【药物名称】SMA-41
化学结构式(Chemical Structure):
参考文献No.337587
标题:Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth f
作者:Rewcastle, G.W.; Denny, W.A.; Bridges, A.J.; Zhou, H.; Cody, D.R.; McMichael, A.; Fry, D.W.
来源:J Med Chem 1995,38(18),3482
合成路线图解说明:

Coupling of chloroquinazoline (I) with 3-bromoaniline (II) in refluxing isopropanol yielded anilinoquinazoline (III). The nitro group was then reduced with Fe dust and AcOH in aqueous ethanol to give amine (IV). Finally, condensation with acrylic acid (V) using 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide.HCl (EDC) in DMF provided the target acrylamide.

合成路线图解说明:

Arylamine (I) is converted into the corresponding methyltriazene (II) by formation of the corresponding diazonium salt with NaNO2 in HCl/H2O, followed by reaction with methylamine. Finally, the target compound is obtained by coupling of (II) with the corresponding amine in refluxing isopropanol.

参考文献No.649178
标题:Studies of the model of action of antitumor triazenes and triazines. 6. 1-Ayl-3-(hydroxymethyl)-3-methyltriazenes: Synthesis, chemistry, and antitumor properties
作者:Vaughan, K.; Tang, Y.; Llanos, G.; Horton, J.K.; Simmonds, R.J.; Hickman, J.A.; Stevens, M.F.
来源:J Med Chem 1984,27(3),357
合成路线图解说明:

Arylamine (I) is converted into the corresponding methyltriazene (II) by formation of the corresponding diazonium salt with NaNO2 in HCl/H2O, followed by reaction with methylamine. Finally, the target compound is obtained by coupling of (II) with the corresponding amine in refluxing isopropanol.

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