A convenient method for the synthesis of α-carboxylate ester bromolactones via bromolactonization of alkenoic diesters

Abstract

We developed a simple and efficient method to construct a variety of α-ester bromolactones in good to excellent yields with high diastereoselectivies. The protocol uses readily prepared malonate ester derivatives as substrates, water as an additive and inexpensive N-bromosuccinimide as the halogen source; no catalyst or toxic additive is required. The resulting substituted bromolactones are the fundamental units of many useful molecules.