Synthesis of antimicrotubule dibenzoxepines
Synthesis of antimicrotubule dibenzoxepines
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DOI：
10.1016/j.tetlet.2010.04.039
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发表时间：
2010-06-09
影响因子：
1.8
通讯作者：
Baudoin, Olivier
中科院分区：
文献类型：
--
作者：
Colombel, Virginie;Joncour, Agnes;Baudoin, Olivier
使用 Suzuki-Miyaura 偶联、格氏加成和环化脱水作为关键步骤，以简单的方式合成了 B 环和 C 环上带有各种取代基的新二苯并氧杂环己烷 5a-i。评估所有类似物的抗微管活性并与参考化合物进行比较。迄今为止，化合物 5d-f 显示出此类别秋水仙素的最高活性。 (C) 2010 Elsevier Ltd. 保留所有权利。
New dibenzoxepines 5a-i bearing various substituents on B- and C-rings were synthesized in a straightforward manner using a Suzuki-Miyaura coupling, a Grignard addition, and a cyclodehydration as key steps. The antimicrotubule activity of all analogues was evaluated and compared to reference compounds. Compounds 5d-f displayed the highest activity for this type of allocolchicinoids to date. (C) 2010 Elsevier Ltd. All rights reserved.