共查询到20条相似文献,搜索用时 187 毫秒
1.
2.
为了寻求新的N-芳基吡唑类先导化合物, 用5种拟除虫菊酯类农药的活性基团——菊酸与高活性杀虫剂氟虫腈和其中间体5-氨基-3-氰基-1-(2,6-二氯-4-三氟甲基-苯基)吡唑在其氨基位置采用亚结构对接的方法合成得到了10个新的芳基吡唑菊酰胺类化合物. 经1H NMR, ESI-MS和元素分析对化合物的结构进行了表征. 初步生物活性测定结果表明, 在37.5 mg/L浓度下, N-[3-氰基-1-(2,6-二氯-4-三氟甲基苯基)-4-(三氟甲基亚磺酰基)-1H-吡咯-5-基]-3-(2,2-二氯乙烯基)-2,2-二甲基环丙酰胺(3b)对小菜蛾Amaranthus spinosus抑制活性达到100%, LC50为15.1 mg/L. 初步雌雄大鼠急性经口毒性综合评价属中毒级, 同时还检测了2-(4-氯苯基)-N-[3-氰基-1-(2,6-二氯-4-三氟甲基苯基)-1H-吡唑-5-基]-3-甲基丁酰胺(3i)的晶体结构. 相似文献
3.
4.
5.
对近年来手性2-氨基-1-苯基乙醇类药物的不对称合成方法进行了总结和概述. 重点介绍了不对称氢化、CBS还原、不对称Henry反应等新方法在2-氨基-1-苯基乙醇类药物如R-沙丁胺醇、R-沙美特罗和D-索他洛尔等合成中的应用. 相似文献
6.
离子液体中6-(2,3-环氧丙氧基)-2(1H)-喹啉酮及其衍生物的合成 总被引:3,自引:2,他引:3
6-(3-氨基-2-羟基丙基)-2-(1H)-喹啉酮衍生物被发现具有新的正性肌力的活性. 设计合成了一系列新的氨丙醇类喹啉酮化合物. 首先研究了6-羟基-2-(1H)-喹啉酮环氧化物2在离子液体中的合成, 该反应后处理简便, 收率高, 对环境友好. 然后用合成得到的2-(1H)-喹啉酮环氧化合物在离子液体中与一系列具有生物活性的有机碱反应, 合成了氨丙醇类2-(1H)-喹啉酮化合物3. 然后由6-羟基-2-(1H)-喹啉酮出发, 在离子液体中, 进行了一锅法合成氨丙醇类2-(1H)-喹啉酮化合物的研究. 制得的2b, 3b~3f 6个新化合物用IR, 1H NMR, MS和元素分析进行了结构表征. 相似文献
7.
8.
9.
10.
11.
Victoria A. Ivolgina Margarita S. Chernov’yants Leonid D. Popov Vitaliy V. Suslonov Natalya A. Avtushenko Nikolay V. Luanguzov 《Phosphorus, sulfur, and silicon and the related elements》2020,195(5):421-428
AbstractAs a part of investigation of thyreostatic activity of mercapto-substituted triazoles, the structure, spectroscopic properties of 4-amino-5-(furan-2-yl)-4H-1,2,4-triazole-3-thione were obtained. 4-amino-5-(furan-2-yl)-4H-1,2,4-triazole-3-thione forms steady charge-transfer complex in dilute chloroform solution, coordinating one iodine molecule (lgβ?=?3.47). The reaction product of 4-amino-5-(furan-2-yl)-4H-1,2,4-triazole-3-thione is presented by uncharged adduct: C6H6N4OS·I2. The crystal structure of the adduct was studied in detail by single crystal X-ray diffraction. The results of thermogravimetric analysis revealed the stability of adduct in a solid state at the temperature range 50–500?°C. 相似文献
12.
Michael reactions of isopropylidenemalononitrile with cyanothioacetamide (in the presence of 4-methoxyphenacyl bromide), cyclohexane-1,3-dione, and 4-hydroxycoumarin, gave 6-amino-2-(4-methoxy-benzoylmethylsulfanyl)-4,4-dimethyl-1,4-dihydropyridine-3,5-dicarbonitrile, 2-amino-4,4-dimethyl-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile, and 2-amino-4,4-dimethyl-5-oxo-4H,5H-pyrano[3,2-c]-chromene-3-carbonitrile, respectively. In the reaction of isopropylidenemalononitrile with cyanoacetamide, only dimerization product of the former, 2-amino-4,6,6-trimethylcyclohexa-2,4-diene-1,1,3-tricarbonitrile, was isolated. Its structure was proved by X-ray analysis. 相似文献
13.
Cyril Prknyi Hui Liang Yuan Nam Sook Cho Jin-Hwa J. Jaw Tamar E. Woodhouse Thomas L. Aung 《Journal of heterocyclic chemistry》1989,26(5):1331-1334
The synthesis of two new acyclic nucleoside analogs, 2-(2′,3′-dihydroxypropyl)-5-amino-2H-1,2,4-thiadiazol-3-one (1) and 3-(2′,3′-dihydroxypropyl)-5-amino-3H-1,3,4-thiadiazol-2-one (2), is reported. The first compound, 1, was obtained by reaction of 3-chloro-1,2-propanediol with the sodium salt of 5-amino-2H-1,2,4-thiadiazol-3-one (3) in anhydrous dimethylformamide. Similarly, 5-amino-3H-1,3,4-thiadiazol-2-one (4) reacted with 3-chloro-1,2-propanediol to give 2. The thiadiazole 4 was prepared by condensation-cyclization of hydrazothiodicarbonamide (9). 相似文献
14.
YANG Hui QIU Guo-fu FENG Xichun HE Jian-she HU Xian-ming **College of Pharmacy Wuhan University Wuhan P. R. China 《高等学校化学研究》2002,18(4)
IntroductionChloramphenicol,which was isolated fromStreptomyces venezuelae in 1 947[1] ,is used as abroad- spectrum antibiotic possessing activityagainst many Gram- negative and Gram- positivemicroorganisms. (± ) - 2 - Acetamido- 3 - hydroxy- 1 -(4- nitrophenyl) - 1 - propanone[(± ) - 1 ]is one of theintermediates of producing chloramphenicol.Petrow et al.[2 ] reported some transformations of(± ) - 1 in hydrolysis reactions. However,thereaction products were complicated under multiplehydr… 相似文献
15.
A simple, novel, and efficient route for the synthesis of 5-amino-3-aryl-1-(tert-butyl)-1H-pyrazole-4-carboxamides 1 has been devised. Preparation of pyrazole bromide 3 from potassium tricyanomethanide can be accomplished in only two steps in good yield and features a selective Sandmeyer reaction on the corresponding diaminopyrazole. This allows for a more versatile synthesis of 5-amino-3-aryl-1-(tert-butyl)-1H-pyrazole-4-carboxamides 1 than was previously possible. 相似文献
16.
1-Aryl-5-amino-4-(cyanoformimidoyl)imidazoles 2 were reacted with malononitrile under mild experimental conditions and led to 3-aryl-5,7-diamino-6-cyano-3H-imidazo[4,5-b]pyridines 5, when the reaction was carried out in the presence of DBU, or to 3-aryl-5-amino-6,7-dicyano-3H-imidazo[4,5-b]pyridines 3, in its absence. Both reactions evolved from the adduct formed by nucleophilic attack of the malononitrile anion to the carbon of the cyanoformimidoyl substituent. A 5-amino-1-aryl-4-(1-amino-2,2-dicyanovinyl)imidazole 4 was isolated when this reaction was carried out in the presence of DBU. The structure of compound 4 was confirmed by spectroscopic methods and by reaction with triethyl orthoformate and with acetic anhydride, leading respectively to 9-aryl-6-(cyanomethylidene)purines 11 and 12. Imidazole 2b was also reacted with ethyl acetoacetate, a carbon acid with a pK(a) comparable to that of malononitrile. Similar reaction conditions were used and the product isolated was a 6-carbamoyl-1,2-dihydropurine 10, showing that a different mechanism was operating in this case. 相似文献
17.
介绍了一种简单的制备(1R,3S)-3-氨基1环己烷羧酸的方法。以环己烷-1,3-二羧酸的顺反混合物为原料。经过关环得顺式的酸酐,然后酯化,在脂肪酶AY-30的作用下进行去对称性水解。得光学活性的环己烷-1,3-二羧酸的单乙酯产物,经过改进的Curtis重排反应后,羧酸基团转变为氨基。然后经过酯水解、去保护基团,得到光学纯的(1R,3S)-3-氨基-1-环己烷羧酸。 相似文献
18.
Andrzej GondelaKrzysztof Walczak 《Tetrahedron letters》2003,44(39):7291-7293
Novel 1-(dihydroxypropyl)-5-substituted uracils were synthesized in the reaction of 1-(4-nitrophenyl)-5-substituted uracil derivatives with appropriate aminopropanediols under mild conditions. In the case of 3-amino-1,2-propanediol both racemic and enantiomerically enriched products were obtained. These compounds may be considered as new building blocks for oligonucleotide synthesis. 相似文献
19.
Alberto Bargagna Pietro Schenone Francesco Bondavalli Mario Longobardi 《Journal of heterocyclic chemistry》1980,17(6):1201-1206
Cycloaddition of sulfene to N,N-disubstituted 3-amino-2-methyl-1-phenyl-2-propen-1-ones (I) and 3-amino-1,2-diphenyl-2-propen-1-ones (II) occurred in good to moderate yield only in the case of aliphatic N-substitution to give 4-dialkylamino-3,4-dihydro-(5-methyl-6-phenyl)(5,6-diphenyl)-1,2-oxathiin 2,2-dioxides. Polar 1,4-cycloaddition of dichloroketene to I and II occurred only in the former case, giving in good to moderate yield N,N-disubstituted 4-amino-3,3-dichloro-3,4-dihydro-5-methyl-6-phenyl-2H-pyran-2-ones which were dehydrochlorinated with DBN to N,N-disubstituted 4-amino-3-chloro-5-methyl-6-phenyl-2H-pyran-2-ones. In the reaction of 2-methyl-1-phenyl-3-diphenylamino-2-propen-1-one with dichloroketene, a product was isolated which was proven by uv, ir, nmr and chemical evidence to be the dipolar ion VI, the supposed intermediate of the polar 1,4-cycloaddition of dichloroketene to N,N-disubstituted enaminones. 相似文献
20.
Dzygiel A Rzeszotarska B Masiukiewicz E Cmoch P Kamieński B 《Chemical & pharmaceutical bulletin》2004,52(2):192-198
Methyl 5-amino-1H-[1,2,4]triazole-3-carboxylate hydrochloride (1). and free ester (2). were obtained and 2 was reacted with Ac(2)O to give the acetylated products 3-6. Compounds 1-6 were studied using HPLC, GC-MS, FTIR and multinuclear NMR spectroscopy, including the cross-polarisation magic angle spinning (CPMAS) technique. The results of the acetylation of 2 were compared to those of the acetylation of 5-amino-1H-[1,2,4]triazole, and for 2 a significant decrease in the susceptibility to acetylation was found. The reaction of 2 with Ac(2)O at 20 degrees C, regardless of the amount and the concentration of the latter, including neat Ac(2)O, proceeds fully regioselectively and leads to one product: methyl 1-acetyl-5-amino-1H-[1,2,4]triazole-3-carboxylate (3). In sharp contrast to 5-amino-1H-[1,2,4]triazole, neither an additional monoacetylated isomer, whether annular or exocyclic, nor any diacetylated derivative could be detected. The diacetylation of 2 requires the process to be carried out in neat boiling Ac(2)O and, as in the case of 5-amino-1H-[1,2,4]triazole, gives two diacetylated isomers. These are methyl 1-acetyl-3-(acetylamino)-1H-[1,2,4]triazole-5-carboxylate (4) and 1-acetyl-5-(acetylamino)-1H-[1,2,4]triazole-3-carboxylate (5). Hypothetical pathways of their formation have been suggested. A mixture of 4 and 5 upon hydrolysis of the ring acetyl group gives the monoacetylated derivative methyl 5-(acetylamino)-1H-[1,2,4]triazole-3-carboxylate (6). The spectroscopic, structural and conformational characteristics of compounds 1-6 have been given and methods for their preparation have been provided. 相似文献