发明名称 Facile method for synthesizing baccatin III compounds
摘要 A process for synthesizing a C-7 protected baccatin III compound represented by formula (A), which comprises reacting a 10-deacetylbaccatin III compound represented by formula (B) with a protecting agent and an acylating agent in the presence of a secondary amine and a nitrogen-containing compound. Also, a process for synthesizing a C-7 protected 10-deacetylbaccatin III compound represented by formula (C), which comprises reacting a 10-deacetylbaccatin III compound represented by formula (B) with a protecting agent in the presence of a secondary amine and a nitrogen-containing compound. In both processes the nitrogen-containing compound is selected from a nitrogen-containing heterocycle or a trialkylamine. When the nitrogen-containing heterocycle is selected, it may be an unsubstituted or a substituted pyridine or an unsubstituted or a substituted pyrazine. When a trialkylamine is selected, it may be, for example, triethylamine or diisopropylethylamine. wherein PG<SUB>1 </SUB>represents the organic residue of the protecting agent, PG<SUB>2 </SUB>represents the organic residue of the acylating agent, and R represents a simple or substituted aryl group or a heterocyclic group.
申请公布号 US2005256323(A1) 申请公布日期 2005.11.17
申请号 US20050127234 申请日期 2005.05.12
申请人 IMMUNOGEN, INC. 发明人 BALOGLU ERKAN
分类号 C07D305/14;C07F7/18;(IPC1-7):C07D35/14 主分类号 C07D305/14
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