【药物名称】PD-166309
化学结构式(Chemical Structure):
参考文献No.541841
标题:Butenolide endothelin antagonists with improved aqueous solubility
作者:Patt, W.C.; Cheng, X.-M.; Repine, J.T.; Lee, C.; Reisdorph, B.R.; Massa, M.A.; Doherty, A.M.; Welch, K.M.; Bryant, J.W.; Flynn, M.A.; Walker, D.M.; Schroeder, R.L.; Haleen, S.J.; Keiser, J.A.
来源:J Med Chem 1999,42(12),2162
合成路线图解说明:

Aldol condensation of piperonal (I) with 4-methoxyacetophenone (II) afforded chalcone (III). Subsequent addition of KCN to (III) in the presence of AcOH gave nitrile (IV), which was hydrolyzed in methanol in the presence of p-TsOH to provide ketoester (V). Subsequent base-catalyzed condensation of (V) with aldehyde (VI), followed by cyclization in refluxing AcOH furnished the target butenolide.

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