Process for Preparing Protected Amidines
    1.
    发明申请
    Process for Preparing Protected Amidines 审中-公开
    制备保护脒的方法

    公开(公告)号:US20080319206A1

    公开(公告)日:2008-12-25

    申请号:US11816998

    申请日:2006-02-22

    IPC分类号: C07D205/04 C07C257/10

    摘要: A process for preparing a protected amidine group of formula (I): wherein R6 represents, for example, C1-10 alkyl (optionally substituted), aryl, C1-3 alkylaryl or C1-3 alkyloxyaryl; which comprises reacting a nitrile containing compound with an oxyamine of formula (II): R6ONH2 wherein R6 is as defined above for (I); in the presence of a thio-keto activating agent of formula (III): HS—Ry, —C(O)-Z wherein Z is -(1-4C)alkyl, —OH, —O-(1-4C)alkyl, —SH, —S(1-4C)alkyl, —NH2, —NH(1-4C)alkyl or —N[(1-4C)alkyl]2; Ry is (1-2C)alkyl (optionally substituted); or Z and Ry are linked so as to form a 5- or 6-membered ring of formula (IV): wherein X is —CH2—, —O—, —NH— or —N(1-4C)alkyl; p is 1 or 2; m is 1 or 2 and Rz is independently selected from H, (1-4C)alkyl, halo and amino.

    摘要翻译: 制备式(I)的保护的脒基的方法:其中R 6表示例如C 1-10烷基(任选取代的),芳基,C 1-3烷基芳基或C 1-3烷氧基芳基; 其包括使含腈化合物与式(II)的氧胺反应:R6ONH2,其中R6如对于(I)所定义; 在式(III)的硫代酮活化剂存在下:HS-Ry,-C(O)-Z其中Z是 - (1-4C)烷基,-OH,-O-(1-4C)烷基 ,-SH,-S(1-4C)烷基,-NH 2,-NH(1-4C)烷基或-N [(1-4C)烷基] 2; Ry是(1-2C)烷基(任选取代的); 或Z和Ry连接形成式(Ⅳ)的5-或6-元环:其中X是-CH 2 - , - O - , - NH-或-N(1-4C)烷基; p为1或2; m为1或2,Rz独立地选自H,(1-4C)烷基,卤素和氨基。