共查询到20条相似文献,搜索用时 750 毫秒
1.
2.
3.
4.
新型环烷烯并嘧啶并噻唑-3-酮类化合物的合成 总被引:1,自引:0,他引:1
以环戊酮、环庚酮为起始原料合成的环烷烯并[1,2-d]嘧啶-2-硫酮(2)与氯乙酸、芳香醛反应, 合成具有潜在抗癌活性的稠合杂环化合物5-芳基-2,8-二芳亚甲基-2,3,6,7-四氢-5H,8H-环戊烯并[1,2-d]噻唑并[3,2-a]嘧啶-3-酮(3)以及5-芳基-2,10-二芳亚甲基-2,3,6,7,8,9-六氢-5H,10H-环庚烯并[1,2-d]噻唑并[3,2-a]嘧啶-3-酮(4). 3和4的结构经1H NMR, IR, MS分析确认. 相似文献
5.
N-{2-氯-5-[3-甲基-2,6-二氧-4-三氟甲基-2,3-二氢嘧啶-1(6H)-基]苯基}酰胺类化合物的合成及除草活性 总被引:2,自引:0,他引:2
为了寻找高效、安全的除草活性化合物, 合成了12个全新的N-{2-氯-5-[3-甲基-2,6-二氧-4-三氟甲基-2,3-二氢嘧啶-1(6H)-基]苯基}酰胺类化合物, 其化学结构经IR, 1H NMR, LC/MS和元素分析确证. 初步生物活性测定结果表明, 该类化合物具有一定的除草活性, 如7a, 7b, 7c, 7g, 7h, 7i, 7k和7l在有效成分75 g/hm2剂量下, 茎叶处理对苘麻(Abutilon theophrasti)、刺苋(Amaranthus spinosus)等阔叶杂草具有良好的除草活性, 其抑制率达100%. 相似文献
6.
7.
通过烯丙基溴化锌对手性亚胺的两次不对称加成, 合成了光活性的双烯丙基化的新型手性二胺. 首先经N-Boc保护和Dess-Martin氧化制得了光活性的(S)-N-Boc-3-苯基-2-氨基丙醛. (S)-N-Boc-3-苯基-2-氨基丙醛与(S)-缬氨基酸甲酯缩合生成手性亚胺, 在七水合三氯化铈(CeC13•7H2O)催化以及底物的手性诱导作用下, 该手性亚胺与烯丙基溴化锌经不对称加成反应合成了高光活性的单烯丙基化手性胺. 该手性胺与2-噻吩甲醛缩合生成新的手性亚胺, 再次通过不对称烯丙基加成反应合成了含有四个手性中心的高光学纯的双烯丙基化手性二胺. 目标化合物和关键中间体的结构均被1H NMR, 13C NMR及MS确证. 相似文献
8.
以(S)-N-Boc焦谷氨酸乙酯为原料, 经DIBAL-H还原得到半缩醛, 然后经Wittig反应得到相应的烯烃, 最后氢化制得(S)-N-Boc-α-氨基庚二酸二(单)酯, 总收率为85.1%(二酯)和86.1%(单酯). 另外, 以(S)-N-Boc-哌啶-2-甲酸为原料经酯化和氧化得内酰胺, 然后经还原、Wittig反应、氢化得到(S)-N-Boc-α-氨基辛二酸二(单)酯, 总收率为72.5%(二酯)和72.4%(单酯). 产品用1H NMR, MS表征. 相似文献
9.
10.
以L-鼠李糖为起始原料, 制备1-溴-2,3,4-三-O-乙酰基-β-L-吡喃型鼠李糖, 然后在甲苯中与Pb(SCN)2作用, 得到中间体2,3,4-三-O-乙酰基-α-L-吡喃型鼠李糖基异硫氰酸酯(1). 利用2,3,4-三-O-乙酰基-α-L-吡喃型鼠李糖基异硫氰酸酯易发生亲核加成的性质, 在不同溶剂中, 与取代的苯并噻唑胺(2a~2f)、取代的苯并噻唑肼(2g~2l)、氧化和非氧化的哒嗪酮甲酰肼(2m, 2n)以及取代的嘧啶胺(2o, 2p)反应, 合成了16种新的(氨基)硫脲类化合物3a~3p. 所有化合物的结构均经IR, 1H NMR, LC-MS和元素分析确证, 并对它们的生物活性做了初步测试. 相似文献
11.
Olcay Bekircan Zekeriya Bıyıklıoğlu Irfan Acar Hakan Bektas Halit Kantekin 《Journal of organometallic chemistry》2008,693(21-22):3425-3429
The synthesis of metallophthalocyanines [6–9; M = Ni(II), Zn(II), Co(II) and Cu(II)] with four 1,2,4-triazole units obtained from 4-{(4-chloro-2-fluorobenzyl)[3-(4-chlorophenyl)-5-(4-methylphenyl)-4H-1,2,4-triazol-4-yl]amino}phthalonitrile (5) in the presence of dimethylaminoethanol and the corresponding anhydrous metal salts is described. The thermal stabilities of the Pc compounds were determined by thermogravimetric analysis. The new compounds were characterized by a combination of IR, 1H NMR, 13C NMR, UV–Vis, elemental analysis. 相似文献
12.
Hajja S. Alonazy Hassan M.A. AL-Hazimi Makarem M.S. Korraa 《Arabian Journal of Chemistry》2009,2(2):101-108
A series of 5,6-bis(4-substitutedphenyl)-2H(3)-pyridazinones 2a–f have been synthesized from the condensation of the corresponding benzil monohydrazones 1 either with ethyl cyanoacetate or diethyl malonate in ethanol. The synthesized pyridazinones were converted to the corresponding 3-chloro derivatives 3a–f by the action of phosphoryl chloride. Reaction of the latter halogenated pyridazines with various aromatic amines led to the formation of new 3-aminoaryl pyridazines (4) in moderate yield. The structures of all new compounds 2b,c,e,f, 3b–e, 4 were fully identified by the analysis of their 1H and 13C NMR and mass spectra. Some of these synthetic heterocyclic compounds were screened for their antimicrobial activities but they were almost negative. 相似文献
13.
14.
A series of new 2-[2-(2,6-dichlorophenyl)amino]phenyl methyl-3-[(5-substituted phenyl)-1,5-dihydro-1H-pyrazol-3-yl-amino]-6-iodoquinazolin-4(3H) ones (6a–m) have been synthesized by the reaction of 2-[2-(2,6-dichlorophenyl)amino]phenyl methyl-3-substituted phenyl acryl amido-6-iodoquinazolin-4(3H) ones with hydrazine hydrate in the presence of glacial acetic acid. The chalcone (5a–m) have been prepared by the condensation of 2-[2-(2,6-dichlorophenyl)amino]phenyl methyl-3-acetamido-6-iodoquinazolin-4(3H) one with different substituted aromatic aldehyde. The compound 1 on treatment with 5-iodoanthranilic acid in pyridine undergoes cyclisation gave 2-[2-(2,6-dichlorophenyl)amino]phenyl methyl-6-iodo-3,1-benzoxazin-4(3H) one (2). Treatment on benzoxazine with hydrazine hydrate gave 3-amino-2-[2-(2,6-dichlorophenyl)amino]phenyl methyl-6,8-dibromo quinazolin-4(3H) one (3) followed by acetylation synthesized 2-[2-(2,6-dichlorophenyl)amino]phenyl methyl-3-acetamido-6,8-dibromoquinazolin-4(3H)-one (4). The structure of synthesized compounds has been elucidated by IR, 1H NMR, 13C NMR and elemental analysis. The products were screened for antibacterial and antifungal activity. Among the series containing some of the compounds showed promising results against standard drugs. 相似文献
15.
Sadiq-ur-Rehman Muhammad Aziz Choudhary Moazzam H. Bhatti Saqib Ali 《Journal of the Iranian Chemical Society》2012,9(1):35-45
A new series of di- and tri-organotin(IV) compounds with the general formula R4?n SnL n , where R?=?Me (1,2), Et (3), n-Bu (4,5), n-Oct (6), Ph (7) and L?=?(E)-3-(4-methoxyphenyl)-2-(4-chlorophenyl)-2-propenoate, were synthesized by reaction of silver salt of ligand or ligand acid with diorganotin dichloride/oxide and triorganotin chloride in 2:1 and 1:1 molar ratio, respectively. These compounds were characterized by elemental analyses, FT-IR, multinuclear (1H, 13C, 119Sn) NMR and mass spectrometry. The spectroscopic results revealed that all the diorganotin(IV) compounds possess trigonal bipyramidal structures in solution and octahedral geometry in the solid state around the tin atom. A linear polymeric trigonal bipyramidal structure in the solid state and a tetrahedral environment around the tin atom in non-coordinating solvents has been proposed for the triorganotin(IV) compounds. All synthesized compounds were tested in vitro against a number of microorganisms to assess their biocidal activity. These studies revealed that ligand acid and some of its organotin compounds show promising activity against different strains of bacteria and fungi but lowered than reference drugs. 相似文献
16.
《Journal of Saudi Chemical Society》2014,18(5):735-743
A simple, highly useful synthesis of 1-(2-(4,5-dimethyl-2-phenyl-1H-imidazol-1-yl)ethyl)piperazine derivatives is achieved by a four component cyclo condensation of diacetyl, aromatic aldehyde, 2-(piperazin-1-yl)ethanamine and ammonium acetate using SO42−/Y2O3 as a catalyst in ethanol. The synthesized compounds were characterized by IR, 1H and 13C NMR and mass spectral studies. All the synthesized compounds were screened for their in vitro antimicrobial studies. Among the newly synthesized compounds 5d, 5e, 5h and 5m showed excellent antibacterial and antifungal activities when compared to the standard drugs. 相似文献
17.
Radhakrishnan Mahesh Sourabh Mundra Thangaraj Devadoss Lakshmi P. Kotra 《Arabian Journal of Chemistry》2019,12(7):1436-1446
The cysteine protease, falcipain-2 is an important drug target in human malaria parasite Plasmodium falciparum. A new series of 2-(4-(substituted benzoyl)-1,4-diazepan-1-yl)-N-phenylacetamide derivatives 5(a–t) were designed as per pharmacophoric requirements of falcipain-2 inhibitors using ligand-based approach. The target compounds were synthesized from the key intermediate, 2-(1,4-Diazepan-1-yl)-N-phenylacetamide, by coupling it with appropriate carboxylic acids using carbodiimide chemistry. Structural features of target compounds were characterized by spectral data (1H NMR, and mass) and elemental analyses. The purity of the final compounds was confirmed by HPLC. The compounds were tested for their in vitro falcipain-2 inhibitor activity on recombinant falcipain-2 enzyme. Five compounds 5b, 5g, 5h, 5j, 5k showed good inhibitory activity (>60%), against falcipain-2 at 10 μM concentration, and fifteen compounds showed weak to moderate inhibitor activity. Compound 5g, the most potent compound from this series showed 72% inhibition at 10 μM concentrations. 相似文献
18.
《Arabian Journal of Chemistry》2014,7(2):181-187
5-(4-Chlorophenyl amino)-2-mercapto-1,3,4-thiadiazole (I) was refluxed with formaldehyde and ammonium chloride in ethanol yielding the Mannich base 5-(4-chloro phenyl amino)-3-aminomethyl-2-mercapto-1,3,4-thiadiazole (II). Esterification with 4-chloro-(2,6-dinitro phenoxy)-ethyl acetate (III) under anhydrous conditions gave the intermediate (IV). Subsequent hydrazinolysis with hydrazine hydrate gave the corresponding hydrazide 3-amino methyl-5-(4-chloro phenyl amino)-2-mercapto-4′-(2′,6′-dinitro phenoxy)-acetyl hydrazide (V). The hydrazide was converted into the Schiff bases (VIa–b) by reacting with 2-chlorobenzaldehyde and 3-methoxy-4-hydroxy benzaldehyde in presence of methanol containing 2–3 drops of acetic acid. Diazotisation with aromatic amines, sulphanilic acid and sulphur drugs gave the formazans (VIIa–g) respectively. Chemical structures have been established by elemental analysis and the spectral techniques of FTIR, 1H NMR and mass. Antimicrobial activity (in vitro) was evaluated against the two pathogenic bacterial strains. Escherichia coli and Salmonella typhi, three fungal strains Aspergillus niger, Penicillium species and Candida albicans. The compounds have shown moderate activity. 相似文献
19.
The 4-(α-hydroxyalkylidene)-Δ2-5-isoxazolones2 exist in the β-ketoenol form (“vinyloge car?ylic acids”),2a,c react with guanidine and amidines to give only the enolates4, whereas they react both with hydrazines and 1,2-diamines to form the enamines6 and9 (“vinyloge amids”). The 4-(α-ethoxyalkylidene)-Δ2-5-isoxazolones 7 (“vinyloge esters”) condense with guanidine, benzamidine, and urea to affort the enamines8. Attempted ring-opening by bases failed whilst catalytic hydrogenation of the enamines6 and8 yielded the pyrazoles10,11 and diazepines12. The structures of the compounds have been elucidated by NMR and IR-spectra. 相似文献
20.
Jignesh P. Raval Krunal G. Desai Kishor R. Desai 《Journal of Saudi Chemical Society》2012,16(4):387-393
Heterocyclic compounds containing pyrazolyl-oxopropyl-quinazolin-4(3H)-one are reported to possess significant biological activity. Syntheses of 6-bromo-2-(3-chloro-2-oxopropyl)-3-(4-fluorophenyl)quinazolin-4(3H)-one 2 6-bromo-3-(4-fluorophenyl)-2-(3-hydrazinyl-2-oxopropyl)quinazolin-4(3H)-one 3 and 6-bromo-2-(3-(3-(4-(1-(2-chlorophenyl)-3-methyl-1H-pyrazol-5(4H)-ylideneamino)phenyl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-oxopropyl)-3-(4-fluorophenyl)quinazolin-4(3H)-one 5a–j using microwave irradiation have been described. These compounds have been characterized on the basis of the UV, IR, 1H NMR, 13C NMR, Mass and elemental analysis. Compounds have been evaluated for their antimicrobial activity. 相似文献