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Paper | Regular issue | Vol 63, No. 2, 2004, pp.271-282
Published online, 8th December, 2003
DOI: 10.3987/COM-03-9913
The Asymmetric Synthesis of Linear Dihydropyrano Coumarins for Alzheimer’s Disease

Shi Shun, Ling-Yi Kong,* Han-Qing Zhang, Shan-An He, and Masatake Niwa

*Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China

Abstract

Ca2+ antagonistic and acetylcholinesterase (AchE) inhibitory activity-guided cis-3’S, 4’S-disubstituted linear dihydropyranocoumarins were synthesized asymmetrically. The syntheses were performed with resorcinol or 2-methylresorcinol, enantioselectivity was chosen AD-mix-β to dihydroxylate asymmetrically. All products were screened against AchE in vitro and one showed potential inhibitory activity.