SIOC 中文
CJOG
Adv search

Chin. J. Org. Chem. ›› 2008, Vol. 28 ›› Issue (07): 1204-1206. Previous Articles     Next Articles

Original Articles

新型含异噁唑环的喹唑啉衍生物的合成和抑蛋白酪氨酸酶 α和ε活性研究

雍建平a,b ; 阿吉艾克拜尔•艾萨*,a   

  1. (a中国科学院新疆理化技术研究所 乌鲁木齐 830011)
    (b中国科学院研究生院 北京 100039)
  • 收稿日期:2007-08-13 修回日期:2007-12-08 发布日期:2008-07-28
  • 通讯作者: 阿吉艾克拜尔•艾萨

Synthesis of Novel Isoxazole Ring Containing Quinazoline Deriva-tives and in vitro Inhibitory Activity Against PTPα and PTPε

YONG, Jian-Ping a,b; HAJI, Akber Aisa*,a   

  1. (a Xinjiang Technical Institute of Physics and Chemistry , Chinese Academy of Science, Urumqi 830011)
    (b Graduate School of Chinese Academy of Science, Beijing 100039)
  • Received:2007-08-13 Revised:2007-12-08 Published:2008-07-28
  • Contact: HAJI, Akber Aisa

PDF

668

Cited

2

7-Nitro-4-chrolo-quinazoline (4) was synthesized by two-step reactions using 4-nitro-2-amino-
benezic 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/NH4Cl. Subsequently, 3-(substituted-phenyl)isoxa- zole-5-methylamino-4(3H)-quinazoline derivatives 6a～6e were obtained by solid-grinding 5a～5e and 4 under the basic Al2O3 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 PTPα, PTPε, and showed that the tested compounds had no notable inhibitory activity in the concentration of 20 μg/mL.

Key words: 3-(substituted-phenyl)-isoxazole-5-methylamine, PTPε, 3-(substituted- phenyl)-isoxazole-5-methylamino-4(3H)-quinazoline derivative, inhibitory activity against PTPα, 7-nitro-4-chrolo-quinazoline