【药物名称】Sulofenur, LY-186641
化学结构式(Chemical Structure):
参考文献No.136726
标题:Novel agents effective against solid tumors: The diarylsulfonylureas. Synthesis, activities and analysis of quantitative structure-activity relationships
作者:Grossman, C.S.; Kramer, K.E.; Crowell, T.A.; Grindey, G.B.; Rieder, B.J.; Rinzel, S.M.; Harper, R.W.; Howbert, J.J.; Tao, E.V.; Aikins, J.; Shaw, W.N.; Poore, G.A.; Todd, G.C.
来源:J Med Chem 1990,33(9),2393-407
合成路线图解说明:

1) 5-Indansulfonamide (I) is converted to ethyl N-(5-indansulfonyl)carbamate (II) with ethyl chloroformate and potassium carbonate in refluxing 2-butanone, which is then reacted with 4-chloroaniline (III) in toluene at reflux to provide sulofenur. 2) Alternatively, (I) can be converted to its anion with NaOH in aqueous acetone, then reacted with 4-chlorophenylisocyanate (IV) to give sulofenur directly.

参考文献No.139960
标题:Sulofenur
作者:Howbert, J.J.
来源:Drugs Fut 1991,16(6),517
合成路线图解说明:

1) 5-Indansulfonamide (I) is converted to ethyl N-(5-indansulfonyl)carbamate (II) with ethyl chloroformate and potassium carbonate in refluxing 2-butanone, which is then reacted with 4-chloroaniline (III) in toluene at reflux to provide sulofenur. 2) Alternatively, (I) can be converted to its anion with NaOH in aqueous acetone, then reacted with 4-chlorophenylisocyanate (IV) to give sulofenur directly.

参考文献No.802340
标题:Indentification of diarylsulfonylureas as novel anticancer drugs
作者:Grindey, G.B.
来源:Proc Amer Assoc Cancer Res 1988,29553-6
合成路线图解说明:

1) 5-Indansulfonamide (I) is converted to ethyl N-(5-indansulfonyl)carbamate (II) with ethyl chloroformate and potassium carbonate in refluxing 2-butanone, which is then reacted with 4-chloroaniline (III) in toluene at reflux to provide sulofenur. 2) Alternatively, (I) can be converted to its anion with NaOH in aqueous acetone, then reacted with 4-chlorophenylisocyanate (IV) to give sulofenur directly.

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