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    METHOD AND INTERMEDIATES FOR THE SYNTHESIS OF KORUPENSAMINES
    4.
    发明申请
    METHOD AND INTERMEDIATES FOR THE SYNTHESIS OF KORUPENSAMINES 审中-公开
    用于合成KORUPENSAMINES的方法和中间体

    公开(公告)号：WO1996015111A1

    公开(公告)日：1996-05-23

    申请号：PCT/US1995014896

    申请日：1995-11-13

    Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTA

    Inventor： REGENTS OF THE UNIVERSITY OF MINNESOTA ,  HOYE, Thomas, R.

    IPC: C07D217/24

    CPC classification number: C07C43/23 ,  C07C43/225 ,  C07C43/315 ,  C07C309/65 ,  C07D217/02 ,  C07D217/04 ,  C07F5/025 ,  C07F7/1804 ,  Y02P20/55

    Abstract: A method of preparing a korupensamine or an analog thereof comprising: (a) reacting a compound of formula (III), wherein each of R and R is CH3 or H, X is I, Y is (C1-C4)alkyl, benzyl or CHO, and each of R and R is (C1-C4)alkyl, benzyl, (C2-C5)acyl or an acid-labile hydroxy protecting group; with a compound of formula (IV), wherein R is benzyl, (C2-C5)acyl or an acid-labile hydroxy protecting group, R is B(OH)2, and R is (C1-C4)alkyl; in the presence of a Pd(0) catalyst and an inorganic base in an organic solvent, to yield a compound of formula (V), wherein Y, R , R , R , R , R and R are as defined above for compounds of formula (III) and (IV). Additionally the intermediates of formula (III), wherein X is Br, Cl or I, Y is H, (C1-C4)alkyl, benzyl, or CHO, each of R and R 3 is a protecting group selected from the group consisting of (C1-C4)alkyl, benzyl, (C2-C5)acyl and an acid-labile hydroxy protecting group; and R is H or (C2-C5)acyl; or wherein X is Br, Cl or I, Y is H, (C1-C4)alkyl, benzyl, or CHO, each of R and R is H or CH5, R is H or (C2-C5)acyl and R is a protecting group selected from the group consisting of (C1-C4)alkyl, benzyl, (C2-C5)acyl and an acid-labile hydroxy protecting group; and the intermediates of formula (IV), wherein R is Cl, Br, I, B(OH)2, an anhydride or ester of B(OH)2, or OSO2R , wherein R is (C1-C4)perfluoroalkyl, and each of R and R is H, (C1-C4)alkyl, benzyl, (C2-C5)acyl or an acid-labile hydroxy protecting group.

    Abstract translation: 一种制备高甘露聚糖或其类似物的方法，包括：（a）使式（III）化合物与其中R 1和R 2各自为CH 3或H的化合物反应，X为I，Y为（C1- C4）烷基，苄基或CHO，R 3和R 4各自为（C 1 -C 4）烷基，苄基，（C 2 -C 5）酰基或酸不稳定羟基保护基; 与式（IV）化合物反应，其中R 5为苄基，（C 2 -C 5）酰基或酸不稳定羟基保护基，R 6为B（OH）2，R 7为（ C1-C4）烷基; 在Pd（0）催化剂和无机碱存在下，在有机溶剂中，得到式（Ⅴ）化合物，其中Y，R 1，R 2，R 3，R 4 >，R 5和R 7如上文对式（III）和（IV）化合物所定义。 另外，式（III）的中间体，其中X是Br，Cl或I，Y是H，（C1-C4）烷基，苄基或CHO，R 1和R 2各自为H或CH 3 <，R 3>是选自（C 1 -C 4）烷基，苄基，（C 2 -C 5）酰基和酸不稳定羟基保护基的保护基; 和R 4是H或（C 2 -C 5）酰基; 或其中X是Br，Cl或I，Y是H，（C1-C4）烷基，苄基或CHO，R 1和R 2各自是H或CH 5，R 3是H或（ C 2 -C 5）酰基和R 4是选自（C 1 -C 4）烷基，苄基，（C 2 -C 5）酰基和酸不稳定羟基保护基的保护基; 和式（Ⅳ）的中间体，其中R 6是Cl，Br，I，B（OH）2，B（OH）2的酸酐或酯或OSO 2 R 9，其中R 9是 （C 1 -C 4）全氟烷基，R 5和R 7各自为H，（C 1 -C 4）烷基，苄基，（C 2 -C 5）酰基或酸不稳定羟基保护基。

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