Efficient Synthesis of Azaspirodienones by Microwave-Assisted Radical Spirocyclization of Xanthate-Containing Ugi Adducts

摘要

The sequential use of an Ugi reaction and radical spirocyclization under microwave irradiation conditions is described. The process provides rapid access to spirodienone lactams.In medicinal chemistry, the screening of small-molecule libraries is of great importance in drug discovery. In this regard, an important goal in organic synthesis continues to be the development of efficient synthetic technologies that provide rapid access to libraries of molecules with broad structural diversity. Success in establishing an efficient combination of different reactions can lead to the assembly of libraries of small molecules (e.g., combinatorial chemistry). The selection of efficient consecutive processes does, indeed, merit consideration as a viable alternative means to create libraries of molecules bearing a variety of functional groups and having broad structural diversity.