公开(公告)号：US4564674A

公开(公告)日：1986-01-14

申请号：US662833

申请日：1984-10-19

申请人： Shiro Terashima ,  Yoshikazu Kimura ,  Michiyo Suzuki ,  Teruyo Matsumoto ,  Rumiko Abe

发明人： Shiro Terashima ,  Yoshikazu Kimura ,  Michiyo Suzuki ,  Teruyo Matsumoto ,  Rumiko Abe

IPC分类号： C07F7/18 ,  C07H15/252 ,  C07H15/24

CPC分类号： C07H15/252 ,  C07F7/1856

摘要： A process for producing an anthracycline derivative represented by the general formula: ##STR1## where R.sup.1 is an acyl group, each of X.sup.1 and X.sup.2 is a hydrogen atom, a methoxy group, a hydroxyl group, a halogen atom or a lower alkyl group, each of Y.sup.1 and Y.sup.2 is a hydrogen atom, an alkoxy group or a hydroxyl group, and Z is a hydrogen atom or a protected hydroxyl group, which comprises reacting an anthracyclinone derivative represented by the general formula: ##STR2## where R is a hydrogen atom or a trialkylsilyl group, and X.sup.1, X.sup.2, Y.sup.1, Y.sup.2 and Z are as defined above, with a 1-acyl-sugar derivative represented by the general formula: ##STR3## where R.sup.2 is an acyl group and R.sup.1 is as defined above, in the presence of a silyl sulfonic acid derivative represented by the general formula:R.sup.5 R.sup.4 R.sup.3 SiOSO.sub.2 A (IV)where each of R.sup.3, R.sup.4 and R.sup.5 is an alkyl group and A is an alkyl group, an aryl group, a polyfluoroalkyl group or a hydrogen atom.

摘要翻译： 一种制备由以下通式表示的蒽环衍生物的方法：其中R1是酰基，其中X1和X2分别是氢原子，甲氧基，羟基，卤原子或低级 烷基，Y 1和Y 2各自为氢原子，烷氧基或羟基，Z为氢原子或被保护的羟基，其包括使由通式（II）表示的蒽环腈衍生物： ）其中R是氢原子或三烷基甲硅烷基，X 1，X 2，Y 1，Y 2和Z如上所定义，与通式如下的1-酰基 - 糖衍生物反应：其中R 2为 在通式R5R4R3SiOSO2A（IV）表示的甲硅烷基磺酸衍生物存在下，酰基和R 1如上所定义，其中R3，R4和R5各自为烷基，A为烷基，芳基 基团，多氟烷基或氢原子。