[reaction: see text] An efficient one-step synthesis of 2,4-diazabicyclo[4.2.0]octa-1(6),2-dien-5-ones 3 from methyl 2-chloro-2-cyclopropylideneacetate (1) and amidines 2a-c as well as N,N-dimethylguanidine (2d) is described. Similar to the benzocyclobutenes, the cyclobutene-annelated pyrimidones 3 undergo thermal ring opening and the resulting o-quinodimethane analogues readily cycloadd dienophiles to yield tetrahydroquinazolone derivatives.
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