Anderson W K, Corey P F
J Med Chem. 1977 Dec;20(12):1691-4. doi: 10.1021/jm00222a034.
Treatment of N-aryl-N-acetylalanine derivatives, 3, with acetic anhydride-dimethyl acetylenedicarboxylate gave the dimethyl N-aryl-2,5-dimethylpyrrole-3,4-dicarboxylates, 4. Reduction of 4 and acylation of 5 gave 2a-j and 6. All of the title compounds 2a-j and 6 showed significant reproducible activity in the P388 in vivo antileukemic assay.
用乙酸酐 - 二甲基乙炔二羧酸酯处理N - 芳基 - N - 乙酰丙氨酸衍生物3,得到二甲基N - 芳基 - 2,5 - 二甲基吡咯 - 3,4 - 二羧酸酯4。4的还原和5的酰化得到2a - j和6。所有标题化合物2a - j和6在P388体内抗白血病试验中均表现出显著的可重复活性。