PD-158143

Chemical Name: 4,4'-(1-Methyl-4,4-diphenylbutylidene)bis[2-(perhydroazepin-1-ylmethyl)phenol] dioxalate
项目整合开发状态: Biological Testing
项目研究机构: Neurex (Originator), Pfizer (Originator)
合成路线:The esterification of 4,4-bis(4-hydroxyphenyl)pentanoic acid (I) with diazomethane in ethyl ether/methanol gives the methyl ester (II),which is treated with phenylmagnesium bromide in THF to yield 4,4-bis(4-hydroxyphenyl)-1,1-diphenyl-1-pentanol (III).The reduction of (III) with H2 over Pd/C in methanol affords 4,4-bis(4-hydroxyphenyl)-1,1-diphenylpentane (IV),which is finally condensed with azepane (V) and formaldehyde in hot ethanol/water.
📌 参考资料/链接:
参考文献标题:Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers
文献作者:Schelkun,R.M.; Yuen,P.; Malone,T.C.; Rock,D.M.; Stoehr,S.; Szoke,B.; Tarczy-Hornoch,K.
参考来源:Bioorg Med Chem Lett 1999,9(16),2447