Hines J W, Stammer C H
J Med Chem. 1977 Jul;20(7):965-7. doi: 10.1021/jm00217a023.
The synthesis of the title compound, 3-hydroxyisoxazole-5-hydroxamic acid (4b), by two procedures is described. The first, involving the treatment of dimethyl acetylenedicarboxylate with hydroxylamine, had previously been reported to give the 3-hydroxyisoxazole-5-carboxylic acid (4a). In the second, treatment of chlorofumaroyl dichloride with hydroxylamine also gave the intermediate chlorofumarodihydroxamic acid (6). Compound 6 was found to have some activity against P388 lymphocytic leukemia.
本文描述了通过两种方法合成标题化合物3-羟基异恶唑-5-异羟肟酸(4b)的过程。第一种方法是用羟胺处理乙炔二甲酸二甲酯,此前报道该方法会生成3-羟基异恶唑-5-羧酸(4a)。第二种方法是用羟胺处理氯富马酰二氯,同样得到中间体氯富马二异羟肟酸(6)。发现化合物6对P388淋巴细胞白血病具有一定活性。