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1.
Santhosh Penta Kranthi Kumar Gadidasu Srinivas Basavoju Vedula Rajeswar Rao 《Tetrahedron letters》2013
A series of simple or/and aryl, heteryl hydrazono pyrazolyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-6-yl)-2H-pyran-2-one derivatives have been efficiently synthesized in excellent yields via one-pot, multi-component approach. The importance of this methodology is that in a one-pot operation four new bonds (3C–N and 1C–S) are generated. The structure of compound 5a was confirmed by single-crystal X-ray diffraction. The newly synthesized compounds were evaluated for their in vitro antimicrobial activity against gram-positive bacteria (Staphylococcusaureus and Bacillussubtilis), gram-negative bacteria (Escherichiacoli andKlebsiellapneumoniae), antifungal activity against Candida albicans, and nematicidal activity against Meloidogyneincognita. Among all the compounds 6f showed excellent antimicrobial and nematicidal activity against tested bacteria, fungi, and nematodes. 相似文献
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V. A. Yanchenko A. M. Demchenko M. O. Lozinskii 《Chemistry of Heterocyclic Compounds》2004,40(4):516-518
We propose a method for obtaining derivatives of 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine by alkylation of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol by substituted -chloroacetanilides, followed by cyclization of the intermediate by phosphorus oxychloride. 相似文献
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This study presents an efficient synthesis of 3-[6-(substituted-phenyl)-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazol-3-yl]-1H-indazole via dehydrative condensation with cyclization of 4-amino-5-(1H-indazol-3-yl)-4H-[1,2,4]triazole-3-thiol and fluorinated or nonfluorinated carboxylic acids in presence of phosphorous oxychloride. The multistep reaction pathway proceeds through different compounds. Present synthesis has the advantages of easily accessible starting materials, convenient synthesis, simple reaction condition, wider substrate scope, and higher yield (75% to 90% isolated). 相似文献
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ω-溴代芳香基乙酮与3-(D-葡萄糖-1-基)-4-氨基-5-巯基-1,2,4-三唑反应 合成了一系列新颖的3-(D-葡萄糖-1-基)-6-芳基-7H-1,2,4三唑并[3,4-b[1,3 ,4]噻二嗪.用元素分析,IR,NMR,MS对其结构进行了表征,研究了其NMR波谱特 征,并以^1H-^1H COSY,^13C-^1H COSY,COLOC二维NMR技术对其^1H NMR,^13C NMR的谱峰进行了全归属 相似文献
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3-苯氧甲基-6-(2,4-二氟苯基)-7H-1,2,4-三唑并[3,4-b][1,3,4]噻二嗪的合成与晶体结构研究 总被引:2,自引:0,他引:2
由苯氧乙酸出发,经多步反应,制得3-苯氧甲基-4-氨基-5-巯基-1,2, 4-三唑,它与2-氯-2',4'-二氟苯乙酮进行环化反应,生成3-苯氧甲基-6-( 2,4-二氟苯基)-7H-1,2,4-三唑并[3,4-b][1,3,4]噻二嗪,通过元素分析、红外 光谱、核磁共振氢谱与碳谱、质谱进行表征,并利用单晶X射线衍射法测定其结构 。晶体属单斜晶系、P2_(1/c)空间群,a = 1.339(3) nm, b = 1.4683(4) nm, c = 0.8606(2) nm, β = 108.49(2)°, Z = 4, F(000) = 736, R_1 = 0.0509。还 对均三唑并噻二唑两类稠杂环的晶体结构作了比较。 相似文献
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Ranjana Aggarwal Shilpa Sharma Mona Hooda Dionisia Sanz Rosa M. Claramunt Brendan Twamley Isabel Rozas 《Tetrahedron》2019,75(50):130728
The first visible-light mediated, simple, efficient and ecofriendly protocol for the regioselective synthesis of novel [1,2,4]triazolo[3,4-b][1,3,4]thiadiazines has been developed by the reaction of α-bromodiketones, generated in situ by the bromination of a diverse array of β-diketones with N-bromosuccinimide, with 4-amino-[1,2,4]triazole-3-thiols. The methodology does not require the presence of any additives and this reaction proceeded in the presence of EDG (OMe), EWG (Cl) and heteroarenes (thiophenyl) giving the expected products in good to excellent yields. A solvent free protocol was also established to accomplish the synthesis of target compounds but it required PTSA as a catalyst and yields are comparatively poor. The structure of the regioisomer has been confirmed unambiguously by heteronuclear 2D-NMR [(1H-13C) HMBC, (1H-15N) HMBC, (1H-13C) HMQC] spectroscopic and X-ray crystallographic studies. 相似文献
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Thirupaiah Bade 《合成通讯》2013,43(20):2350-2354
The synthesis of 3-(2-(5-(benzylideneamino)-3-phenyl-1H-pyrazol-1-yl)thiazol-4-yl)-4-hydroxy-6-methyl-2H-pyran-2-one derivatives was achieved through a one-pot, four-component reaction involving condensation of 3-(2-bromoacetyl)-4-hydroxy-6-methyl-2H-pyran-2-one, thiosemicarbazide, phenacylcyanaide, and various aryl aldehydes in dry alcohol and few drops of acetic acid under reflux condition. This four-component reaction has some advantages such as ease of handling, good yields, and easy workup. All structures of newly prepared compounds were confirmed by analytical and spectral data. 相似文献
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合成了18个含有1H-1,2,4-三唑的咪唑[2,1-b]-1,3,4-噻二唑以及S-三唑[3,4-b]-1,3,4-噻二唑的稠杂环衍生物,经元素分析及谱学表征,探讨2,5,6-三取代咪唑[2,1-b]-1,3,4-噻二唑的可能生成机制.对大肠杆菌、绿脓杆菌、枯草杆菌等初步抑菌试验证明,多数化合物表现了较好的抑菌活性. 相似文献
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《结构化学》2020,39(8):1531-1538
The title compound phenyl(6-phenyl-3-p-tolyl-6,7-dihydro-5 H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-7-yl)methanone(PTM), designed using 4-amino-3-p-tolyl-1H-1,2,4-triazole-5(4 H)-thione as the starting material, was successfully synthesized via a two-step synthesis route and finally characterized by NMR, FT-IR, single-crystal X-ray diffraction and mass spectrometry techniques. The crystal structure of trans-PTM was obtained from X-ray diffraction: C_(24)H_(20)N_4OS, Mr = 412.52, monoclinic system, space group P2_1/c, a = 16.650(3), b = 13.876(3), c = 8.812(2) ?, β = 100.340(3)°, V = 2002.8(7) ?~3, F(000) = 865, Z = 4, D_c = 1.3680 g/cm~3, λ = 0.71073 ?, μ = 0.186 mm~(-1) and the final R = 0.0786 for 3514 unique reflections with 2044 observed ones(Ⅰ 2σ(Ⅰ)). The biological activities of antimicrobial and regulation of plant growth of PTM were investigated. The results indicated that PTM showed weak antimicrobial activity on Bacillus pumilus, while promoted the growth of radish and inhibited that of wheat in a dose-dependent manner. Therefore, PTM may be developed as a potential drug to promote the growth of dicotyledonous plants or as an herbicide to inhibit that of monocotyledonous plants in the future. 相似文献
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The title compound 3-benzyl-6-trichloromethyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole I (C11HTC13N4S, Mr = 333.62) has been synthesized, and its structure was determined by elemental analyses, IR, ^1H NMR, ^13C NMR, and X-ray diffractions. The crystal is of triclinic, space group P1^-, with a = 5.898(3), b = 10.510(4), c = 11.580(5) A, α = 74.936(7), β= 75.476(7), γ = 79.647(7)°, V= 665.9(5)/A^3, F(000) = 336, Z= 2, Dc = 1.664 g/cm^3, 2 = 0.71073A, p = 0.834 mm^-1, the final R = 0.0605 and wR = 0.0900. The secondary bonding interactions (SBIs) S…N and π-π stacking interactions are found in the crystal structure and they link the molecules into a three-dimensional network. 相似文献
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A novel method for synthesis of 2-R-5-Ar(Het)-5,6-dihydro-7H-[1,2,4]triazolo[5,1-b][1,3]thiazin-7-ones by condensation of 3-R-4,5-dihydro-1H-1,2,4-triazole-5-thiones with 3-aryl(heteryl)-2-propenoyl chlorides is proposed. 相似文献
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Ethyl 2-amino-4-methyl-5-(1H-1,2,4-triazol-1-yl)thiophene-3-carboxylate 2, obtained from Gewald reaction of 1-(1H-1,2,4-triazol-1-yl)acetone 1 with ethyl cyanoacetate and sulfur, was transferred into iminophosphorane 3. Further reaction of 3 with aromatic isocyanates gave carbodiimides 4, which were treated subsequently with a secondary amine to give 6-(1H-1,2,4-triazol-1-yl)-thieno[2,3-d]pyrimidin-4(3H)-ones 6 in good yields in the presence of a catalytic amount of sodium ethoxide. 相似文献
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在三氯氧磷催化下, 6种3-脂肪基-1,2,4-三唑(1a~1f)和3-苯基-1,2,4-三唑(1g)分别与对苯二甲酸和2-氨基-1,4-对苯二甲酸发生环化反应, 高产率合成了14种双枝三唑并噻二唑稠环衍生物(2和3), 并对其进行了结构表征及药物活性测试. 目标化合物对Cdc25B和PTP1B抑制活性筛选结果表明, 化合物2f, 3a和3g对Cdc25B有较高的抑制活性, IC50值分别为(3.45±0.60), (0.69±0.10)和(1.52±0.19) μg/mL; 化合物3a和3b对PTP1B表现出较高的抑制活性, IC50值分别为(0.98±0.13)和(2.00±0.16) μg/mL. 相似文献
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A reaction of 3-benzylthiotriazole-4-amines with aromatic aldehydes leads to the formation of 6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines. A dihydrothiadiazine ring opening along the N-N bond occurs by the action of strong bases.
Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 6, pp. 1249–1252, June, 2008. 相似文献
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3-(2-Furanyl)indoles were firstly synthesized in a one-pot procedure by the reaction of 3-cyanoacetyl indole, aromatic aldehydes and isocyanides in ethanol in the presence of ammonium acetate. 相似文献