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Synthesis, resolution, and antiplatelet activity of 3-substituted 1(3H)-isobenzofuranone
Hua Yang1, Gao-Yun Hu, Jun Chen
1Research Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Central South University, Changsha 410013, PR China.
Abstract:
A series of 3-substituted-1(3H)-isobenzofuranone 6a-g and 7a-g were synthesized from phthalic anhydride. The compound 6a-g was resolved. The antiplatelet activities of these compounds were evaluated using in vitro experiment of platelet aggregation. The levels of antiplatelet activity were displayed as following sequence: l-isomer >dl-isomer>d-isomer, respectively. The alkylphthalide is more active than the corresponding alkenephthalide. All these compounds were less active than n-butylphthalide (NBP, 6c) and Aspirin (Asp).
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