Divergent Access to Histone Deacetylase Inhibitory Cyclopeptides via Late- Stage Cyclopropane Ring Cleavage Strategy. Short Synthesis of Chlamydocin

11 July 2019, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


We present a unified step-economical strategy to access histone deacetylase inhibitory peptides, based on late-stage installation of zinc-binding functionalities via the cleavage of the strained cyclopropane ring in the common pluripotent cyclopropanol precursor. The efficacy of the proposed diversity-oriented approch has been validated by short stereoselective synthesis of a natural product chlamydocin and a number of its analogs.


amino acids
diversity-oriented synthesis
histone deacetylase
total synthesis


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