科研之友
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摘要
4-Hydroxycoumarin has been directly benzylated at C-3 position with a good number of secondary benzylic alcohols using copper triflate catalyst (2 mol%) in toluene under reflux. The protocol provides an efficient, expedient and atom-economic access to warfarin and coumatetralyl analogues with potential anticoagulant activity. The protocol has been extended to benzylation of 4-hydroxy-1-methylquinolin-2(1H)-1-one, N-methylbarbiturate and some other active methylene compound; with remarkable success.
- 出版日期2012-4
