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1.
N-5-四唑基-N′-芳甲酰基脲的合成及其生物活性   总被引:5,自引:0,他引:5  
合成了 15个新的含四唑基的芳甲酰基脲类化合物 ,用IR ,1HNMR和元素分析证实了它们的结构 ,并进行了初步的生物活性试验 ,生测结果证明一些目标化合物具有优良的植物生长调节活性 ,其中N 5 四唑基 N′ 对甲氧基苯基甲酰基脲(2h)和N 5 四唑基 N′ 对溴苯基甲酰基脲 (2j)具有很好的生长素活性 ,2h ,2j和N 5 四唑基 N′ 对甲基苯基甲酰基脲 (2m )具有优良的细胞分裂素活性  相似文献   

2.
N-(5-四唑基)-N'-芳氧乙酰基脲的合成及生物活性   总被引:7,自引:3,他引:4  
细胞分裂素;N-(5-四唑基)-N'-芳氧乙酰基脲的合成及生物活性  相似文献   

3.
为寻找新的高活性农药 ,根据生物等排原理 ,设计合成了 10种未见文献报道的N′ 5 ( 1H 1,2 ,3 ,4 四唑基 ) N 芳甲酰基硫脲类化合物 .它们的结构经IR ,1HNMR和元素分析确证 .初步的生物活性测定结果表明 ,部分化合物具有优良的除草活性或植物生长调节活性 .  相似文献   

4.
以乙酰乙酸乙酯为起始原料,经四步反应制备了关键中间体3-甲基-5-苯基异嗯唑甲酰肼(2);2分别与取代苯腙基乙酰乙酸乙酯和取代苯腙基乙酰丙酮反应合成了一系列新型的1.(3′-甲基-5′-苯基-异噁唑4′-甲酰基)-3-甲基4-苯腙基吡唑酮和1-(3′-甲基-5′-苯基-异噁唑-4′-甲酰基)-3,5-二甲基4-芳偶氮基...  相似文献   

5.
N-5-(1H-1,2,4-三唑基)-N′-芳甲酰基脲的合成与生物活性   总被引:5,自引:2,他引:3  
以5-氨基-1H-1,2,4-三唑-3-羧酸与酰基异氰酸酯反应,合成了15个新的N-5-(1H-1,2,4-三唑基)-N′-芳甲酰基脲,用核磁共振氢谱、红外光谱和元素分析确证了其结构,并进行了室内生物活性测试.生测试验证明部分酰基脲类化合物具有良好的植物生长调节活性,其中N-5-(3-羧基-1,2,4-三唑基)-N′-o-氯苯甲酰基脲、N-5-(3-羧基-1,2,4-三唑基)-N′-o-溴苯甲酰基脲和N-5-(3-羧基-1,2,4-三唑基)-N′-P(或m)-甲基苯甲酰基脲具有优良的生长素活性.  相似文献   

6.
N-5-(1H-1,2,4-三唑基)-N'-芳甲酰基脲的合成与生物活性   总被引:7,自引:2,他引:5  
以5-氨基-1H-1,2,4-三唑-3-羧酸与酰基异氰酸酯反应,合成了15个新的N- 5-(1H-1,2,4-三唑基)-N'-芳甲酰基脲,用核磁共振氢谱、红外光谱和元素分 析确证了其结构,并进行了室内生物活性测试。生测试验证明部分酰基脲类化合物 具有良好的植物生长调节活性,其中N-5(3-羧基-1,2,4-三唑基)-N'-o-氯苯甲 酰基脲、N-5-(3-羧基-1,2,4-三唑基)-N'-o-溴苯甲酰基脲和N-5-(3-羧基-1, 2,4-三唑基)-N'-p(或m)-甲基苯甲酰基脲具有优良的生长素活性。  相似文献   

7.
微波辐射条件下 ,首先由 2 苯并呋喃甲酰氯在相转移条件下依次与硫氰酸铵和芳甲酰肼反应合成了一系列 1 芳甲酰基 4 ( 2′ 苯并呋喃甲酰基 )氨基硫脲 .进一步在微波辐射的条件下由这些氨基硫脲分别与碘酸钾、醋酸或醋酸汞等试剂作用高产率地制得了 1 芳甲酰基 4 ( 2′ 苯并呋喃甲酰基 )氨基脲、2 芳基 5 ( 2′ 苯并呋喃甲酰胺基 ) 1,3 ,4 噻二唑和 2 芳基 5 ( 2′ 苯并呋喃甲酰胺基 ) 1,3 ,4 二唑 .  相似文献   

8.
N'-5-四唑基-N-芳甲酰基硫脲的合成及其生物活性研究(I)   总被引:17,自引:0,他引:17  
李淑贤  汪焱钢 《有机化学》2003,23(11):1311-1313
为寻找新的高活性农药,根据生物等排原理,设计合成了10种未见文献报道的 N'-5-(1H-1,2,3,4-四唑基)-N-芳甲酰基硫脲类化合物。它们的结构经IR,~1H NMR和元素分析确证。初步的生物活性测定结果表明,部分化合物具有优良的除草 活性或植物生长调节活性。  相似文献   

9.
N'-5-四唑基-N-芳甲酰基硫脲的合成及其生物活性研究(Ⅰ)   总被引:9,自引:1,他引:8  
为寻找新的高活性农药,根据生物等排原理,设计合成了10种未见文献报道的N'-5-(1H-1,2,3,4-四唑基)-N-芳甲酰基硫脲类化合物.它们的结构经IR,1H NMR和元素分析确证.初步的生物活性测定结果表明,部分化合物具有优良的除草活性或植物生长调节活性.  相似文献   

10.
N-芳基-异丙胺甲酰基膦酰胺甲酯的研究陈茹玉,李慧英,任康太(南开大学元素有机化学研究所,天津,300071)关键词膦酰胺,氨基甲酰基膦酸酯,氢键N,N-二烷基-氨基甲酰基膦酰胺酯类化合物具有调节植物生长的活性[1],N,N-二烷基-氨基甲酰基膦酸二...  相似文献   

11.
Reduction of 2-benzoylbenzoxazole oxime gives 2-(-aminobenzyl) benzoxazole, converted to the formyl or acetyl derivative by treatment with, respectively, ethyl formate or acetic anhydride. Thiourea derivatives are obtained by treating 2-(-aminobenzyl) benzoxazole with arylisothiocyanates. Heating the above formyl or acetyl derivative with phosphorus oxychloride converts them to 3-phenyl- and 3-phenyl-1-methylimidazo [5, 1-b]-benzoxazole, which are representative members of a new tricyclic system. It did not prove possible to cyclize 1-[-(benzoxazolyl-2) benzyl]-3-phenylthiourea.  相似文献   

12.
We present here the synthesis and characterization of four photolabile derivatives of urea in which alpha-substituted 2-nitrobenzyl groups are covalently attached to the urea nitrogen. These derivatives photolyze readily in aqueous solution to release free urea. The alpha-substituents of the 2-nitrobenzyl group strongly influence the rate of the photolysis reaction measured with transient absorption spectroscopy. Rates of photolysis at pH 7.5 and room temperature (approximately 22 degrees C) for N-(2-nitrobenzyl)urea, N-(alpha-methyl-2-nitrobenzyl)urea, N-(alpha-carboxymethyl-2-nitrobenzyl)urea, and N-(alpha-carboxy-2-nitrobenzyl)urea are, respectively, 1.7 x 10(4), 8.5 x 10(4), 4.0 x 10(4), and 1.1 x 10(5) s(-)(1). The quantum yields determined by measurement of free urea following irradiation by a single laser pulse at 308 nm were 0.81 for N-(2-nitrobenzyl)urea, 0.64 for N-(alpha-methyl-2-nitrobenzyl)urea, and 0.56 for N-(alpha-carboxy-2-nitrobenzyl)urea. The caged N-(alpha-carboxy-2-nitrobenzyl)urea is not a substrate of the enzyme urease, while the photolytically released urea is. Also, neither this caged urea nor its photolytic side products inhibit hydrolysis of free urea by urease. Thus, the alpha-carboxy-2-nitrobenzyl derivative of urea is suitable for mechanistic investigations of the enzyme urease.  相似文献   

13.
Zusammenfassung Die relativen Basizitätskonstanten von 5H-Dibenzo(a,h)phenoxazon-(5) (I) (K=3,2 · 10–2), 5H-Dibenzo(a,j)phenoxazon-(5) (II) (K=6,5 · 10–2), 9-(N-1-Naphthylamino)-5H-dibenzo(a,j)phenoxazon-(5) (III) (K=1,12), 9-(N-2-Naphthylamino)-5H-dibenzo(a, j)phenoxazon-(S) (IV) (K=1,22), 9-Anilino-5H-dibenzo(a,j) phenoxazon-(5) (V) (K=1,28) und 9-(p-Tolylamino)-5H-dibenzo(a,j)phenoxazon-(5) (VI) (K=1,45) wurden für das Puffersystem Acetat-Antipyrinperchlorat in wasserfreier Essigsäure bestimmt. Die Verbindungen II, V und VI wurden zur visuellen Indikation von Titrationen schwacher Basen mit Perchlorsäure in wasserfreier Essigsäure benutzt. Mit Indicator II können Basen mit pKa(H2O)-Werten von 2–4 und mit den Indicatoren V und VI stärkere Basen mit pKa(H2O)-Werten von 4–7 bestimmt werden.
Dibenzophenoxazone-(5)-derivatives as neutralisation indicators in non-aqueous acetic acid
The relative basicity constants of 5H-dibenzo(a,h)phenoxazone-(5) (I) (K=3.2×10–2), 5H-dibenzo(a,j)phenoxazone-(5) (II) (K=6.5×10–2), 9-(N-1-naphthylamino)-5H-dibenzo(a,j)phenoxazone-(5) (III) (K=1.12), 9-(N-2-naphthylamino)-5H-dibenzo(a,j)phenoxazone-(5) (IV) (K=1.22), 9-anilino-5H-dibenzo(a,j)phenoxazone-(5) (V) (K=1.28) and 9-(p-tolylamino)-5H-dibenzo(a,j)phenoxazone-(5) (VI) (K=1.45) have been determined with respect to the buffer system antipyrine acetate-antipyrine perchlorate in non-aqueous acetic acid. The compounds II, V and VI were employed for visual indication of titrations of weak bases with perchloric acid in non-aqueous acetic acid. Indicator II is convenient for the titration of bases with pK a (H2O) values 2–4 and indicators V and VI for bases with pKa(H2O) values 4–7.
  相似文献   

14.
[N-(2-Furoyl)-, N-(5-methyl-2-furoyl)-, N-(5-chloro-2-furoyl)-, N-(5-bromo-2-furoyl)-, N-(5-iodo-2-furoyl)-, N-(5-nitro-2-furoyl)-, and N-(tetrahydro-2-furoyl) ureas were obtained by acylation of urea with the corresponding acid chlorides.For part XXXIV, see [23].  相似文献   

15.
An organocatalytic asymmetric Michael addition of ketones to alkylidene malonates has been developed. In the presence of 20 mol % of urea 1a or N-(pyrrolidin-2-ylmethyl)trifluoromethanesulfonamide 1j, the reactions of ketones with alkylidene malonates afford the desired Michael adducts in moderate to good yields with good to high enantioselectivities under mild conditions.  相似文献   

16.
胥杨  薛思佳  孙晋峰  方治坤  尹安琴  陈龙 《有机化学》2008,28(11):1997-2000
以5-邻氯苯基-2-呋喃甲酰氯和丙氨酸为起始原料, 通过非均相法得到N-(5-邻氯苯基-2-呋喃甲酰氨基)丙氨酸, 再与10种不同取代苯胺反应, 通过N,N’-二环己基碳二亚胺和4-二甲氨基吡啶(DCC/DMAP)偶合法设计合成了10个未见文献报道的N-(5-邻氯苯基-2-呋喃甲酰氨基)丙氨酰胺类衍生物4a~4j. 通过元素分析, 1H NMR, IR 和MS确定化合物的结构, 初步生物活性测试表明标题化合物具有一定的除草活性.  相似文献   

17.
Abstract

The occurence of isoproturon [N-(4-isopropylphenyl)-N′, N′-dimethyl urea] and its metabolites was investigated in soil solution, runoff and creek water from a farm in Scheyern (Bavaria, FRG) after a heavy rainfall event following the application in spring 1994. The analytical procedure included enrichment by C 18 solid-phase extraction and reversed-phase HPLC with diode array detection. The major degradation product in most of the samples was identified as 2-hydroxy-isoproturon [N-(4-(2-hydroxyisopropyl)-phenyl)-N′. N′ dimethyl urea] using the authentic compound. The latter has been isolated from wheat cell culture medium and its structure elucidated by NMR and MS. Furthermore, the polar metabolites monodesmethyl-isoproturon [N-′ (4-Isopropylphenyl)-N′-methyl urea] and 2-hydroxy-monodesmethyl-isoproturon [N-(4-Isopropylphenyl)-N′-methyl urea] and 2-hydroxy-monodesmethyl-isoproturon [N-(4-(2-hydroxyisopropyl)-phenyl)-N′-methyl urea] were identified by comparison of their retention times and DAD-UV spectra with reference compounds.

The detection of isoproturon in soil solution down to 170 cm depth and in creek water in concentrations exceeding 4 μg/1 and also of the polar metabolites in concentrations up to 0,9 μg/1 indicated the mobility of this phenylurea herbicide and its degradation products. Therefore the metabolites should be considered in studies on the migration of isoproturon and in the ecotoxicological evaluation.  相似文献   

18.
A new series of 1‐(5‐(benzylsulfinyl)‐3‐methyl‐1,3,4‐thiadiazol‐2(3H)‐ylidene)‐thiourea/urea derivatives ( 1a – j ) were designed and synthesized. For the first time, (i) a new process was developed for N‐methylation of 1,3,4‐thiadiazole moiety using dimethyl carbonate an environmentally benign reagent in presence of N,N,N′,N‐tetramethylethylenediamine and (ii) the sulfide was selectively oxidized to sulfoxide in higher yield by using chlorine (g) in aqueous acetic acid media under mild reaction condition. The synthesized compounds ( 1a – j ) were investigated for their antimicrobial activities. The tested compounds ( 1a – j ) were exhibited moderate to excellent antibacterial activities against both Gram‐positive and Gram‐negative bacterial strains. The same compounds exhibited good antifungal activities against selected fungal strains. Particularly, the compounds 1b , 1d , 1h , and 1i were proved to be promising leads exhibiting both antibacterial and antifungal activities compared with standard drugs, ciprofloxacin, and fluconazole. The presence of 1,3,4‐thiadiazole moiety has a significant role in the display of antimicrobial activity. In addition, the presence of both sulfinyl and thiourea or urea functionalities has enhanced the activity as per obtained antimicrobial activity data.  相似文献   

19.
Methods for the introduction of a radioactive 13C label into N-(2-chlorophenyl-sulfonyl)-N'-(4-methoxy-6-methyl-1,3,5-triazin-2-yl)urea, which has herbicidal activity, are described.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 5, pp. 654–656, May, 1989.  相似文献   

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