首页>
外国专利>
METHODS FOR THE TOTAL CHEMICAL SYNTHESIS OF ENANTIOMERICALLY-PURE 7-(2'-TRIMETHYLSILYL) ETHYL CAMPTOTHECIN
METHODS FOR THE TOTAL CHEMICAL SYNTHESIS OF ENANTIOMERICALLY-PURE 7-(2'-TRIMETHYLSILYL) ETHYL CAMPTOTHECIN
展开▼
机译:全化学合成对映体纯的7-(2'-三甲基甲硅烷基)乙基喜树碱的方法
展开▼
页面导航
摘要
著录项
相似文献
摘要
The present invention discloses and claims five (5) novel, highly efficient synthetic routes for the total synthesis of enantiomerically-pure (i.e., 99%) 7-(2-trimethylsilyl)ethyl camptothecin (BNP1350; Karenitecin; Cositecan). These aforementioned synthetic schemes are the first to disclose the total syntheses of 7-(2-trimethylsilyl)ethyl camptothecin using a highly novel direct, non-linear and convergent synthetic strategy which involves annealing the key C7-(trimethylsilyl)ethyl side chain-bearing A ring key synthons to an enantiomerically-pure tricyclic pyridone; rather than through the conventional methodology which incorporates the C7-(trimethylsilyl)ethyl side chain as the final synthetic step on a totally synthesized camptothecin parent compound. The current novel synthetic approaches reported herein since utilize desirably functionalized A-ring with preinstalled trimethyl silyl ethyl side chain, the aforementioned synthetic methodologies have a wider scope of making wide range of pharmaceutically relevant A-ring substituted BNP1350 analogs by substituting desirably functionalized nitro or protected amino phenyl carboxy A-ring as the starting material.
展开▼