Golfomycin A, a Novel Designed Molecule with DNA‐Cleaving Properties and Antitumor Activity

Abstract

Retroaldol reaction, propargyl–allenyl isomerization, and [4 + 2] cycloaddition are the steps involved in the reaction of the title compound 1 with 1,8-diazabi-cyclo[5.4.0]undec-7-ene at room temperature in THF. The product 2, like 1, reacts readily with nucleophiles such as methyl thioglycolate. The biological activity of these compounds is presumably due to this reactivity.