Diethyl 3-oxocyclobutylphosphonate (5) has been synthesised via a novel one-pot cyclisation reaction of the α-phenylsulphonyl-γ, δ-epoxyphosphonate 8. Addition of 5-lithio-1- trityl-1, 2, 4-triazole to ketone 5 and deprotection then afforded cis-3-hydroxy-3-(1, 2, 4- triazol-3-yl) cyclobutylphosphonic acid (cis-4) which showed modest in vitro inhibition of the enzyme imidazole glycerol phosphate dehydratase. In an attempt to obtain the ...
