Modular synthesis of polyene side chain analogues of the potent macrolide antibiotic etnangien by a flexible coupling strategy based on hetero-bis-metallated alkenes

An efficient procedure for the concise synthesis of hetero-bis-metallated alkenes as useful building blocks for the modular access to highly elaborate polyenesand stabilized analogues is reported. By applying these bifunctionalolefins in convergent Stille/Suzuki–Miyaura couplings, novel, carefully selected side chain analogues of the potent RNA polymeraseinhibitor etnangien were synthesized by a modular late stage coupling strategy and evaluated for antibacterial and antiproliferative activities.