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1.
异氰酸苯醇和N-[2-(4,6-二甲基)-嘧啶基]-羟胺(5)反应生成1-[2-(4,6-二甲基)-嘧啶基]-1-羟基-3-苯基脲(6)。化合物(6)在三乙胺存在下和氯甲酸乙醇反应生成2-[2-(4,6-二甲基)-嘧啶基]-4-苯基-1,2,4-噁二唑烷-3,5-二酮(1)。 相似文献
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为寻找结构新颖的嘧啶类杀菌剂,以2-氯嘧啶-4-甲酸、1-甲基-4-吡唑硼酸频哪醇酯、取代苯胺或取代苄胺等为原料,经Suzuki偶联和酰胺化反应合成了13种2-(1-甲基-1H-吡唑-4-基)嘧啶-4-甲酰胺类化合物,其结构经过1H NMR、13CNMR、IR、HRMS鉴定,并利用X射线单晶衍射法确定了N-苄基-2-(1-甲基-1H-吡唑-4-基)嘧啶-4-甲酰胺(4h)的晶体结构.初步测试了目标化合物对3种植物病原菌的杀菌活性,在浓度为100 mg/L时, N-(4-甲基苯基)-2-(1-甲基-1H-吡唑-4-基)嘧啶-4-甲酰胺(4f)和N-(4-氯苄基)-2-(1-甲基-1H-吡唑-4-基)嘧啶-4-甲酰胺(4j)对水稻纹枯菌表现出较高的杀菌活性,抑制率分别为85.3%和79.1%.分子对接研究显示4f可与琥珀酸脱氢酶活性腔内的氨基酸残基形成2个氢键和1个阳离子-π相互作用. 相似文献
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《合成化学》2015,(7)
以3-甲基-1-苯基-2-吡唑啉-5-酮为原料,经Vilsmeier-Haack反应和Biginelli反应制得4-(5-氯-3-甲基-1-苯基-唑-4-基)-5-甲酸乙酯-6-甲基-3,4-二氢嘧啶-2(1H)-硫酮(3);3与芳醛经Knoevenagel反应合成了5个新型的含吡唑的噻唑[3,2-a]并嘧啶类化合物(5a~5e),其结构经1H NMR,13C NMR,IR和ESI-MS表征。采用MTT法测定了5a~5e的抗肿瘤活性。结果表明:5a~5e对人前列腺癌PC-3细胞均具有一定的体外抗增殖活性,其中2-【4-{[6-(乙氧羰酯)-5-(5-氯-3-甲基-1-苯基-吡唑-4-基)-3-氧代-7-甲基-噻唑并[3,2-a]嘧啶-2(5H)-亚基]甲基}苯氧基】乙酸(5a)活性最强,其IC50为44.45μM。 相似文献
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本文利用2-氨基喹啉和2-氨基苯骈咪唑作为亲核试剂,与5-(双甲硫基亚甲基)丙二酸亚异丙酯(1)、5-(甲硫基亚烃基)丙二酸亚异丙酯(3)反应,开发出3-取代-(1H)-嘧啶-[1,2-a]喹啉-1-酮(5)和2-取代嘧啶[1,2-a]苯骈咪唑-4-(10H)-酮(6)通用的简便合成法。 相似文献
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用烯基膦亚胺与苯基异氰酸酯、仲胺的串联aza-Wittig反应合成了8个新的2-二烷氨基-3-苯基-5-甲基-6-(1H-1,2,4-三唑-1-基)-噻吩并[2,3-d]嘧啶-4(3H)-酮衍生物(6a~6h),其结构经1H NMR, MS和元素分析表征.初步生物活性测试结果表明,部分6表现出一定的抑菌活性,其中6f在浓度为5×10-5g·L-1时,对棉花炭疽菌的抑制率达到87%. 相似文献
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应用串联氮杂Wittig反应设计合成了一系列新的2-烷氨(芳氧)基-3,8-二苯基-5-芳基-6-甲基-5,8-二氢-4H-吡唑并[4',3':5,6]吡喃并[2,3-d]嘧啶-4(3H)-酮衍生物。通过氢核磁共振谱仪(1H NMR)、傅里叶变换红外光谱仪(FTIR)和元素分析等方法对所合成的化合物进行了结构表征,用X射线单晶衍射确证了化合物2-二正丙基氨基-3,8-二苯基-5-(4-甲基苯基)-6-甲基-5,8-二氢-4H-吡唑并[4',3':5,6]吡喃并[2,3-d]嘧啶-4(3H)-酮(Ⅲi)晶体结构。室内的杀菌和杀虫活性测试结果表明:目标化合物具有一定的杀菌活性,其中部分化合物对黄瓜灰霉菌(Botrytis cinereapers)在50 mg/L剂量下抑制率达到90%以上,显示了优异的杀菌活性;对水稻褐飞虱无明显的杀虫活性,但发现对粘虫具有较高的杀灭效果,大多数抑制率达到90%以上。 相似文献
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V. L. Gein O. V. Bobrovskaya K. A. Tkachenko L. F. Gein 《Russian Journal of General Chemistry》2014,84(7):1349-1352
Depending on the reaction condition, 1-(4-aminosulfonylphenyl)-5-aryl-4-aroyl-3-hydroxy-3-pyrrolin-2-ones reacted with aromatic amines to yield 3-arylamino-3-pyrrolin-2-ones or 4-[aryl (arylamino) methylene]tetrahydropyrrole-2,3-diones. Reactions of 1-(4-aminosulfonylphenyl)-5-aryl-4-aroyl-3-hydroxy-3-pyrrolin-2-ones with hydrazine hydrate afforded pyrrolo[3,4-c]pyrazol-6-ones. 相似文献
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2-芳胺基-5-[5'-氨基-1'-(4''-氯苯基)-1', 2', 3'-三唑-4'-基]——-1, 3, 4-恶二唑的合成 总被引:11,自引:0,他引:11
利用1-[5'-氨基-1'-(4'-氯苯基)-1', 2', 3'-三唑-4'-甲酰基]-4-芳基氨基硫脲在汞盐Hg(OAc)2-HOAc中加热缩合, 制得11种新的2-芳胺基-5-[5'-氨基-1'-(4'-氯苯基)-1', 2', 3'-三唑-4'-基]---1, 3, 4-恶二唑。所有化合物的结构经元素分析, IR、MS以及1H NMR确认。选择代表物作生测试验, 结果表明, 2b, 2k中MIC3.1mg/L时, 对大肠杆菌及金黄色葡萄球菌繁殖有明显抑制。 相似文献
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The title compound (R)-N'-[2-(4-methoxy-6-chloro)-pyrimidyl]-N-[3-methyl-2-(4-chlorophenyl)butyryl]-urea has been synthesized, and its crystal structure and biological behaviors were studied. Crystallographic data: C17H18Cl2N4O3, Mr = 397.25, monoclinic, space group P21/c, a = 12.331 (2), b = 14.025(3), c = 23.085(5) (A), β = 99.607(4)°, Z = 8, V = 3936.2(13) (A)3, Dc = 1.341 g/cm3, F(000) = 1648, R = 0.0718, wR = 0.1585 and μ(MoKα) = 0.353 mm-1. The preliminary biological tests showed that the title compound has definite insecticidal and fungicidal activities. 相似文献
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Krow GR Lester WS Liu N Yuan J Hiller A Duo J Herzon SB Nguyen Y Cannon K 《The Journal of organic chemistry》2001,66(5):1811-1817
Methyl- and phenyl-substituted N-(ethoxycarbonyl)-2-azabicyclo[2.2.0]hex-5-enes 6 were reacted with NBS in wet DMSO to afford bromohydrins. Mixtures of unrearranged 6-exo-bromo-5-endo-hydroxy-2-azabicyclo[2.2.0]hexanes 7a,b and rearranged 5-anti-bromo-6-anti-hydroxy-2-azabicyclo[2.1.1]hexanes 8a,b were formed stereoselectively from the parent alkene 6a and 4-methyl alkene 6b. The 5-methyl alkene 6c affords only unrearranged bromohydrin 7c and dibromohydrin 9. By contrast, solely rearranged 3-endo-substituted-2-azabicyclo[2.1.1]hexane bromohydrins 8d-f result from additions to 3-endo-methyl alkene 6d, 3-endo-4-dimethyl alkene 6e, and 3-endo-phenyl alkene 6f. As an alternative route to bromohydrins, the parent 5,6-exo-epoxide 10a and 5-endo-methyl-5,6-exo-epoxide 10b were ring opened with bromine/triphenylphosphine to afford unrearranged 5-endo-bromo-6-exo-hydroxy-2-azabicyclo[2.2.0]hexanes 11a,b, while the 3-endo-methyl epoxide 10c afforded solely the rearranged 5-anti-bromo-6-anti-hydroxy-3-exo-methyl-2-azabicyclo[2.1.1]hexane isomer 8g. Tributyltin hydride reduction of bromohydrins 7a,b and 11a afforded novel 2-azabicyclo[2.2.0]hexan-5-ols 13a,b and -6-ol 14, and bromohydrins 8a,b, 8d-g afforded new 2-azabicyclo[2.1.1]-hexan-5-ols 15a,b and 15d-g. 相似文献
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经1-[5'-氨基-1'-(4"-氯苯基)-1',2',3'-三唑-4'-甲酰基]-4-(3'-溴苯基)-3-氨基硫脲在浓硫酸作用下制得2-(3'-溴苯胺基)-5-[5'-氨基-1'-(4"-氯苯基)-1',2',3'-三唑-4'-基]-1,3,4-噻二唑化合物。该化合物的晶体结构经X射线衍射分析确定, 化合物属三斜晶系, P1空间群, a=1.1784(2), b=1.4455(2),c=1.1353(1)nm; α=100.68(1), β=109.50(1), γ=79.89(1)°; V=1.7779nm^3; 分子式C~1~6H~1~1BrClN~7S, Mr=448.75; Dc=1.673g/cm^3, Z=4,μ=58.16cm^-^1, 最终偏离因子R=0.084, Rw=0.086。分析化合物的键长, 键角数据表明, 该分子具有离域π键结构。 相似文献
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微波辐射下2-[4-二-(4-氟苯)甲基]哌嗪乙酰腙化合物的合成 总被引:3,自引:0,他引:3
微波辐射条件下, 以丙酮作溶剂, 1-[二-(4-氟苯)甲基]哌嗪与氯乙酸乙酯反应得到2-[二-(4-氟苯)甲基]哌嗪乙酸乙酯(1), 1与水合肼在微波辐射条件下反应得到2-[二-(4-氟苯)甲基]哌嗪乙酰肼(2), 进一步在微波辐射条件下由2-[二- (4-氟苯)甲基]哌嗪乙酰肼(2)与取代芳香醛反应制得目标化合物3a~3f. 合成的6个目标化合物通过熔点测定和质谱、红外光谱、核磁共振氢谱分析、元素分析对其结构进行确证. 相似文献
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Synthetic approaches to 6
-9-methoxy-5, 11-dimethylpyrido[4,3-
] fluorene are described, thus 2-[1-(4-pyridyl)ethyl]6-methoxyindanone has been reacted with vinylmagnesium bromide to yield 2-[1-(4-pyridyl)ethyl]-6 methoxy-1-vinyl-1-indanol. However, on dehydration this compound rearranges to 2-[1-(4-pyridyl)ethyl]-3-ethylidene-5-methoxyindene rather than the required isomer 3-ethylidine-2-[1-(4-pyridyl)ethyl]-5-methoxyindane needed fro pericyclic ring-closure to the pyrido[4,3-
]fluorene system. Reaction of
-2-[1-methyl-1-(4-pyridyl)methylene]-6-methoxyindanone with ethylene triphenylphosphorane similarly gives 6-methoxy-spiro-2-[1-(2,3-dimethyl-3-(4-pyridyl)-cyclopropyl) indanone rather than the desired indane. 相似文献
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Quinazolinecarboxylic Acids. Synthesis of Alkyl [2-(Ethoxycarbonyl)-3,4-dihydro-4-oxoquinazolin-3-yl]-, [2-(Ethoxycarbonyl)quinazolin-4-yloxy]- and (5,6,7,8-Tetrahydro-2-phenylquinazolin-4-ylthio)alkanoates The [(2-aminobenzoyl)amino]alkanoic acids and their esters 1 showed a different reaction behaviour with diethyl oxalate. Compound 1 (n = 2,3) was converted into the quinazolinylalkanoates 3 . o-Aminohippurate yielded with ethyl (chloroformyl)formate a mixture of the amide 4 and the cyclized quinazolinone 7b . Ethyl 3,4-dihydro-4-oxoquinazoline-2-carboxylate ( 6 ) reacted with 2-bromoalkanoates, in the presence of NaH, to the [2-(ethoxycarbonyl)-3,4-dihydro-4-oxoquinazolin-3-y1]acetates 7 in the case of alkyl bromoacetate, and to the O-alkylated derivatives 8 with the ethyl 2-bromopropionate and -butyrate. 2-Aminobenzamide ( 5 ) gave with ethyl 3-(chloroformyl)-2-propenoate and methyl 3-(chloroformyl)propionate the amides 9 or 11 , respectively, and not the expected quinazolinones. The cyclized product 12 was obtained from 11 and ethyl bromoacetate. Tetrahydroquinazolin-4(3H)-thione 14 was synthesized by the reaction of 13 with NH3, and it was alkylated at the S-atom with bromoalkanoates to 15 . The hydrazide 16 was synthesized from 15b with hydrazine hydrate. 相似文献