【药物名称】Pirodavir, R-77975
化学结构式(Chemical Structure):
参考文献No.10727
标题:Novel pyridazinamine derivs
作者:Stokbroekx, R.A.; Van der Aa, M.J.M.; Luyckx, M.G.M.; Grauwels, G.A.J. (Janssen Pharmaceutica NV)
来源:AU 8825751; EP 0320032; JP 1989207278; US 4992433
合成路线图解说明:

The condensation of 2-(1-benzylpiperidin-4-yl)ethanol (I) with 4-hydroxybenzoic acid ethyl ester (II) by means of triphenylphosphine and diazenedicarboxylic acid diethyl ester in THF gives 4-[2-(1-benzylpiperidin-4-yl)ethoxy]benzoic acid ethyl ester (III) as fumarate salt. This compound is debenzylated by hydrogenation with H2 over Pd/C in ethanol, yielding the free product (IV), which is finally condensed with 3-chloro-6-methylpyridazine (V) by means of K2CO3 in DMF.

参考文献No.187983
标题:Pirodavir
作者:Casta馿r, J.; Prous, J.
来源:Drugs Fut 1992,17(11),997
合成路线图解说明:

The condensation of 2-(1-benzylpiperidin-4-yl)ethanol (I) with 4-hydroxybenzoic acid ethyl ester (II) by means of triphenylphosphine and diazenedicarboxylic acid diethyl ester in THF gives 4-[2-(1-benzylpiperidin-4-yl)ethoxy]benzoic acid ethyl ester (III) as fumarate salt. This compound is debenzylated by hydrogenation with H2 over Pd/C in ethanol, yielding the free product (IV), which is finally condensed with 3-chloro-6-methylpyridazine (V) by means of K2CO3 in DMF.

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