Rodeschini Vincent, Boiteau Jean-Guy, Van de Weghe Pierre, Tarnus Céline, Eustache Jacques
Laboratoire de Chimie Organique et Bioorganique Associé au CNRS, Université de Haute-Alsace, Ecole Nationale Supérieure de Chimie de Mulhouse, 3 rue Alfred Werner, F-68093 Mulhouse Cedex, France.
J Org Chem. 2004 Jan 23;69(2):357-73. doi: 10.1021/jo035065+.
The preparation of a series of new fumagillin-derived MetAP-2 inhibitors is described. The synthetic approach was designed so as to permit modification of the fumagillin backbone at sites inaccessible through semisynthesis or previously existing total syntheses. An Evans aldolization and a ring-closing metathesis allowed the preparation of a pivotal intermediate which could then be functionalized in various ways using already established or newly developed methodologies.
本文描述了一系列新的烟曲霉素衍生的甲硫氨酸氨肽酶-2（MetAP-2）抑制剂的制备。设计的合成方法能够对烟曲霉素骨架进行修饰，这些修饰位点是通过半合成或先前已有的全合成方法无法实现的。埃文斯羟醛缩合反应和关环复分解反应使得制备一种关键中间体成为可能，然后可以使用已有的或新开发的方法以各种方式对该中间体进行官能团化。
