【药物名称】
化学结构式(Chemical Structure):
参考文献No.561084
标题:Potent estrogenic agonists bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore
作者:Endo, Y.; Iijima, T.; Yamakoshi, Y.; Yamaguchi, M.; Fukasawa, H.; Shudo, K.
来源:J Med Chem 1999,42(9),1501
合成路线图解说明:

1,12-Dicarba-closo-dodecaborane (I) was lithiated with n-butyllithium in 1,2-dimethoxyethane and subsequently converted to the C-copper(I) derivative (II) with cuprous chloride. Coupling of (II) with p-iodoanisole (III) in the presence of pyridine furnished the C-arylated compound (IV). This was converted to the C-methoxycarbonyl derivative (V) via formation of the corresponding lithiocarborane, and then treatment with methyl chloroformate. Reduction of the methyl ester group with LiAlH4 produced alcohol (VI). Finally, cleavage of the methyl ether by means of boron tribromide yielded the title compound.

参考文献No.561796
标题:Structure-activity of estrogenic agonists bearing dicarba-closo-dodecarbone. Effect of geometry and separation distance of hydroxyl groups at the ends of molecules
作者:Endo, Y.; Iijima, T.; Amakoshi, Y.; Kubo, A.; Itai, A.
来源:Bioorg Med Chem Lett 1999,9(23),3313
合成路线图解说明:

1,12-Dicarba-closo-dodecaborane (I) was lithiated with n-butyllithium in 1,2-dimethoxyethane and subsequently converted to the C-copper(I) derivative (II) with cuprous chloride. Coupling of (II) with p-iodoanisole (III) in the presence of pyridine furnished the C-arylated compound (IV). This was converted to the C-methoxycarbonyl derivative (V) via formation of the corresponding lithiocarborane, and then treatment with methyl chloroformate. Reduction of the methyl ester group with LiAlH4 produced alcohol (VI). Finally, cleavage of the methyl ether by means of boron tribromide yielded the title compound.

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