[摘要]：inhibitor cyclophostin were synthesized. The substitution reaction of phosphono allylic carbonate with Me acetoacetate gave the vinyl phosphonate. Attempted hydrogenation/debenzylation gave an unexpected enolether lactone. Alternatively, selective hydrogenation, demethylation, cyclization and debenzylation gave the phosphonate analog of cyclophostin as a separable mixt. of diastereomers I and II. The trans phosphonate isomer was more active than the cis isomer against AChE from two sources.
