新产品编号:1126893
Chemical Name: 3-[3-Carboxy-2-methyl-1-[(E)-5,5,8,8-tetramethyl-5,6,7,8-tetrahydroanthracen-2-ylmethylene]-2(Z)-propenyl]benzoic acid; 4-(3-Carboxyphenyl)-3-methyl-5-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydroanthracen-2-yl)-2(Z),4(E)-pentadienoic acid
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-bromoanthracene (I) was lithiated with tert-butyllithium in THF at -78 C,and subsequently condensed with dimethylformamide to provide,after aqueous workup,aldehyde (II).This was condensed with butenoate (III) in the presence of potassium tert-butoxide in cold THF to give intermediate (IV),which by final addition of water experienced hydrolysis to the target dicarboxylic acid.
📌 参考资料/链接：
参考文献标题:Alicyclic phospholipase A2 inhibitors
文献作者:Bronson,J.J.; Carroll,F.I.; Greene,K.M.; Lewin,A.; Mansuri,M.M.; D'Andrea,S.V.(Bristol-Myers Squibb Co.)
参考来源:CA 2125802; EP 0629604; JP 1995017913; US 5436369
📄 详细内容
合成路线:5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-bromoanthracene (I) was lithiated with tert-butyllithium in THF at -78 C,and subsequently condensed with dimethylformamide to provide,after aqueous workup,aldehyde (II).This was condensed with butenoate (III) in the presence of potassium tert-butoxide in cold THF to give intermediate (IV),which by final addition of water experienced hydrolysis to the target dicarboxylic acid.
参考文献标题:Dicarboxylic acid inhibitors of phospholipase A2
文献作者:Springer,D.M.; et al.
参考来源:Bioorg Med Chem Lett 1997,7(7),793