Abstract

A synthetic strategy for natural (+)-FR900482 ( 1) was developed by featuring a convergent and enantioselective sequence which commences with 5-hydroxyisophthalic acid and L-diethyl tartrate. The proposed key intermediate 4 was synthesized starting from FK973, the triacetyl derivative of 1, and successful reconversion of 4 into 1 was also achieved. These preliminary studies definitely demonstrated that 4 is suitable as a potential relay compound toward 1 and that the crucial final sequence of reactions ( 4→1 ) involving delicate deprotection and oxidation steps can be realized.

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