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1-β-D-呋喃核糖基-1,2,4-三唑-3-酰胺铂配合物的合成研究 总被引:1,自引:0,他引:1
cis-[Pt(DMSO)2Cl2], K[Pt(DMSO)Cl3]分别与两摩尔1-β-D-呋喃核糖基-1,2,4-三唑-3-酰胺(Ribavirin)进行络合反应, 制得了高收率的二配位铂配合物; 讨论了不同摩尔的1-β-D-呋喃核糖基-1,2,4-三唑-3-酰胺与cis-[Pt(DMSO)2Cl2]和K[Pt(DMSO)Cl3]进行络合反应的结果; 对[Pt (N4,N7-Ribavirin)(DMSO)Cl]配合物(1)的X衍射晶体结构进行了测定. 相似文献
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合欢皮中两个新八糖苷的分离鉴定和活性研究 总被引:2,自引:0,他引:2
从合欢皮95%乙醇提取物中分离得到2个新的八糖苷(1, 2), 经化学方法与光谱分析将其结构鉴定为3-O-[β-D-吡喃木糖基-(1→2)-α-L-吡喃阿拉伯糖基-(1→6)-β-D-吡喃葡萄糖基]-21-O-[(6S)-2-反式-2-羟甲基-6-甲基-6-O-β-D-吡喃鸡纳糖基-2,7-辛二烯酸基]-金合欢酸-28-O-β-D-吡喃葡萄糖基-(1→3)-[α-L-呋喃阿拉伯糖基-(1→4)]-α-L-吡喃鼠李糖基-
(1→2)-β-D-吡喃葡萄糖基酯(1)和3-O-[β-D-吡喃木糖基-(1→2)-α-L-吡喃阿拉伯糖基-(1→6)-β-D-2-去氧-2-乙酰氨基吡喃葡萄糖基]-21-O-[(6S)-2-反式-2-羟甲基-6-甲基-6-O-β-D-吡喃鸡纳糖基-2,7-辛二烯酸基]-金合欢酸-28-O-β-D-吡喃葡萄糖基-(1→3)-[α-L-呋喃阿拉伯糖基-(1→4)]-α-L-吡喃鼠李糖基-(1→2)-β-D-吡喃葡萄糖基酯(2), 分别命名为合欢皂苷J25 (1, Julibroside J25)和合欢皂苷J22 (2, Julibroside J22). 1和2在体外对4种人癌细胞增殖有明显的抑制作用. 相似文献
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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
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以豆腐果苷为原料, 在冰醋酸催化下和邻苯二胺缩合生成中间体2-(4-β-D-吡喃阿洛糖苷-苯基)-苯并咪唑(2), 2与卤代烃在K2CO3作用下以乙醇为溶剂合成了一系列1-烃基-2-(4-β-D-吡喃阿洛糖苷-苯基)-苯并咪唑类化合物3a~3h. 新化合物2和3a~3h的结构经1H NMR, IR和MS (HRMS)确认, 并对2和3a~3h进行了药理活性筛选. 结果表明, 部分化合物具有良好的镇静活性; 其中化合物2 (100 mg•kg-1), 3f (100 mg•kg-1)与豆腐果苷相比较具有更强的药理活性. 相似文献
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黑龙骨中两个新强心苷的结构鉴定 总被引:1,自引:0,他引:1
系统研究黑龙骨Periploca forrestii Schltr.中的化学成分, 利用各种色谱技术进行分离, 得到2个新类型的强心苷,黑龙骨苷甲和乙. 并通过化学和光谱方法(MS, 1H, 13C NMR和2D NMR)鉴定其结构为: 5β-羟基-8,14β-环氧-强心 甾- 20(22)-烯-3-O-β-D-磁麻吡喃糖苷(1)和5β-羟基-8,14β-环氧-强心甾-20(22)-烯-3-O-β-D-葡萄吡喃糖基-(1→4)-β-D-磁麻吡喃糖苷(2). 相似文献
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N-烷基/芳基-N'-(4-芳基噻唑-2-基)-N"-糖基胍的合成及生物活性研究 总被引:3,自引:1,他引:3
2,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖基异硫氰酸酯(1)与2-氨基-4-取代苯基噻唑(2a~2b)反应, 生成糖基硫脲衍生物3a~3b, 再在伯胺存在下经氯化汞脱硫, 得到一系列新的N-烷基/芳基-N'-(4-芳基噻唑-2-基)-N"-糖基胍类化合物(4a~4e, 5a~5e). 所有新化合物的结构均经IR, 1H NMR, MS谱和元素分析证实, 所得产物均为β-构型. 生物活性测试结果表明, 化合物4b和5d对HIV-1 PR表现出了较高的抑制活性. 相似文献
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以豆腐果苷为原料, 与盐酸羟胺缩合反应生成4-β-D-吡喃阿洛糖苷-苯甲醛肟(2), 2与次氯酸叔丁酯发生取代反应生成4-β-D-吡喃阿洛糖苷-α-氯苯甲醛肟(3); 再将3与Schiff碱通过1,3-偶极环加成生成一系列3-(4-β-D-吡喃阿洛糖苷-苯基)-4-芳基-5-芳基-1,2,4-噁二唑啉(5a~5h). 3和 5a~5h共9个化合物均未见文献报道, 其结构经1H NMR, IR和MS (HRMS)加以确认, 并对5a~5h进行了药理活性筛选. 结果表明, 部分化合物具有良好的镇静活性. 其中, 化合物5g (200, 100 mg•kg-1)和5h (200, 100 mg•kg-1)与豆腐果苷相比较具有更强的活性. 相似文献
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A series of eight N1-(β-D-ribofuranosyl)-C4-(coumarin-4′′-yl)-1,2,3-triazoles have been synthesized by Cu(I)-catalyzed click reaction of 1-azido-1-deoxy-2,3,5-tri-O-benzoyl-β-D-ribofuranose with differently substituted 4-ethynylcoumarins followed by debenzoylation of the resulted N1-(2′,3′,5′-tri-O-benzoyl-β-D-ribofuranosyl)-C4-(coumarin-4″-yl)-1,2,3-triazoles in 71 to 89% overall yields. The structures of all the synthesized compounds were established on the basis of their spectral data analysis that was further confirmed by X-ray data analysis of one of the model benzoylated compounds, i.e. N1-(2′,3′,5′-tri-O-benzoyl-β-D-ribofuranosyl)-C4-(7″-isopropoxycoumarin-4″-yl)-1,2,3-triazole. 相似文献
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以已知的2,3,4,6-四-O-苯甲酰基--D-葡萄吡喃糖-(13)-[2,3,4,6-四-O-苯甲酰基-β-D-葡萄吡喃糖-(16)]-2,4-
二-O-乙酰基-β-D-葡萄吡喃糖-(13)-2,4,6-三-O-乙酰基-α-D-葡萄吡喃糖三氯乙酰亚胺酯(2)为供体, 以2-O-苯甲酰
基-4,6-O-苄叉基-α-D-葡萄吡喃糖烯丙基苷(4)作为受体, 立体专一性地偶联得到β-1,3连接的五糖5. 五糖5酸解脱去4,6-苯亚甲基基后与2,3,4,6-四-O-苯甲酰基-α-D-葡萄吡喃糖三氯乙酰亚胺酯(7)偶联, 区域和立体专一性地得到全保护的β-1,3主链β-1,6支链的六糖8. 六糖8脱保护后得到目标化合物香菇多糖核心片段六糖9. 发展了合成该类化合物的一种新方法. 相似文献
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Nucleosides: Synthesis of Some New Naphthimidazole Ribonucleosides as Potential Antibacterial Agents
Reaction of 2-trifluoromethyl- or 2-cyanonaphth[2,3-d] imidazole (1 or 2) with 1-O-acetyl-2,3,5-tri-O- benzoyl-β-D-ribofuranose (3), using the triflate or fusion method afforded 2-trifluoromethyl-1-(2,3,5-tri- O-benzoyl-α-D- or -β-D-ribofuranosyl)naphth[2,3-d]imidazole (4 or 6) and 2-cyano-1-(2,3,5-tri-O-benzoyl-α-D- or β-D-ribofuranosyl)naphth[2,3,-d] imidazole (5 or 7), respectively. The products 4 and 5 or 6 and 7 were separated by chromatography on silica gel. Treatment of the blocked nucleosides 4-7 with methanolic NH3 at 0 °C furnished the deblocked nucleosides 8-11 respectively. Treatment of 10 with 5% NH3 (aq) at 60 °C gave 11. Structural elucidation is based on elemental analysis, UV, FAB-MS and 1H NMR spectra. Compounds 4-11 were subjected to antibacteial testing. Compounds 5, 7 and 10 have significant activity against Staphylococous aureus (gram positive) and Esherichia coli (gram negative) bacteria, whereas the other tested compounds showed no significant activity. 相似文献
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Abstract Conformational investigations using 1D TOCSY and ROESY 1H NMR experiments on 1,3,4,6-tetra-O-acetyl-2-C-(4,6-di-O-acetyl-2,3-dideoxy-α-D-erythro-hexopyranosyl)-2-deoxy-β-D-glucopyranose (8) and related disaccharides showed that for steric reasons the C-linked hexopyranosyl ring occurs in the usually unfavoured 1C4 conformation and reconfirmed the structure of 1,3,4,6-tetra-O-acetyl-2-C-(4,6-di-O-acetyl-2,3-dideoxy-α-D-erythro-hex-2-enopyranosyl)-2-deoxy-β-D-glucopyranose (5). Glycosylation of 2,3,6-tri-O-benzyl-α-D-glucopyranosyl 2,3-di-O-benzyl-4,6-(R)-O-benzylidene-α-D-glucopyranoside (13) with acetate 8 using trimethylsilyl triflate as a catalyst afforded the α-D-linked tetrasaccharide 14. A remarkable side product in this reaction was the unsaturated tetrasaccharide 2,3,6-tri-O-benzyl-4-O-[4,6-di-O-acetyl-2,3-dideoxy-2-C-(4,6-di-O-acetyl-2,3-dideoxy-β-D-erythro-hexopyranosyl)-α-D-erythro-hex-2-enopyranosyl]-α-D-glucopyranosyl 2,3-di-O-benzyl-4,6-(R)-O-benzylidene-α-D-glucopyranoside (16) where in the C-linked hexopyranosyl ring an isomerization to the β-anomer had taken place to allow for the favoured 4C1 conformation. The tetrasaccharide 14 was deacetylated and hydrogenolyzed to form the fully deprotected tetrasaccharide 18. The 1 C 4 conformation of the C-glycosidic pyranose of this tetrasaccharide was maintained as shown by an in depth NMR analysis of its peracetate 19. 相似文献
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《Journal of carbohydrate chemistry》2013,32(3-4):275-283
New oxamides, derivatives of D-glucosamine and aliphatic or aromatic amines were prepared by acylation of methyl 3,4,6-tri-O-acetyl-2-acetamido-2-deoxy-α- or -β-D-glucopyranoside (1c or 1d) with oxalyl chloride, followed by reaction with amine. The reaction was assumed to proceed by the intermediate of N-carbomethoxy N-(methyl 3,4,6-tri-O-acetyl-2-deoxy-α or β-D-glucopyranosid-2-yl) oxamic acid chloride which reacted with amines, and afforded N-acetyl, N-(methyl 3,4,6-tri-O-acetyl-2-deoxy-α- or -β-D-glucopyranosid-2-yl), N′-alkyl or aryloxamide (5–7), and N-(methyl 3,4,6-tri-O-acetyl-2-deoxy-α- or -β-D-glucopyranosid-2-yl), N′-alkyl or aryloxamide (8–13). 相似文献
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Kiyotaka Yoshii Yoshihiro Ohba Tarozaemon Nishiwaki 《Journal of heterocyclic chemistry》1993,30(1):141-144
The reaction of the silylated base of 1,2-benzisoxazol-3(2H)-one ( 1 ) and its 7-methyl derivative 5 and 5-methyl-1,2-benzisothiazol-3(2H)-one ( 9 ), respectively, with 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose followed by basic deprotection gave the corresponding β-D-ribonucleosides, and the silylated base of 1 , when treated with 1-O-acetyl-2,3,5-tri-O-benzoyl-α-D-arabinofuranose in the presence of stannic chloride, afforded the corresponding α-arabinonucleoside. Structural proofs of these nucleosides are provided from elemental analyses and 1H and 13C nmr spectra. 相似文献
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Y. H. R. Jois C. D. Kwong J. M. Riordan J. A. Montgomery J. A. Secrist 《Journal of heterocyclic chemistry》1993,30(5):1289-1292
Ribosylation of 3-amino-5H-[1,2,4]triazolo[4,3-b][1,2,4]triazole ( 1 ) with l-O-acetyl-2,3,5-tri-O-benzoyl-D-ribofuranose and stannic chloride resulted in the following protected nucleoside analogs: 3-amino-1-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl)[1,2,4]triazolo[4,3-β][1,2,4]triazole ( 4 ), 3-amino-1-(2,3,5-tri-O-benzoyl-α-D-ribofuranosyl)[1,2,4]triazolo[4,3-β][1,2,4]triazole ( 5 ), 3-amino-1-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl)[1,2,4]triazolo[4,3-β][1,2,4]triazole ( 5 ), and 3-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl) amino-5H-[1,2,4]triazolo[4,3-b]-[1,2,4]triazole ( 7 ). Compounds 4–6 were deprotected to 3-amino-1-β-D-ribofuranosyl[1,2,4]triazolo[4,3-b][1,2,4]-triazole ( 3 ), 3-amino-1-α-D-ribofuranosyl[1,2,4]triazolo[4,5-b][1,2,4]triazole ( 8 ), and 3-imino-2H-2-β-D-ribo-furanosyl[1,2,4]triazolo[4,3-b][1,2,4]triazole ( 9 ), while 7 could not be deprotected without decomposition. Compounds 1, 4, 6, 7 , and 9 were screened and found to have no antiviral activity. 相似文献