[2+2+2] Cycloadditions of siloxy alkynes with 1,2-diazines: from reaction discovery to identification of an antiglycolytic chemotype.

A newly uncovered Bronsted acid-promoted [2+2+2] cycloaddition between siloxy alkynes and 1,2-diazines produces novel polycyclic compounds with high efficiency and excellent diastereoselectivity under exceedingly mild conditions. A small-molecule library synthesized using this reaction yielded a novel chemotype, which inhibited glycolytic ATP production by blocking glucose uptake in CHO-K1 cells.