共查询到20条相似文献,搜索用时 434 毫秒
1.
含有 1 ,2 ,4 三嗪结构的化合物具有广泛的生理活性。我们曾用α 乙酰基硫代甲酰芳胺为原料 ,合成了一系列三嗪类和其它杂环化合物 ,其中1 ,2 ,4 三嗪类有 4,6 二取代 5 硫酮 1 ,2 ,4三嗪 3 酮[1 ,2 ] ,3 氨基 5 取代苯氨基 6 苯基 1 ,2 ,4 三嗪[3] 等化合物。本文以α 乙酰基硫代甲酰芳胺为原料 ,进一步合成 5 取代苯氨基 6 甲基 1 ,2 ,4 三嗪 3 硫酮。当乙酰基硫代甲酰芳胺 1 (a g)与氨基硫脲 2反应时 ,首先生成缩氨基硫脲 3(a g) ,然后环化得到 5 取代苯氨基 6 甲基 1 ,2 ,4 三嗪 3硫酮 4(a g) ,合成中发现 ,4(a g)可… 相似文献
2.
4—取代苯基—6—叔丁基—5—硫酮—1,2,4—三嗪—3—酮的合成 总被引:1,自引:0,他引:1
含有1,2,4三嗪母体环的化合物与核糖连接后,能参与蛋白质分子的合成,改变蛋白质的分子结构,具有抗癌、抗病毒、抗菌及杀虫除草等多种药物活性。作为三嗪类化合物的重要分支,4,6二取代5硫酮1,2,4三嗪3酮由于合成及分离上的困难,目前研究得较少[1][2]。4位为芳香基、6位为叔... 相似文献
3.
为发展更加高效的三嗪酮杀虫活性分子,本文设计合成了16种氨基部分被取代的三嗪酮衍生物,并测试了其杀虫、抑菌活性。杀虫活性测试表明:在浓度为600mg·kg~(-1)时,化合物N-(苯基氧羰基)-N-(6-甲基-3-氧代-2,3-二氢-1,2,4-三嗪-4(5H)-基)氨基甲酸苯酯(3e,100%、100%、100%)的杀棉铃虫、玉米螟、粘虫活性高于吡蚜酮(20%,35%,50%)。在浓度为0.5mg·kg~(-1)时,化合物3e(60%)的杀蚊幼虫活性高于吡蚜酮(0)。抑菌活性测试表明:三嗪酮酰胺衍生物对玉米小斑病菌和西瓜炭疽病菌表现出较高的抑菌活性;而三嗪酮亚胺衍生物对小麦纹枯病菌表现出较高的抑菌活性。 相似文献
4.
报道一种以羟基卟啉与三嗪和其它亲核试剂为原料一锅法高产率合成不对称多取代三嗪卟啉化合物的简单方法. 研究了2,4,6-三氯三嗪与羟基卟啉、醇和胺通过分级亲核取代反应合成不对称2,4,6-取代三嗪卟啉的方法和反应条件. 以2,4,6- 三氯三嗪和5-(4-羟基)苯基-10,15,20-三苯基卟啉反应生成卟啉单取代二氯三嗪, 然后进一步与醇或胺反应合成了7个三嗪卟啉新化合物, 产物经元素分析, MS, 1H NMR和UV-Vis进行结构表征. 相似文献
5.
6.
7.
8.
4个新型有机磷缩合试剂的合成及其在生物活性肽合成中的应用 总被引:2,自引:0,他引:2
报道了4个新型有机磷化合物:N-二乙氧基磷酰苯并唑酮(DEPBO)、N-(2-氧-1,3,2-二氧杂磷杂环乙烷基)-苯并唑酮(DOPBO)、3-(2'-氧-1',3',2'-二氧杂磷杂环己烷基)-氧-1,2,3-苯共三嗪-4(3H)-酮(DOPBT)和3-(二乙氧基磷酰基)-氧-1,2,3-苯并三嗪-4(3H)-酮(DEPBT)的合成,并研究了它们作为缩会试剂在多肽合成中的应用. 研究结果表明,它们可以成功地用于固相法和溶液法合成多肽,其中DEPBT还可用于环肽的合成. 应用DEPBO和DEPBT合成了促睡眠肽的类似物及从云南中草药繁缕中分离鉴定的一个环七肽等生物活性肽. 相似文献
9.
10.
含1,2,4-三嗪结构的化合物具有抗病毒、调节植物生长等作用。本文用α-叔戊酰基硫代甲酰取代苯胺缩氨基脲环化得到4-取代苯基-6.叔丁基-5-硫酮-1,2,4三嗪-3-酮,进一步环化得到5诹代苯氨基-6-叔丁基-1,2,4-三嗪-3-酮。反应方程式如下: 相似文献
11.
12.
The enantioselective synthesis of the title compound, using Meyers' bicyclic lactam methodology, is described. This compound and a few of its derivatives are useful intermediates in natural product synthesis. 相似文献
13.
Kuranaga T Ohtani N Tsutsumi R Baden DG Wright JL Satake M Tachibana K 《Organic letters》2011,13(4):696-699
The first and highly efficient total synthesis of (-)-brevisin has been achieved. The title compound was synthesized in only 29 steps (longest linear sequence) from commercially available starting materials. The synthesis provided over 70 mg of a marine polycyclic ether compound. 相似文献
14.
Rivkin A Yoshimura F Gabarda AE Cho YS Chou TC Dong H Danishefsky SJ 《Journal of the American Chemical Society》2004,126(35):10913-10922
We provide a full account of the discovery of the (E)-9,10-dehydro derivatives of 12,13-desoxyepothilone B (dEpoB), a new class of antitumor agents with promising in vivo preclinical properties. The compounds, which are to date not available by modification of any of the naturally occurring epothilones, were discovered through total chemical synthesis. We describe how our investigations of ring-closing metathesis reactions in epothilone settings led to the first and second generation syntheses of (E)-9,10-dehydro-12,13-desoxyepothilone congener 6. With further modifications, the synthesis was applied to reach a 26-trifluoro derivative compound (see compound 7). To conduct such studies and in anticipation of future development needs, the total synthesis which led to the initial discovery of compound 7 was simplified significantly. The total synthesis methodology used to reach compound 7 was then applied to reach more readily formulated compounds, bearing hydroxy and amino functionality on the 21-position (see compounds 45, 62, and 63). Following extensive in vitro evaluations of these new congeners, compound 7 was nominated for in vivo evaluations in xenograft models. The data provided herein demonstrate a promising therapeutic efficacy, activity against large tumors, nonrelapseability, and oral activity. These results have identified compound 7 as a particularly promising compound for clinical development. The excellent, totally synthetic, route to 7 makes such a program quite feasible. 相似文献
15.
16.
Sanat K. Mandal Laurence K. Thompson Soma Ray 《Journal of heterocyclic chemistry》1992,29(6):1671-1672
The synthesis of substituted 1,3-bis-(2-pyridylimino)isoindoline 4 from 1,2,4,5-tetracyanobenzene and 2,6-diaminopyridine under mild and dilute conditions constitutes a new approach to produce a functionalized compound 4. The synthesis of an analogous compound 5 from 1,2,4,5-tetracyanobenzene and 2-amino-6-methylpyridine is also described. 相似文献
17.
Yu. G. Khabarov N. Yu. Kuzyakov G. V. Komarova V. A. Veshnyakov A. A. Patrakeev 《Russian Journal of Applied Chemistry》2015,88(12):1981-1985
The conditions of the synthesis of a magnetically active compound by redox transformation of iron(II) and chromium(VI) ions were determined. Under the synthesis conditions, the chromium compounds are recovered from the solution virtually completely. The use of technical-grade lignosulfonates in the step of the condensation of the magnetically active compound leads to considerable enhancement of the magnetic activity. 相似文献
18.
消旋反式菊酸α—氰基—4—氟—3—苯氧基苄酯的合成 总被引:1,自引:0,他引:1
含氟拟除虫菊酯的合成是近年来新型高效拟除虫菊酯研究工作的方向之一。该类化合物由于具有高效、低毒、广谱、低残留、无致癌、致畸作用,有的还具有低鱼毒,杀螨的特性,因此倍受注目。西德拜尔公司开发的百治菊酯(Baythroid)(1)便是其中一种高效杀虫剂。 相似文献
19.
J. Luis Casarrubio Santiago Conde Carlos Corral Jaime Lissavetzky 《Journal of heterocyclic chemistry》1983,20(6):1557-1560
The synthesis of the thiophene analogs of the cardio-selective β-adrenergic blocking agents Practolol and “reversed” Practolol has been attempted starting from 2-acetyl-5-bromothiophene. Although this synthesis worked for the second compound it was not possible to obtain the first one. From this and other results of this paper it can be deduced that the thiophene analog of Practolol must be an unstable compound. 相似文献
20.
In connection with natural products synthesis, we had need of 2-acetylindene (IV). The only reported synthesis of this compound is by Rupe and Müller in 1921.1 These workers formylated benzylacetone (I) and cyclized the major compound (assumed to be II) with acid to give a solid, mp 122°, reported to be IV. 相似文献