Total synthesis of cytostatin

The total synthesis of cytostatin, an antitumor agent belonging to the fostriecin family of natural products, is disclosed. The convergent route features a key epoxide opening reaction to join the two stereotriad units and a single-step late stage, stereoselective installation of the sensitive triene through a β-chelation controlled nucleophilic addition. The synthesis provides rapid access to the C4-C6 and C 10-C 11 stereoisomers of cytostatin and additional analogues to define the substituent role in PP2A binding.