Oxetin was first isolated in 1986 from Streptomyces sp. OM-2317. This beta-amino acid has been shown to inhibit Bacillus subtilis and Piricularia oryzae and is a known glutamine synthetase inhibitor.

Only two syntheses of oxetin have been previously reported. Our approach (Scheme 2) begins with natural amino acid L-serine and proceeds through 1,5-Dioxaspirohexane 17. In addition to completing the synthesis of oxetin, we plan to prepare analogs that have improved antibacterial and pesticidal activities.