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14-羟基菲并[9,10,3’,4’]吲哚里西啶的合成及生物活性研究 总被引:1,自引:0,他引:1
以吡咯为起始原料, 以三氟氧钒(VOF3)氧化偶联重排反应为关键步骤, 经过7步反应, 合成了结构骨架全新的14-羟基菲并[9,10,3’,4’]吲哚里西啶化合物8, 总收率为55%. 采用1H NMR, 13C NMR, IR, MS和HRMS对中间体和目标产物进行了表征. 初步的抗烟草花叶病毒生物活性测试结果表明, 目标化合物8对烟草花叶病毒无明显抑制作用, 但具有较好的抗肿瘤活性, 中间体9-氧代-14-羟基-14a-甲氧基菲并[9,10,3’,4’]吲哚里西啶化合物7却表现出了很好的抗烟草花叶病毒活性. 相似文献
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Synthesis and reactivity of 3-(trichlorogermyl)propanoic acid and 3-(triphenylgermyl) propanoic acid
3-(Trichlorogermyl)propanoic acid (la) reacts with phenylmagnesium bromide in malar ratio 1:4 to give 3-(triphenylgermyl)propanoic acid (2a).In the compounds la and 2a theβ-carboxylic functional group shows some unusual properties when they react with excess of phenylmagnesium bromide.The compound la reacts with phenylmagnesium bromide in molar ratio 1:5 to give phenyl 2-(triphenylgermyl)ethylketone (3a) and in molar ratio 1:6 to give l,l-diphenyl-3-(triphenylgermyl)propanol (4a).The compound 2a reacts with phenylmagnesium bromide in molar ratio 1:2 to give 3a and in molar ratio 1:3 to give 4a also.Dehydration of the compound 4a with dilute hydrochloric acid seems especially easy.Moreover,the compound la reacted with phenylmagnsium bromide in molar ratio 1:6,then the mixture was treated with dilute hydrochloric acid to give 1,1-diphenyl-3-(triphenylgermyl)-1-propene (5a) in one pot reaction.Alkyl Ge-C bond in the compound 5a can be cleaved selectively by lithium aluminium hydride ( LiAlH4) in good yiel 相似文献
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综述了近年来发现的具有各种生物活性的六类有机锗化合物的合成及生物活性,即倍半锗和介吗川类有机化合物,锗氧杂、锗氮杂及锗硫杂环酮类化合物,呋喃、噻唑、咪唑、嘧啶取代锗烷及其类似物,烷锗醇、烷锗醚和烷锗酮类化合物,卟啉锗类化合物,其它具有生物活性的有机锗化合物这六类有机锗化合物,并对该领域的研究前景作了展望。 相似文献
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四配位有机锗化合物的13C NMR表征 总被引:1,自引:0,他引:1
对三十多年所发表的四配位有机锗化合物的核磁共振碳谱进行了综合评论.即对饱和烃基锗、不饱和烃基锗、锗杂环化合物、有机锗卤化合物、有机锗醚化合物这五类有机锗化合物的13C NMR数据作了系统的归纳,对光谱特征进行了总结. 相似文献
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N-(2-氟-4-氯-5-取代苯基)异吲哚-1,3-二酮衍生物的合成及除草活性 总被引:1,自引:0,他引:1
为了发现新的农药先导化合物,以氯酰亚酞和苯氧羧酸酯结构为基础,通过活性亚结构拼接方法,设计合成了一系列新型的N-(2-氟-4氯-5-取代苯基)异吲哚-1,3-二酮衍生物6a~6f和7a~7k.目标化合物以2-氯-4-氟-5-硝基苯酚为原料,经4步反应制得,其结构经过1H NMR,13C NMR,HRMS确证.初步生物活性测试结果表明,大部分化合物在1500 g/ha剂量下,对双子叶杂草苘麻、反枝苋具有优异的芽前芽后除草活性.进一步活性筛选发现,化合物6d在750g/ha剂量下对苘麻、反枝苋具有100%抑制活性,化合物7a,7i在22.5 g/ha剂量下对苘麻的芽后抑制率大于80%,远高于对照药剂三氟羧草醚. 相似文献
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1 INTRODUCTION Both β-triphenylgermanyl propionic acid and its derivatives have recently attracted a great deal of attention due to their strong anti-inflammatory as well as antibiotic properties[1~3]. α-aminobenzyl- phosphonates are also reported to exhibit diverse biological activities[4~6].It is conceivable that the incorporation of the two moieties into one structural unit might produce an unexpected effect on the activity of such a compound, and the studies on this type of novel s… 相似文献
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通过自由基反应,成功的合成了(S)-(+)-娃儿藤碱(1)及其类似物.以2,3,6,7.四甲氧基菲甲酸为原料通过两或三步分别制得(-)-N-(2,3,6,7,四甲氧基-9-菲苄基).2.溴甲基四氢吡咯(7)和(-)-N-(2,3,6,7-四甲氧基-9-菲甲酰基)-2-溴甲基四氢吡咯(9).在催化量的偶氮二异丁腈参与下,溴化物(7)与三正丁基氢化锡反应没有得到预期的产物(S)-(+)-娃儿藤碱,却以较高的收率得到N-(2,3,6,7-四甲氧基-9-菲苄基)哌啶(2).通过分析机理,改用溴化物(9)为底物在同样的条件下分别以33.6%和65%的收率制得(S)-(+)-9-娃儿藤酮(10)和(-)-N-(2,3,6,7-四甲氧基-9-菲甲酰基)-2-甲基四氢吡咯(11).通过实验发现,化合物(10)和(11)的收率与偶氮二异丁腈的加入量密切相关.我们认为偶氮二异丁腈在该反应中充当着双重角色,并提出了可能机理.化合物(10)和(11)经四氢锂铝还原顺利得到(S)-(+)-娃儿藤碱(1)和其结构类似物(+)-N-(2,3,6,7-四甲氧基-9-菲苄基)-2-甲基四氢吡咯. 相似文献
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1 INTRODUCTION The nature and topography of the herbicide binding site in the reaction center of photosystem Ⅱ (PSⅡ) have been the subject of intense interest for many years. Among several commercially important herbicides with different structures such as atrazine and polypeptide of the PSII reaction center[1], the cyanoacrylates with general structure 1 have proved hightly potent and useful as probes[2, 3] of the receptor because their activities as inhibitors of photosynthetic ele… 相似文献