Chen Kaixian

Synthesis and acetylcholinesterase inhibitory activity of (±)-14-fluorohuperzine A

Abstract The synthesis of (±)-14-Fluorohuperzine A has been accomplished and the ability of this agent to inhibit acetylcholinesterase has been measured. Taking into account its racemic form, this compound exhibits 62 times less potent activity than natural (−)-huperzine A.

Improved synthesis of rupintrivir

An improved synthesis of rupintrivir (AG7088) was accomplished using three amino acids (l-glutamic acid, d-4-fluorophenylalanine, and l-valine) as the building blocks. The key fragment ketomethylene dipeptide isostere was constructed with the valine derivative and phenylpropionic acid derivative, followed by coupling with a lactam derivative and an isoxazole acid chloride to provide AG7088 totally in eight steps.