Schinzer Dieter, Bourguet Erika, Ducki Sylvie
Chemisches Institut der Otto-von-Guericke-Universität, Universitätsplatz 2, 39106 Magdeburg, Germany.
Chemistry. 2004 Jul 5;10(13):3217-24. doi: 10.1002/chem.200400125.
The total synthesis of furano-epothilone D by a convergent route is reported. The key fragments are available on a large scale to provide sufficient material for biological evaluation. The approach involves a palladium-catalyzed coupling that generates a highly functionalized aldehyde which is connected in a stereoselective aldol reaction to yield the framework of furano-epothilone D. Finally, a macrolactonization provides furano-epothilone D.
报道了通过汇聚式路线全合成呋喃埃坡霉素D。关键片段可大规模制备,以提供足够的材料用于生物学评价。该方法涉及钯催化的偶联反应,生成一个高度官能化的醛,该醛在立体选择性羟醛反应中连接,以产生呋喃埃坡霉素D的骨架。最后,通过大环内酯化反应得到呋喃埃坡霉素D。