A Domino N-Amidoacylation/Aldol-Type Condensation Approach to the Synthesis of the Topo-I Inhibitor Rosettacin and Derivatives

详细信息    查看全文

• 作者：Fr&eacute ; d&eacute ; ric Pin ; S&eacute ; bastien Comesse ; Morgane Sanselme ; Adam Daï ; ch
• 刊名：Journal of Organic Chemistry
• 出版年：2008
• 出版时间：March 7, 2008
• 年：2008
• 卷：73
• 期：5
• 页码：1975 - 1978
• 全文大小：155K
• 年卷期：v.73,no.5(March 7, 2008)
• ISSN：1520-6904

文摘

journals/joceah/73/i05/figures/jo702387qn00001.gif" ALIGN="left" HSPACE=5>

The pot, atom, and step-economic synthesis of Rosettacintopo-I poison and its derivatives has been achieved using anovel domino N-amidoacylation/aldol-type condensation,followed by decarboxylation of the ester function. The keydomino procedure simply involves mixing HOBt ester asnew reagent with lactam and NaH together in THF or THF/DMF. The reaction seems to be general and led to suitableN-heterocyclic products in moderate to good yields.