Method for synthesizing C-glycosides of ulosonic acids
    3.
    发明授权
    Method for synthesizing C-glycosides of ulosonic acids 失效
    尿苷酸的C-糖苷的合成方法

    公开(公告)号:US06376662B1

    公开(公告)日:2002-04-23

    申请号:US09142937

    申请日:1998-11-17

    IPC分类号: C07H704

    摘要: A method for synthesizing C-glycosides of ulosonic acids such as Neu5Ac, by which diastereocontrolled synthesis of &agr;-C-glycosides of ulosonic acids is attained is disclosed. In the method of the present invention, an ulosonic acid sulfone or phosphite is reacted with an aldehyde or ketone compound in the presence of a lanthanide metal halide.

    摘要翻译: 公开了用于合成诸如Neu5Ac的尿苷酸的C-糖苷的方法,通过该方法获得了关于酸性盐酸的α-C-糖苷的非对映控制合成。 在本发明的方法中,在镧系元素金属卤化物的存在下,将脲二
    酸砜或亚磷酸酯与醛或酮化合物反应。

    Aziridinyl-epothilone compounds
    5.
    发明授权
    Aziridinyl-epothilone compounds 有权
    氮丙啶基 - 埃坡霉素化合物

    公开(公告)号:US07872145B2

    公开(公告)日:2011-01-18

    申请号:US11753785

    申请日:2007-05-25

    IPC分类号: C07D277/22 C07D203/26

    摘要: The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m—Z—wherein Z is —(CHR10)—, —C(═O)—, —C(═O)—C(═O)—, —OC(═O)—, —N(R11)C(═O)—, —SO2—, or —N(R11)SO2—; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together to form a double bond; R2, R3, and R5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2 and R3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl; and R13 is aryl, substituted aryl, heteroaryl or substituted heteroaryl.

    摘要翻译: 本发明涉及如本文进一步描述的氮杂环丙烷基埃坡霉素化合物和/或其药学上可接受的盐和/或溶剂合物,其具有下式:其中K是-O - , - S-或-NR 7 - ; A是 - (CR 8 R 9) - (CH 2)m-Z-,其中Z是 - (CHR 10) - , - C(= O) - , - C(= O)-C(= O) - , - OC ) - , - N(R 11)C(= O) - , - SO 2 - 或-N(R 11)SO 2 - ; B1是羟基或氰基,R1是氢或B1和R1一起形成双键; R2,R3和R5独立地是氢,烷基,取代的烷基,芳基或取代的芳基; 或者R 2和R 3可以与它们所连接的碳一起形成任选取代的环烷基; R4是氢,烷基,烯基,取代的烷基,取代的烯基,芳基或取代的芳基; R6是氢,烷基或取代的烷基; R7,R8,R9,R10,R11和R12独立地是氢,烷基,取代的烷基,环烷基,取代的环烷基,芳基,取代的芳基,杂环烷基,取代的杂环烷基,杂芳基或取代的杂芳基; 并且R 13是芳基,取代的芳基,杂芳基或取代的杂芳基。