Total synthesis of dolastatin 10 through ruthenium-catalyzed asymmetric hydrogenations
Total synthesis of dolastatin 10 through ruthenium-catalyzed asymmetric hydrogenations
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DOI：
10.1016/j.tet.2007.03.036
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发表时间：
2007-07-02
期刊：
影响因子：
2.1
通讯作者：
Genet, Jean-Pierre
中科院分区：
文献类型：
--
作者：
Mordant, Celine;Reymond, Sebastien;Genet, Jean-Pierre
报道了一种有效的微管组装抑制剂dolastatin 10的全合成，其具有显著的抗肿瘤活性。我们的合成方法是基于钌促进的(S)- boc -脯氨酸和(S)- boc -异亮氨酸衍生的β -酮酯的不对称氢化，构建两个关键单元：(2R,3R)- boc -美元异亮氨酸（Dap）和(3R)- boc -美元异亮氨酸（Dil）。(c) 2007 Elsevier Ltd.版权所有。
A total synthesis of dolastatin 10, a potent inhibitor of microtubule assembly, which displayed remarkable antineoplastic activity, is reported. Our synthetic approach was based upon ruthenium-promoted asymmetric hydrogenation of beta-keto esters derived from (S)-Boc-proline and (S)-Boc-isoleucine for the construction of the two key units: (2R,3R)-Boc-dolaproine (Dap) and (3R)-Boc-dolaisoleucine (Dil). (c) 2007 Elsevier Ltd. All rights reserved.