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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
Alternative TitleSynthesis of Novel Isoxazole Ring Containing Quinazoline Derivatives and in vitro Inhibitory Activity Against PTPα and PTPε
雍建平; 阿吉艾克拜尔·艾萨
2008
Source Publication有机化学
ISSN0253-2786
Volume28Issue:7Pages:1204-1208
Abstract

以2-氨基-4-硝基-苯甲酸和醋酸甲脒为原料,合成了7-硝基-喹唑啉酮(3),化合物3在SOCl2的作用下氯代得7-硝基-4-氯-喹唑啉(4);又以取代苯甲醛为起始原料,通过合成肟、1,3偶极环加成反应、甲磺酰化、叠氮化、Zn/NH4Cl还原得中间体3-(取代苯基)-异VA唑-5-甲胺衍生物5a~5e.4与5a~5e在碱性氧化铝作用下固相研磨合成了5种未见文献报道的新型的含异VA唑环的喹唑啉衍生物6a~6e.所合成的化合物通过IR,1HNMR,MS等分析方法进行了表征.体外抑蛋白酪氨酸酶α(PTPα)和蛋白酪氨酸酶ε(PTPε)活性测试结果表明测试样品浓度在20μg/mL下对PTPα和PTPε均无显著的抑制活性.;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.

Keyword7-硝基-4-氯-喹唑啉 3-(取代苯基)-异噁唑-5-甲胺 4-[3-(取代苯基)-异噁唑-5-甲氨基]喹唑啉衍生物 抗蛋白酪氨酸酶活性
Indexed BySCI ; CSCD
CSCD IDCSCD:3351965
Citation statistics
Cited Times:2[CSCD]   [CSCD Record]
Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/2082
Collection资源化学研究室
Corresponding Author阿吉艾克拜尔·艾萨
Affiliation中国科学院新疆理化技术研究所
Recommended Citation
GB/T 7714
雍建平,阿吉艾克拜尔·艾萨. 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[J]. 有机化学,2008,28(7):1204-1208.
APA 雍建平,&阿吉艾克拜尔·艾萨.(2008).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.有机化学,28(7),1204-1208.
MLA 雍建平,et al."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".有机化学 28.7(2008):1204-1208.
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