【药物名称】
化学结构式(Chemical Structure):
参考文献No.30963
标题:Novel benzothiophene cpds. and methods
作者:Carlson, D.G.; Cullinan, G.J.; Fahey, K.J.; Jackson, W.T.; Roehm, N.W.; Spaethe, S.M. (Eli Lilly and Company)
来源:EP 0732331; JP 1999501932; WO 9628156
合成路线图解说明:

Alkylation of 3-methoxybenzenethiol (I) with 4'-methoxyphenacyl bromide (II) afforded sulfide (III). Cyclization of (III) with concomitant rearrangement in the presence of polyphosphoric acid produced a mixture of regioisomers (IV) and (V) that were separated by their different solubility in acetone. Then, Friedel-Crafts acylation of the desired insoluble isomer (IV) with 3,4,5-trimethoxybenzoyl chloride (VI) in the presence of AlCl3 provided the title ketone, which was separated from some demethylated byproduct by means of silica gel chromatography.

参考文献No.38763
标题:Anti-mitotic agents which inhibit tubulin polymerization
作者:Pinney, K.G. (Baylor University)
来源:US 5886025
合成路线图解说明:

Alkylation of 3-methoxybenzenethiol (I) with 4'-methoxyphenacyl bromide (II) afforded sulfide (III). Cyclization of (III) with concomitant rearrangement in the presence of polyphosphoric acid produced a mixture of regioisomers (IV) and (V) that were separated by their different solubility in acetone. Then, Friedel-Crafts acylation of the desired insoluble isomer (IV) with 3,4,5-trimethoxybenzoyl chloride (VI) in the presence of AlCl3 provided the title ketone, which was separated from some demethylated byproduct by means of silica gel chromatography.

参考文献No.533668
标题:Hepatocyte gene therapy in a large animal: A neonatal bovine model of citrullinemia
作者:Lee, B.; Dennis, J.A.; Healy, P.J.; Mull, B.; Pastore, L.; Yu, H.; Aguilar-Cordova, E.; O'Brien, W.; Reeds, P.; Beaude, A.L.
来源:Proc Natl Acad Sci USA 1999,96(7),3981
合成路线图解说明:

Alkylation of 3-methoxybenzenethiol (I) with 4'-methoxyphenacyl bromide (II) afforded sulfide (III). Cyclization of (III) with concomitant rearrangement in the presence of polyphosphoric acid produced a mixture of regioisomers (IV) and (V) that were separated by their different solubility in acetone. Then, Friedel-Crafts acylation of the desired insoluble isomer (IV) with 3,4,5-trimethoxybenzoyl chloride (VI) in the presence of AlCl3 provided the title ketone, which was separated from some demethylated byproduct by means of silica gel chromatography.

参考文献No.555591
标题:Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec
作者:Jones, C.D.; Jevnikar, M.G.; Pike, A.J.; Peters, M.K.; Black, L.J.; Thompson, A.R.; Falcone, J.F.; Clemens, J.A.
来源:J Med Chem 1984,27(8),1057
合成路线图解说明:

Alkylation of 3-methoxybenzenethiol (I) with 4'-methoxyphenacyl bromide (II) afforded sulfide (III). Cyclization of (III) with concomitant rearrangement in the presence of polyphosphoric acid produced a mixture of regioisomers (IV) and (V) that were separated by their different solubility in acetone. Then, Friedel-Crafts acylation of the desired insoluble isomer (IV) with 3,4,5-trimethoxybenzoyl chloride (VI) in the presence of AlCl3 provided the title ketone, which was separated from some demethylated byproduct by means of silica gel chromatography.

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