7-Nitro-4-chrolo-quinazoline （4） was synthesized by two-step reactions using 4-nitro-2-aminobenezic acid and formamidine acetate as starting materials. And then, 3-（substituted-phenyl）- isoxazole-5-methylamine derivatives 5a-5e were synthesized by synthesizing substituted benaldehyde oxime, [3＋2] dipolar cycloaddition reaction with propargyl alcohol, then acylation with methanesulfonyl chloride, substitution with NaN3 and reduction with Zn/NHnCl. Subsequently, 3-（substituted-phenyl）isoxazole-5-methylamino-4（3H）-quinazoline derivatives 6a-6e were obtained by solid-grinding 5a-5e and 4 under the basic Al_2O_3 at room temperature. Their structures were confirmed by IR, HNMR and ESI-MS spectra. The compounds 6a, 6c and 6d were assayed in vitro activity against PTPalpha, PTPepsilon, and showed that the tested compounds had no notable inhibitory activity in the concentration of 20 mug/mL.