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XIAO Qiong, LIU Chang, YIN Dali. Synthesis of a new metabolite of buagarofuran(AF-5)[J]. Journal of China Pharmaceutical University, 2016, 47(6): 673-677. DOI: 10.11665/j.issn.1000-5048.20160607
Citation: XIAO Qiong, LIU Chang, YIN Dali. Synthesis of a new metabolite of buagarofuran(AF-5)[J]. Journal of China Pharmaceutical University, 2016, 47(6): 673-677. DOI: 10.11665/j.issn.1000-5048.20160607
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Synthesis of a new metabolite of buagarofuran(AF-5)

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  • It has been reported that buagarofuran(AF-5)as an anxiolytic drug. It possesses a structural feature including α-agarofuran and the n-butyl side chain. Recently, there is a new metabolite found in clinical study, which is hypothesized that the n-butyl side chain has been oxidized to carboxylic acid. In order to confirm its structure, the target compound was prepared from(4aR, 7R, 8aR)-8a-hydroxy-7-(2-hydroxypropan-2-yl)-4a-methyloctahydronaphthalen-2(1H)-one in a six-step reaction with an overall yield of 16. 7%. The structure is confirmed by NMR and MS.
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    • References (8)
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