Total Asymmetric Synthesis of 3'R,4'R-Disubstituted Angular Dihydropyranocoumarins
- VernacularTitle:3'R,4'R-二取代角型吡喃香豆素的不对称合成
- Author:
Shi SUN
;
Lingyi KONG
;
Hanqing ZHANG
;
Shanan HE
- Publication Type:Journal Article
- Keywords:
3'R,4'R-Khellactone-type coumarin;
Asymmetrical dihydroxylation;
Alzheimer's disease;
Acetylcholinetsterase inhibitor;
Calcium antagonist
- From:
Journal of China Pharmaceutical University
2005;(3):205-209
- CountryChina
- Language:Chinese
-
Abstract:
AIM:To obtain new typical compounds with dual mechanism,antagonizing Ca2+and inhibiting acetylcholinesterase,on Alzheimer's disease.METHODS:Resorcinol was chosen as primitive substrate,and AD-mix-β as asymmetrically dihydroxylated reagent;all products were screened against acetylcholinesterase in vitro.RESULTS:cis-3′R,4′R-disubstituted angular dihydropyranocoumarins were synthesized enantioselectively,however,its inhibitory activity on acetylcholinesterase is distinctively lower than that of cis-3′R,4′R-disubstituted linear dihydropyranocoumarins.