A simple and general synthesis of 4-oxo-4,5,6,7-tetrahydroindoles via a novel intramolecular 1,3-dipolar cycloaddition approach

Article abstract of DOI:10.1016/0040-4039(96)00426-1

A general synthesis of 4-keto-4,5,6,7-tetrahydroindoles 6-12 has been achieved in two steps using a new intramolecular 1,3-dipolar cycloaddition approach in moderate yields (45-60%). The potential of this methodology is demonstrated by the synthesis of a mitomycin skeleton (15) and a topoisomerase-1 inhibitor skeleton (17).