【药物名称】
化学结构式(Chemical Structure):
参考文献No.476326
标题:4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity
作者:Krause, M.; Ligneau, X.; Stark, H.; Garbarg, M.; Schwartz, J.C.; Schunack, W.
来源:J Med Chem 1998,41(21),4171
合成路线图解说明:

4-Iodophenol (I) was protected as the trimethylsilyl ether (II) with Me3SiCl and then coupled with (trimethylsilyl)acetylene (III) using palladium catalyst and CuI to afford the O-desilylated ethynylphenol (IV). This was condensed under Mitsunobu conditions with N-Boc-imidazolylpropanol (VI), prepared from imidazolylpropanol (V) and Boc2O, to afford ether (VII). Deprotection of the Boc group of (VII) with methanolic hydrazine at r.t. yielded a mixture of (VIII) and the fully desilylated analogue (IX), which was isolated by column chromatography and finally crystallized as the maleate salt from EtOH-Et2O.

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