【药物名称】PD-161989
化学结构式(Chemical Structure):
参考文献No.36320
标题:Cyclic amine derivs. of substd. quinoxaline 2,3-diones as glutamate receptor antagonists
作者:Kornberg, B.E.; Nikam, S.; Rafferty, M.F.; Yuen, P.-W. (Pfizer Inc.)
来源:JP 1999506724; US 5874426; WO 9640650
合成路线图解说明:

2-Amino-6-methylbenzoic acid (I) was reduced to alcohol (II) using LiAlH4, and then acetylated in Ac2O at 50 C. The acetyl protected compound (III) was nitrated with HNO3 in AcOH to afford (IV), which was hydrolyzed to the nitroaniline (V) with methanolic KOH. Subsequent condensation with pyrrolidine (VI) in the presence of diethyl azodicarboxylate and triphenylphosphine provided tertiary amine (VII). Hydrogenation of the nitro group of (VII) over Raney-Ni gave phenylenediamine (VIII), which was cyclized with dimethyl oxalate to produce quinoxalinedione (IX). This was finally nitrated with KNO3 in H2SO4 to furnish the title compound.

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