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    Method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof
    1.
    发明授权
    Method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof 失效
    制备4-羟基异亮氨酸非对映异构体及其对映体及其衍生物的方法

    公开(公告)号：US07420087B2

    公开(公告)日：2008-09-02

    申请号：US10537293

    申请日：2003-12-01

    申请人： Charles Mioskowski ,  Alain Wagner ,  Sandra De Lamo Marin ,  Cedric Catala ,  Jean-Michel Becht

    发明人： Charles Mioskowski ,  Alain Wagner ,  Sandra De Lamo Marin ,  Cedric Catala ,  Jean-Michel Becht

    IPC分类号： C07C229/00 ,  C07D305/12

    CPC分类号： C07D307/66 ,  C07C227/32 ,  C07C229/22

    摘要： The invention concerns a method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof of general formula (I), characterized in that it consists in reducing an isoxazole derivative of formula (II) in conditions directly resulting in the derivatives of formula (I), or in obtaining at least a lactone of structure (III) in racemic form(s), or a enantiomerically enriched mixture, followed by opening, in basic conditions, in an aprotic or protic solvent, the desired lactone(s) and, optionally, separating the desired form. The invention is useful for preparing in particular (2S, 3R, 4S)-4-hydroxyisoleucine.

    摘要翻译： 本发明涉及一种制备通式（I）的4-羟基异亮氨酸非对映异构体及其衍生物的方法，其特征在于其在直接得到式（I）衍生物的条件下还原式（II）的异恶唑衍生物， ，或至少获得外消旋形式的结构（III）的内酯或对映异构体富集的混合物，然后在碱性条件下，在非质子或质子溶剂中，所需的内酯和任选的 ，分离所需的形式。 本发明可用于特别制备（2S，3R，4S）-4-羟基异亮氨酸。

    Method for the synthesis of 4-hydroxyisoleucine and the derivatives thereof
    2.
    发明申请
    Method for the synthesis of 4-hydroxyisoleucine and the derivatives thereof 失效

    公开(公告)号：US20070043240A1

    公开(公告)日：2007-02-22

    申请号：US10555875

    申请日：2004-05-07

    申请人： Charles Mioskowski ,  Cedric Catala ,  Alain Wagner

    发明人： Charles Mioskowski ,  Cedric Catala ,  Alain Wagner

    IPC分类号： C07C227/12

    CPC分类号： C07C227/30 ,  C07B2200/07 ,  C07C227/16

    摘要： The invention relates to a method for the synthesis of two isomers, at function OH, alone or in mixtures, of amino acids α or the derivatives thereof, having general formula (B), wherein: linkage C—O of the 4-position carbon (represented by symbol) denotes one or other of isomers III or IV, or mixtures thereof. Moreover, R1 and R2 represent: a hydrogen atom; or either R1 or R2 represents a hydrogen atom and the other substituent is a radical Ra, an acyl group —CORa, such as acetyl, or a functional group —COORa, —SO2Ra, —N (Ra, Rb), Ra and Rb, which are identical or different, representing a C1-C12 linear or branched alkyl radical, optionally substituted, an aryl group with one or more aromatic rings and heterocycles, comprising between 5 and 8C, optionally substituted, or aralkyl, the alkyl substituent and the aryl group being as defined above; or R1 and R2 both represent a substituent as defined above. R3 represents a hydrogen atom or Ra and R4 has the significance of Ra. The invention is characterised in that it comprises: the isomerisation of a compound having formula (I), wherein R1, R2, Ra, R3 and R4 are as defined above, such as to produce a compound having formula (II); and the reduction of the carbonyl function thereof which, depending on the catalytic system employed and the formula (I) compound used, produces one of the isomers having general formula (III) or (IV) or a mixture thereof having formula (B). The invention can be used for the synthesis of (2S, 3R, 4S)-4-hydroxyisoleucine.

    Method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof
    3.
    发明申请
    Method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof 失效
    制备4-羟基异亮氨酸非对映异构体及其对映异构体及其衍生物的方法

    公开(公告)号：US20060205817A1

    公开(公告)日：2006-09-14

    申请号：US10537293

    申请日：2003-12-01

    申请人： Charles Mioskowski ,  Alain Wagner ,  Sandra De Lamo Marin ,  Cedric Catala ,  Jean-Michel Becht

    发明人： Charles Mioskowski ,  Alain Wagner ,  Sandra De Lamo Marin ,  Cedric Catala ,  Jean-Michel Becht

    IPC分类号： A61K31/198 ,  C07C227/02

    CPC分类号： C07D307/66 ,  C07C227/32 ,  C07C229/22

    摘要： The invention concerns a method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof of general formula (I), characterized in that it consists in reducing an isoxazole derivative of formula (II) in conditions directly resulting in the derivatives of formula (I), or in obtaining at least a lactone of structure (III) in racemic form(s), or a enantiomerically enriched mixture, followed by opening, in basic conditions, in an aprotic or protic solvent, the desired lactone(s) and, optionally, separating the desired form. The invention is useful for preparing in particular (2S, 3R, 4S)-4-hydroxyisoleucine

    摘要翻译： 本发明涉及一种制备通式（I）的4-羟基异亮氨酸非对映异构体及其衍生物的方法，其特征在于其在直接得到式（I）衍生物的条件下还原式（II）的异恶唑衍生物， ，或至少获得外消旋形式的结构（III）的内酯或对映异构体富集的混合物，然后在碱性条件下，在非质子或质子溶剂中，所需的内酯和任选的 ，分离所需的形式。 本发明可用于特别制备（2S，3R，4S）-4-羟基异亮氨酸

    Method of use for characterizing the catalytic reactivity of catalyst(s)
    4.
    发明申请
    Method of use for characterizing the catalytic reactivity of catalyst(s) 失效
    用于表征催化剂的催化反应性的方法

    公开(公告)号：US20070161038A1

    公开(公告)日：2007-07-12

    申请号：US10587177

    申请日：2005-01-28

    申请人： Alain Wagner ,  Cedric Catala

    发明人： Alain Wagner ,  Cedric Catala

    IPC分类号： C40B40/04

    CPC分类号： C40B40/18 ,  B01J31/0235 ,  B01J31/0237 ,  B01J31/2239 ,  B01J31/2404 ,  B01J31/26 ,  B01J2219/00738 ,  B01J2231/005 ,  B01J2231/4266 ,  B01J2531/16 ,  B01J2531/26 ,  B01J2531/30 ,  B01J2531/40 ,  B01J2531/80 ,  B01J2531/824 ,  C40B30/08 ,  Y10T436/21 ,  Y10T436/212 ,  Y10T436/214 ,  Y10T436/216 ,  Y10T436/24

    摘要： A method for selecting at least one catalyst from a catalyst library on the basis of the reactivity thereof in a chemical conversion process includes: (a) testing the catalytic activity of a first catalyst from said catalyst library with respect to a reaction medium containing, as the compounds to be converted, at least one reactivity probe having a labeling system and including at least one reaction unit capable of reacting in said chemical conversion; (b) analyzing the reaction medium after said catalytic test for the purpose of qualitatively and/or qualitatively characterizing the resulting compounds; (c) repeating steps (a) and (b) for at least one other catalyst in said library; and (d) comparing the analysis results for each catalyst in order to characterize at least one catalyst having the required reactivity in said chemical conversion.

    摘要翻译： 基于化学转化方法的反应性，从催化剂文库中选择至少一种催化剂的方法包括：（a）测定第一催化剂从所述催化剂文库相对于反应介质的催化活性，所述反应介质含有 待转化的化合物，至少一种具有标记系统的反应性探针，并且包括能够在所述化学转化中反应的至少一个反应单元; （b）在所述催化试验之后分析反应介质，以定性和/或定性地表征所得化合物; （c）对所述文库中的至少一种其它催化剂重复步骤（a）和（b）; 和（d）比较每种催化剂的分析结果，以便表征在所述化学转化中具有所需反应性的至少一种催化剂。

    Method for creating a database enabling the selection of at least one reaction-capable catalyst
    5.
    发明申请
    Method for creating a database enabling the selection of at least one reaction-capable catalyst 审中-公开
    用于创建能够选择至少一种具有反应性的催化剂的数据库的方法

    公开(公告)号：US20070161039A1

    公开(公告)日：2007-07-12

    申请号：US10587336

    申请日：2005-01-28

    申请人： Alain Wagner ,  Cedric Catala

    发明人： Alain Wagner ,  Cedric Catala

    IPC分类号： C40B30/02 ,  C40B40/04

    CPC分类号： C40B30/08 ,  B01J2219/00702

    摘要： The invention relates to a method for creating a database enabling, in particular, the selection of at least one reaction-capable catalyst, comprising the following steps: a) preparing a number of different reaction media containing the same reactivity probe and each having at least one catalyst; b) analyzing, by means of an analytic method, each reaction medium after reaction, and; c) assigning, in the database, an analysis result according to step b) to the reactivity probe, this result characterizing different reaction products obtained from said reactivity probe. The database is a relational database containing: a first entity in which items of information relative to the reaction patterns listed in the data base are recorded; a second entity containing items of information relative to the state of bindings of at least one reaction pattern listed in the first entity; a third entity in which items of information associated with different reaction media are stored, and; at least one fourth entity in which items of information are stored that are linked to the analysis results of the reaction media at the end of a reaction.

    摘要翻译： 本发明涉及一种用于创建数据库的方法，其特别是选择至少一种具有反应能力的催化剂，其包括以下步骤：a）制备包含相同反应性探针的多种不同的反应介质， 一种催化剂; b）通过分析方法分析反应后各反应介质; c）在数据库中将根据步骤b）的分析结果分配给反应性探针，该结果表征从所述反应性探针获得的不同反应产物。 数据库是一个关系数据库，它包含：第一个实体，其中记录了相对于数据库中列出的反应模式的信息项; 第二实体，其包含相对于在第一实体中列出的至少一个反应模式的绑定状态的信息项; 存储与不同反应介质相关联的信息项目的第三实体; 至少一个第四实体，其中在反应结束时存储与反应介质的分析结果相关联的信息项。

    Process for functionalising a phenolic compound carrying an electron-donating group
    8.
    发明申请
    Process for functionalising a phenolic compound carrying an electron-donating group 审中-公开
    功能化携带电子给予基团的酚类化合物的方法

    公开(公告)号：US20070049773A1

    公开(公告)日：2007-03-01

    申请号：US11592930

    申请日：2006-11-03

    申请人： Charles Mioskowski ,  Alain Wagner ,  Nicolas Bensel ,  Virginie Pevere ,  Jean-Roger Desmurs

    发明人： Charles Mioskowski ,  Alain Wagner ,  Nicolas Bensel ,  Virginie Pevere ,  Jean-Roger Desmurs

    IPC分类号： C07C39/24 ,  C07C39/34 ,  C07C45/90

    CPC分类号： C07C45/46 ,  C07C45/565 ,  C07C231/12 ,  C07C231/14 ,  C07C303/28 ,  C07C303/30 ,  C07C233/18 ,  C07C309/66 ,  C07C49/84 ,  C07C47/575

    摘要： The invention concerns a method for functionalizing a phenolic compound bearing an electron-donor group, in said group para position, inter alia a method for the amidoalkylation of a phenolic compound bearing an electron-donor group, and more particularly, a phenolic compound bearing an electron-donor group preferably, in the hydroxyl group ortho position. The method for functionalizing in para position with respect to an electron-donor group carried by a phenolic compound is characterised in that the phenolic compound bearing an electron-donor group is subjected to the following steps: a first step which consists of protecting the hydroxyl group in the form of a sulphonic ester function; a second step which consists in reacting the protected phenolic compound with an electrophilic reagent; optionally, a third step deprotecting the hydroxyl group.

    摘要翻译： 本发明涉及一种用于官能化带有电子给体基团的酚类化合物的方法，尤其是具有电子给体基团的酚类化合物的酰胺基烷基化方法，更具体地说，涉及带有 电子给体基团优选在羟基邻位。 相对于由酚类化合物携带的电子给体基团在对位官能化的方法的特征在于具有电子给体基团的酚类化合物经受以下步骤：第一步，其保护羟基 呈磺酸酯官能团的形式; 第二步是使受保护的酚类化合物与亲电试剂反应; 任选地，第三步骤使羟基脱保护。

    Method for the synthesis of 4-hydroxyisoleucine and the derivatives thereof
    9.
    发明授权
    Method for the synthesis of 4-hydroxyisoleucine and the derivatives thereof 失效

    公开(公告)号：US07326805B2

    公开(公告)日：2008-02-05

    申请号：US10555875

    申请日：2004-05-07

    申请人： Charles Mioskowski ,  Cédric Catala ,  Alain Wagner

    发明人： Charles Mioskowski ,  Cédric Catala ,  Alain Wagner

    IPC分类号： C07C229/00

    CPC分类号： C07C227/30 ,  C07B2200/07 ,  C07C227/16

    摘要： The invention relates to a method for the synthesis of two isomers, at function OH, alone or in mixtures, of amino acids α or the derivatives thereof, having general formula (B), wherein: linkage C—O of the 4-position carbon (represented by symbol) denotes one or other of isomers III or IV, or mixtures thereof. Moreover, R1 and R2 represent: a hydrogen atom; or either R1 or R2 represents a hydrogen atom and the other substituent is a radical Ra, an acyl group —CORa, such as acetyl, or a functional group —COORa, —SO2Ra, —N (Ra, Rb), Ra and Rb, which are identical or different, representing a C1-C12 linear or branched alkyl radical, optionally substituted, an aryl group with one or more aromatic rings and heterocycles, comprising between 5 and 8C, optionally substituted, or aralkyl, the alkyl substituent and the aryl group being as defined above; or R1 and R2 both represent a substituent as defined above. R3 represents a hydrogen atom or Ra and R4 has the significance of Ra. The invention is characterised in that it comprises: the isomerisation of a compound having formula (I), wherein R1, R2, Ra, R3 and R4 are as defined above, such as to produce a compound having formula (II); and the reduction of the carbonyl function thereof which, depending on the catalytic system employed and the formula (I) compound used, produces one of the isomers having general formula (III) or (IV) or a mixture thereof having formula (B). The invention can be used for the synthesis of (2S, 3R, 4S)-4-hydroxyisoleucine.