式（I）化合物，其中取代基X为-CHO或-CH（OR 1）OR 2，其中R 1和R 2彼此独立地为（C 1 -C 6） - 烷基或R 1和 R2一起是亚烷基（-CH 2）n - ，其中n是2,3,4或5，R是-F，-Cl，-NO 2， - （CH 2）m -COOR 3， - （CH 2）m -CONHR 3， - （CH2）m-CN，-SO2NH-COOR3，-SO2NH-CO-NHR3，-SO2NH-SO2-R3，-NHSO2R3，-PO3R3，-NH-SO2-CF3，-SO2NR4，其中R3是氢， （C 1 -C 6） - 烷基，（C 3 -C 6）环烷基或（C 1 -C 6） - 烷基 - （C 3 -C 6）环烷基，R 4是基团= CN（CH 3）2，m是0,1,2 ，3或4.本发明还涉及一种制备式（I）化合物的方法，其中X是任选保护的甲酰基，R是本身对于合成的反应条件是惰性的基团 其包括使式（II）化合物（II）与式（III）取代的苯基 - 卤素化合物（III）反应，其中取代基Hal为卤素基团。