由蓝藻素B合成天然海鞘素（ET - 729、ET - 745、ET - 759B、ET - 736、ET - 637、ET - 594）
Synthesis of natural ecteinascidins (ET-729, ET-745, ET-759B, ET-736, ET-637, ET-594) from cyanosafracin B.
作者信息
Menchaca Roberto, Martínez Valentín, Rodríguez Alberto, Rodríguez Natividad, Flores María, Gallego Pilar, Manzanares Ignacio, Cuevas Carmen
机构信息
Pharma Mar, S. A. C/Avda de los Reyes, 1.P.I. La Mina-Norte. 28770 Colmenar Viejo, Madrid, Spain.
出版信息
J Org Chem. 2003 Nov 14;68(23):8859-66. doi: 10.1021/jo034547i.
The semisynthetic process initially described for the synthesis of 1 (ET-743) has been extended to the preparation of other natural ecteinascidins. For the synthesis of 2 (ET-729) a demethylation of a N-Me intermediate was carried out by a selective oxidation with MCPBA. Other natural ecteinascidins (ET-745, ET-759B, ET-736, ET-637, ET-594) were accessible from key intermediate 25. The described methodologies allow for the preparation of a wide variety of ecteinascidins by procedures that can be easily scaled up.
最初描述的用于合成1（ET-743）的半合成过程已扩展至其他天然海鞘素的制备。对于2（ET-729）的合成，通过用间氯过氧苯甲酸（MCPBA）进行选择性氧化实现了N-甲基中间体的脱甲基反应。其他天然海鞘素（ET-745、ET-759B、ET-736、ET-637、ET-594）可从关键中间体25制得。所描述的方法能够通过易于放大规模的程序制备多种海鞘素。
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