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    COMBINATORIAL APPROACH TO CHIRAL REAGENTS OR CATALYSTS HAVING AMINE OR AMINO ALCOHOL LIGANDS
    2.
    发明申请
    COMBINATORIAL APPROACH TO CHIRAL REAGENTS OR CATALYSTS HAVING AMINE OR AMINO ALCOHOL LIGANDS 审中-公开
    具有胺或氨基醇配体的CHIRAL试剂或催化剂的组合方法

    公开(公告)号：WO00024510A1

    公开(公告)日：2000-05-04

    申请号：PCT/US1999/024967

    申请日：1999-10-22

    IPC分类号： B01J31/18 ,  B01J31/22 ,  C07B53/00 ,  C07C215/28 ,  C07C215/30 ,  C07C215/50 ,  C07C229/36 ,  C07D307/52 ,  C07K5/062 ,  C40B30/08 ,  C40B40/18 ,  B01J31/00 ,  B01J31/14 ,  B01J31/28 ,  B01J31/32 ,  B01J31/34 ,  B01J31/36 ,  B01J31/38

    CPC分类号： B01J31/2243 ,  B01J31/1805 ,  B01J31/223 ,  B01J2219/00738 ,  B01J2219/00745 ,  B01J2219/00747 ,  B01J2531/10 ,  B01J2531/20 ,  B01J2531/30 ,  B01J2531/40 ,  B01J2531/82 ,  B01J2531/84 ,  C07B53/00 ,  C07B2200/07 ,  C07C215/28 ,  C07C215/30 ,  C07C215/50 ,  C07C229/36 ,  C07D307/52 ,  C07K5/06026 ,  C40B30/08 ,  C40B40/18

    摘要： Functionalized amine derivatives are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions. Organoboronic acids (4) react with amines (2) and alpha-hydroxy aldehydes (3) to give anti-alpha-amino alcohols (1) with very high diastereoselectivities (> 99 % de). When optically pure alpha-hydroxy aldehydes are used in this process, no racemization occurs and the products are obtained with very high enantioselectivities (> 99 % ee). The reaction also works with unprotected glyceraldehyde to give the corresponding amino diol derivatives, while unprotected carbohydrates give the corresponding amino polyols. The chiral amino alcohol products of this process or their derivatives, react further with metals or non-metals to give adducts that are effective catalysts for a variety of asymmetric reactions. Overall, the present invention relies on the facile synthesis of the chiral amino alcohol ligands for the rapid construction of combinatorial libraries of chiral catalysts. These libraries can then be used to identify the most suitable catalyst for a particular asymmetric transformation.

    摘要翻译： 通过在温和条件下使胺，羰基衍生物和有机硼化合物反应来制备官能化胺衍生物。 有机硼酸（4）与胺（2）和α-羟基醛（3）反应，得到具有非常高的非对映选择性（> 99％de）的抗α-氨基醇（1）。 当在该方法中使用光学纯的α-羟基醛时，不会发生外消旋化，并且以非常高的对映选择性（> 99％ee）获得产物。 该反应也适用于未保护的甘油醛，得到相应的氨基二醇衍生物，而未保护的碳水化合物则得到相应的氨基多元醇。 该方法的手性氨基醇产物或其衍生物进一步与金属或非金属反应，得到作为各种不对称反应的有效催化剂的加合物。 总之，本发明依赖于手性氨基醇配体的容易合成，用于快速构建手性催化剂组合文库。 然后可以使用这些文库来识别用于特定不对称转化的最合适的催化剂。

    GROUP 5 METAL COMPLEXES USEFUL FOR AMINE FUNCTIONALIZATION AND SYNTHETIC PROCESS FOR MANUFACTURE THEREOF
    6.
    发明申请
    GROUP 5 METAL COMPLEXES USEFUL FOR AMINE FUNCTIONALIZATION AND SYNTHETIC PROCESS FOR MANUFACTURE THEREOF 审中-公开
    用于胺功能化的第5组金属络合物及其制备的合成方法

    公开(公告)号：WO2012040853A1

    公开(公告)日：2012-04-05

    申请号：PCT/CA2011/050609

    申请日：2011-09-28

    申请人： THE UNIVERSITY OF BRITISH COLUMBIA ,  SCHAFER, Laurel L. ,  LAUZON, Jean Michel P. ,  AYINLA, Rashidat O. ,  EISENBERGER, Patrick

    发明人： SCHAFER, Laurel L. ,  LAUZON, Jean Michel P. ,  AYINLA, Rashidat O. ,  EISENBERGER, Patrick

    IPC分类号： C07C217/76 ,  C07B37/00 ,  C07B43/04 ,  C07C217/48 ,  C07C227/00 ,  C07C227/32 ,  C07F9/00 ,  B01J31/36

    CPC分类号： C07F9/005 ,  B01J31/1805 ,  B01J31/2217 ,  B01J2231/32 ,  B01J2531/58 ,  C07B37/02 ,  C07B2200/07 ,  C07C209/68 ,  C07C213/08 ,  C07C233/07 ,  C07C233/58 ,  C07C233/65 ,  C07C303/38 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/42 ,  C07D211/96 ,  C07D215/06 ,  C07D265/30 ,  C07D279/12 ,  C07D491/10 ,  C07C211/48 ,  C07C217/84 ,  C07C311/16

    摘要： The present invention provides Group 5 metal complexes useful for amine functionalization and synthetic process for manufacture thereof. Provided in this application are halo group 5 metal-amidate complexes having the structure of Formula I: I wherein: M is a group 5 metal, such as Ta, Nb or V; X is a halo substituent, such as CI, F, I or Br; n = 1 or 2,; s = 1 or 2; R 1 and R 2 are each independently H; a C 1 - C 25 substituted or unsubstituted, linear, branched or cyclic alkyl; or substituted or unsubstituted aryl or heterocyclic groups; R' is independently a C 1 - C 25 substituted or unsubstituted, linear, branched or cyclic alkyl; a substituted or unsubstituted aryl; a substituted or unsubstituted heterocyclic group; or NR 3 2 ; and each R 3 is independently a C 1 - C 25 substituted or unsubstituted, linear, branched or cyclic alkyl; a substituted or unsubstituted aryl; or substituted or unsubstituted heterocyclic group, and a process for synthesis thereof. Also provided are the corresponding metallaaziridine complexes. The metal complex of Formula I, and the corresponding metallaaziridine complex are useful as a catalysts in ct-alkylation of secondary amines and, therefore, also provided are methods of using the metal complex of Formula I, and the corresponding metallaaziridine complex in o-alkylation of secondary amines. This application also provides methods of using the corresponding non-halo group 5 metal-amidate complexes and metallaaziridine complexes in α-alkylation of heterocycles.

    摘要翻译： 本发明提供了可用于胺官能化的第5族金属络合物及其制造方法。 本申请中提供了具有式I结构的卤代基5金属 - 酰胺化物络合物：其中：M是第5族金属，如Ta，Nb或V; X是卤素取代基，例如Cl，F，I或Br; n = 1或2 s = 1或2; R1和R2各自独立地为H; C1-C25取代或未取代的直链，支链或环状烷基; 或取代或未取代的芳基或杂环基; R'独立地为C 1 -C 25取代或未取代的直链，支链或环状烷基; 取代或未取代的芳基; 取代或未取代的杂环基; 或NR3 2 并且每个R 3独立地为C 1 -C 25取代或未取代的直链，支链或环状烷基; 取代或未取代的芳基; 或取代或未取代的杂环基，及其合成方法。 还提供了相应的喹唑啉复合物。 式I的金属络合物和相应的金氮idine啶络合物可用作仲胺烷基化中的催化剂，因此还提供了使用式I的金属络合物和相应的金属氮杂环丁烷络合物在邻烷基化中的方法 的仲胺。 本申请还提供了在杂环烷基化中使用相应的非卤代基团5金属 - 酰胺化物络合物和金属氮杂环丁烷配合物的方法。