Total synthesis and antitumor activity of ZK??EPO: the first fully synthetic epothilone in clinical development

…, B Buchmann, W Schwede, W Skuballa…

Index: Klar, Ulrich; Buchmann, Bernd; Schwede, Wolfgang; Skuballa, Werner; Hoffmann, Jens; Lichtner, Rosemarie B. Angewandte Chemie - International Edition, 2006 , vol. 45, # 47 p. 7942 - 7948

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Citation Number: 121

Abstract

We applied a highly convergent strategy based on our lead-optimization program that offered good flexibility for introducing structural modifications at nearly every position of the 16-membered-ring skeleton. This strategy is reflected in our synthetic route to ZK-EPO (Scheme 2) where we applied a Wittig reaction to connect C12 and C13, an aldol reaction [10, 11] to establish stereocenters C6 and C7, and finally a Yamaguchi cyclization for ...