title: Synthesis of the spiroketal core of integramycin.
abstract: A concise synthetic strategy towards the spiroketal core of the HIV-integrase inhibitor integramycin (1) was developed. The required ketone precursor was efficiently constructed from two simple and easily accessible subunits by means of a hydrozirconation/copper catalyzed acylation reaction. The effects of different protecting groups on the spiroketalization step were also investigated.
authors.affiliation: Department of Medicinal Chemistry, Helmholtz Centre for Infection Research, Inhoffenstr. 7, 38124 Braunschweig, Germany.
authors.forename: Evgeny V
authors.initials: EV
authors.lastname: Prusov
keywords: anti-infectives; hydrozirconation; natural products; spiroketals; total synthesis