基本信息:
- 专利标题： 阿贝卡星及其中间体地贝卡星的合成新方法
- 专利标题（英）：New synthetic method of arbekacin and intermediate of dibekacin thereof
- 申请号：CN201110131544.8 申请日：2011-05-19
- 公开(公告)号：CN102786564A 公开(公告)日：2012-11-21
- 发明人： 乔仁忠 , 蔡岩 , 孙政军 , 吴柯 , 樊长莹 , 张金 , 张鹏
- 申请人： 北京化工大学 , 齐鲁天和惠世制药有限公司
- 申请人地址： 北京市朝阳区北三环东路15号
- 专利权人： 北京化工大学,齐鲁天和惠世制药有限公司
- 当前专利权人： 北京化工大学,齐鲁天和惠世制药有限公司
- 当前专利权人地址： 北京市朝阳区北三环东路15号
- 代理机构： 北京思海天达知识产权代理有限公司
- 代理人： 张燕慧
- 主分类号： C07H15/234
- IPC分类号： C07H15/234 ; C07H1/00
The invention relates to a new synthetic method of arbekacin and an intermediate of dibekacin thereof. The method adopts kanamycin B as an initial synthetic raw material; five amino groups of kanamycin B are protected by butoxycarbonyl; 4''-position and 6''-position hydroxyls are protected by aldol condensation; 3'-position and 2''-position hydroxyls are selectively acylated; a 4'-position hydroxyl is sulfonylated; then an epoxy structure is formed; the epoxy structure is treated by potassium n-butylxanthate to form double bonds; and catalytic hydrogenation is performed to obtain dibekacin; dibekacin is used as a raw material; all amino groups and hydroxyls of the dibekacin are protected by hexamethyl disilyamine; side chain connection of 1-position amino group is performed with synthetic active ester; the silyl protection is removed; and finally arbekacin is obtained by hydrazine hydrate hydrazinolysis. The synthetic method is simple in operation, high in yield, friendly for environment, low in production cost, and quite suitable for industrial production.
公开/授权文献:
- CN102786564B 阿贝卡星及其中间体地贝卡星的合成新方法 公开/授权日：2015-05-13
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07H | 糖类；及其衍生物；核苷；核苷酸；核酸 |
| ------C07H15/00 | 含有直接连在糖化物基团的杂原子上的烃基或取代烃基的化合物 |
| --------C07H15/20 | .碳环类 |
| ----------C07H15/22 | ..被氮原子取代的环己烷环 |
| ------------C07H15/222 | ...至少被两个氮原子取代的环己烷环 |
| --------------C07H15/226 | ....至少有两个糖化物基团直接连在环己烷环上 |
| ----------------C07H15/234 | .....连在环己烷环的非相邻环碳原子上，例如卡那霉素、托普霉素、暗霉素、庆大霉素A2 |