A practical synthesis of highly hindered biphenyl-2-carboxylates via nucleophilic aromatic substitution of tert-butyl 2-methoxybenzoates with aryl Grignard reagent

被引:10
作者
Aki, S [1 ]
Haraguchi, Y [1 ]
Sakikawa, H [1 ]
Ishigami, M [1 ]
Fujioka, T [1 ]
Furuta, T [1 ]
Minamikawa, J [1 ]
机构
[1] Otsuka Pharmaceut Co Ltd, Tokushima Factory 2, Synth Lab, Tokushima 7710182, Japan
关键词
D O I
10.1021/op0001279
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
The fluorenone derivative (OPC-34165) has potent repairing and protecting activities for peripheral and central nervous system degeneration. A synthesis of the biphenyl-2-carboxylic acid derivative, which is the key intermediate of OPC-34165, is described employing the SNAr reaction of tert-butyl 2-methoxybenzoate with aryl Grignard reagent in refluxing THF-toluene.
引用
收藏
页码:535 / 538
页数:4
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