Dr. Hutchison et al., A SIMPLE AND GENERAL-SYNTHESIS OF 4-OXO-4,5,6,7-TETRAHYDROINDOLES VIAA NOVEL INTRAMOLECULAR 1,3-DIPOLAR CYCLOADDITION APPROACH, Tetrahedron letters, 37(17), 1996, pp. 2887-2890
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 cycloaddi
tion approach in moderate yields (45-60%). The potential of this metho
dology is demonstrated by the synthesis of a mitomycin skeleton (15) a
nd a topoisomerase-1 inhibitor skeleton (17). (C) 1996 Elsevier Scienc
e Ltd