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    Process for the synthesis of eneamide derivatives
    6.
    发明授权
    Process for the synthesis of eneamide derivatives 有权
    合成烯酰胺衍生物的方法

    公开(公告)号：US07884243B2

    公开(公告)日：2011-02-08

    申请号：US10583902

    申请日：2004-12-22

    申请人： Alain Burgos ,  Blandine Bertrand ,  Sonia Roussiasse ,  Jean-François Pluvie ,  Sylvie Blanchet ,  Juliette Martin ,  Florence Perrin ,  Françoise Bourdeau

    发明人： Alain Burgos ,  Blandine Bertrand ,  Sonia Roussiasse ,  Jean-François Pluvie ,  Sylvie Blanchet ,  Juliette Martin ,  Florence Perrin ,  Françoise Bourdeau

    IPC分类号： C07C233/00

    CPC分类号： C07C231/10 ,  C07C233/06 ,  C07C2602/08 ,  C07C2602/10

    摘要： A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, —CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or —COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, which comprise: a hydrogenation/isomerization reaction in presence of a heterogeneous catalyst, of an oxime derivatives of formula (II) wherein R1, R2 and R3 are as defined above with an acyl derivative of formula (III) (R4CO)mX wherein R4, m and X are as defined above.

    摘要翻译： 制备由式（I）表示的烯 - 酰胺衍生物的方法，其中R 1和R 2和R 3独立地为氢原子，烷基，环烷基，环烷基烷基，烷基芳基，芳基，杂环，氰基， 烷氧基，芳氧基，羧基，氨基甲酰基-CONR 5 R 6（其中R 5和R 6独立地是烷基，芳基烷基或芳基，所述环被取代或不被官能团或与R5）或-COOR5基团（其中 R5是烷基，烷基芳基或芳基），所述烷基，环烷基，环烷基烷基，烷基芳基和芳基被官能团取代或不与R5取代; 或R 1和R 2一起形成环（该术语包括单环，二和更高多环系）; R4是氢原子，烷基，芳基，烷基芳基，所述基团被卤素原子取代或未被取代为Cl，Br或F; X是氧原子或离去基团，m是整数1或2; 当m为1时，X为离去基团; 当m为2时，X为氧原子，其包括：在非均相催化剂存在下的氢化/异构化反应，式（II）的肟衍生物，其中R 1，R 2和R 3如上定义，与酰基衍生物 式（III）（R4CO）mX其中R4，m和X如上所定义。

    In situ or one-pot hydrogenation and reductive amination process
    7.
    发明申请
    In situ or one-pot hydrogenation and reductive amination process 失效
    原位或一锅加氢和还原胺化方法

    公开(公告)号：US20080125606A1

    公开(公告)日：2008-05-29

    申请号：US11656573

    申请日：2007-01-23

    申请人： Alain Burgos ,  Jacques Tonnel ,  Valerie Dambrin ,  Denis Lucet ,  Patricia Poirier

    发明人： Alain Burgos ,  Jacques Tonnel ,  Valerie Dambrin ,  Denis Lucet ,  Patricia Poirier

    IPC分类号： C07C213/02 ,  C07C47/04

    CPC分类号： C07C213/02 ,  C07C2601/14 ,  C07C217/74

    摘要： An in situ or one-pot process for the preparation of the compounds of formula (I) uses a compound of general formula (I): and includes:a) the hydrogenation of a nitrile group of the compound of general formula (II): in which R1 to R4 are especially H or alkyl and n varies from 0 to 4, in the presence of a hydrogenation catalyst, a methylating agent and an organic acid as solvent, and at a temperature Ta below the initiation temperature of a reductive amination reaction, to give a primary amine from the nitrile group; andb) the reductive amination of the primary amine in the presence of hydrogen, at a temperature Tb above Ta, to give the dimethylated amine of general formula (I) by activation of the methylating age.

    摘要翻译： 用于制备式（I）化合物的原位或一锅法使用通式（I）的化合物：其包括：a）通式（II）的化合物的腈基的氢化： 其中R 1至R 4特别是H或烷基，n在0至4之间变化，在氢化催化剂，甲基化剂和作为溶剂的有机酸的存在下，在低于 还原胺化反应的起始温度，从腈基中得到伯胺; 和b）在氢存在下，在高于Ta的温度Tb下，伯胺的还原胺化，得到通过甲基化时代的活化的通式（I）的二甲基化胺。

    Method for preparing amino acid esters of nucleoside analogues
    9.
    发明申请
    Method for preparing amino acid esters of nucleoside analogues 审中-公开
    制备核苷类似物氨基酸酯的方法

    公开(公告)号：US20060178512A1

    公开(公告)日：2006-08-10

    申请号：US11051895

    申请日：2005-02-04

    申请人： Cheruthur Govindan ,  Alain Burgos ,  Huayun Yu ,  Sarah Topper

    发明人： Cheruthur Govindan ,  Alain Burgos ,  Huayun Yu ,  Sarah Topper

    IPC分类号： C07F9/6512

    CPC分类号： C07D473/00

    摘要： Describes a process for preparing esters of nucleoside analogues comprising condensing a nucleoside analogue with a protected amino acid in the presence of a tertiary amine and in the presence of an activating amount of an activating agent chosen from organo phosphoryl halide, organo phosphinic halide, aliphatic sulfonyl halide, and aromatic sulfonyl halide.

    摘要翻译： 描述了制备核苷类似物的酯的方法，包括在叔胺存在下将核苷类似物与受保护的氨基酸缩合，并且在活化剂量的活化剂存在下，选自有机磷酰卤，有机次膦酰卤，脂族磺酰基 卤化物和芳族磺酰卤。