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1.
以中草药有效成分β-榄香烯为起始原料, 经烯丙位的氯代反应及亲核取代反应, 成功地合成一种含水溶性基团TEG的三齿吡啶螯合剂, 并与稳定的三羰基铼配位, 得到了一种新的三羰基铼配合物, 在此基础上利用铼的放射性同位素Re-188进行了放射性标记. 反应中间体及最终化合物分别用IR, 1H NMR, HRMS, HPLC或元素分析等技术进行表征, 并对该化合物进行了初步的体外抗癌活性研究. β-Elemene-TEG-Re(CO)3配合物的合成、放射化学合成及体外抗癌活性评价, 为探讨榄香烯体内靶点和作用机制提供了可能, 并为最终开发基于β-榄香烯的放射性药物奠定了基础.  相似文献   

2.
以中草药有效成分β-榄香烯为起始原料, 在碱性条件下与氨基化的聚乙二醇(PEG)反应合成了一系列β-榄香烯单取代PEG衍生物, 利用IR, 1H NMR及13C NMR对其结构进行了表征. 并采用WST-1法观察其对人宫颈癌细胞(Hela)、人白血病细胞(K562)的抑制作用, 探讨其体外抗肿瘤活性. 细胞实验结果表明经PEG修饰的β-榄香烯的抗癌活性有不同程度的增强.  相似文献   

3.
黄丹  鄢明  沈琪 《有机化学》2007,27(6):739-743
研究了在过渡金属配合物催化下α-重氮-β-二羰基化合物与醇的插入反应, 考察了重氮化合物的结构、醇的结构、催化剂的性质、反应溶剂和反应温度对这一反应的影响. 发现当重氮化合物与甲醇的物质的量比为1∶10, 1 mmol% Rh2(OAc)4为催化剂和回流的苯的条件下, 反应能够以高的化学产率生成α-甲氧基-β-二羰基化合物. 手性醇衍生的重氮乙酰乙酸酯反应的产物中两种非对应异构体的比例为3∶2~1∶1.  相似文献   

4.
以薯蓣皂素为原料, 经过磺酰酯化、N-溴代丁二酰亚胺(NBS)氧化加成、Pb(OAc)4远程氧化关环、消去反应、间氯过氧苯甲酸(mCPBA)氧化、高氯酸开环及锌粉还原7步反应, 合成多羟基甾体25(R)-异螺甾环-5-烯-2β,3α,19-三醇. 并用IR, 1H NMR, 13C NMR, MS及元素分析对各中间体及目标化合物进行了表征.  相似文献   

5.
徐石海  廖小建  林慧 《有机化学》2008,28(5):861-864
采用抗肿瘤活性追踪法对采自中国南海西沙群岛永兴岛柔荑软珊瑚Nephthea sp.中抗肿瘤活性成分进行研究, 报道了两种具有细胞毒活性的甾醇化合物, 经过MS, IR, 1H NMR, 13C NMR (DEPT), HSQC 和HMBC等光谱技术鉴定为: 24-甲基胆甾-5-烯-3β,8β-二醇(1)和24-亚甲基胆甾-4-烯-3β,6β-二醇(2), 化合物1为新化合物, 利用X-ray单晶衍射技术验证化合物2的立体结构. 化合物1对肝癌细胞(BEL-7402), 小鼠白血瘤细胞(P388)和人结肠癌细胞(LOVO)作用的IC50值分别为18.0, 25.5和20.6 μg/mL; 化合物2对肿瘤细胞P388和人乳腺癌细胞(MCF)作用的IC50值分别为1.0和2.5 μg/mL.  相似文献   

6.
王宏社  苗建英 《有机化学》2007,26(2):266-268
NaHSO4•SiO2作催化剂, 1,3-二羰基化合物和伯胺在室温下反应合成了一系列β-烯胺酮(酯), 该法反应条件温和, 产率高, 催化剂能回收再利用.  相似文献   

7.
肖卿  王剑波 《化学学报》2007,65(16):1733-1735
报道烯(炔)基硫醚与α-重氮羰基化合物, 在[RuCl2(p-cymene)]2催化下, 经由金属卡宾发生硫叶立德[2,3]-σ重排反应(Doyle-Kirmse反应). 在Ru(II)作用下, α-重氮羰基化合物与烯丙基硫醚的反应以较好收率生成相应的[2,3]-σ重排产物高烯丙基硫醚. 同样条件下与炔丙基硫醚的反应则生成[2,3]-σ重排产物联烯和呋喃衍生物, 后者是联烯进一步在Ru(II)作用下重排的产物.  相似文献   

8.
Aldisin及其衍生物的合成和α-葡萄糖苷酶抑制活性研究   总被引:2,自引:0,他引:2  
以三氯氧磷为环化试剂, 回流状态下, N-(2-吡咯甲酰基)-β-丙氨酸经分子内酰化环化反应, 合成了吡咯[2,3-c]氮杂二酮稠环化合物Aldisin及其衍生物1-Methylaldisin和3-Bromoaldisin, 通过1H NMR, 13C NMR, IR, FABMS和元素分析对其结构进行了表征. 以X射线衍射法研究了3-Methylaldisin的晶体结构. 测定了三个化合物对α-葡萄糖苷酶的抑制作用.  相似文献   

9.
2,4-戊二酮分别与不同的伯胺反应,合成出2种新的大空间位阻的β-二亚胺配体。其中β-二亚胺配体1与格氏试剂甲基碘化镁(MeMgI)反应得到相应四配位镁的甲基配合物,配体1的锂盐与溴化镁(MgBr2)反应制备出Mg-Li双金属溴配合物。新β-二亚胺配体和相应镁的甲基配合物和溴配合物的晶体结构均通过单晶X射线衍射确定,相应镁的甲基配合物和溴配合物在苯乙酮的硅氢化反应中显示了较好的催化活性。  相似文献   

10.
2,4-戊二酮分别与不同的伯胺反应,合成出2种新的大空间位阻的β-二亚胺配体。其中β-二亚胺配体1与格氏试剂甲基碘化镁(MeMgI)反应得到相应四配位镁的甲基配合物,配体1的锂盐与溴化镁(MgBr2)反应制备出Mg-Li双金属溴配合物。新β-二亚胺配体和相应镁的甲基配合物和溴配合物的晶体结构均通过单晶X射线衍射确定,相应镁的甲基配合物和溴配合物在苯乙酮的硅氢化反应中显示了较好的催化活性。  相似文献   

11.
王亚军  沈宗旋  张雅文 《有机化学》2006,26(9):1291-1294
用三乙胺催化环状α-酮酯和α-酮酰胺同硝基甲烷的Henry反应, 首次合成了12个多官能团的β-硝基醇, 它们的结构用元素分析、红外光谱和核磁共振进行了表征. 这一反应速度较快, 室温下进行, 条件温和, 产率较好, 是合成多官能团硝基醇的有效方法.  相似文献   

12.
Rhenium tricarbonyl complexes have been recently investigated as novel anticancer agents. However, little is understood about their mechanisms of action, as well as the means by which cancer cells respond to chronic exposure to these compounds. To gain a deeper mechanistic insight into these rhenium anticancer agents, we developed and characterized an ovarian cancer cell line that is resistant to a previously studied compound [Re(CO)3(dmphen)(ptolICN)]+, where dmphen=2,9‐dimethyl‐1,10‐phenanthroline and ptolICN=para‐tolyl isonitrile, called TRIP. This TRIP‐resistant ovarian cancer cell line, A2780TR, was found to be 9 times less sensitive to TRIP compared to the wild‐type A2780 ovarian cancer cell line. Furthermore, the cytotoxicities of established drugs and other rhenium anticancer agents in the TRIP‐resistant cell line were determined. Notably, the drug taxol was found to exhibit a 184‐fold decrease in activity in the A2780TR cell line, suggesting that mechanisms of resistance towards TRIP and this drug are similar. Accordingly, expression levels of the ATP‐binding cassette transporter P‐glycoprotein, an efflux transporter known to detoxify taxol, were found to be elevated in the A2780TR cell line. Additionally, a gene expression analysis using the National Cancer Institute 60 cell line panel identified the MT1E gene to be overexpressed in cells that are less sensitive to TRIP. Because this gene encodes for metallothioneins, this result suggests that detoxification by this class of proteins is another mechanism for resistance to TRIP. The importance of this gene in the A2780TR cell line was assessed, confirming that its expression is elevated in this cell line as well. As the first study to investigate and identify the cancer cell resistance pathways in response to a rhenium complex, this report highlights important similarities and differences in the resistance responses of ovarian cancer cells to TRIP and conventional drugs.  相似文献   

13.
The seven-coordinate rhenium(III) complex cation [ReIII(dhp)(PPh3)2]+ was isolated as the iodide salt from the reaction of cis-[RevO2I(PPh3)2] with 2,6-bis(2-hydroxyphenyliminomethyl)pyridine (H2dhp) in ethanol. In the complex fac-[Re(CO)3(H2dhp)Br], prepared from [Re(CO)5Br] and H2dhp in toluene, the H2dhp ligand acts as a neutral bidentate N,N-donor chelate. The complexes were characterized by elemental analysis, infrared and 1H NMR spectroscopy and X-ray crystallography.  相似文献   

14.
In new N-methyl[60]fullereno[c]pyrrolidine derivatives, the organometallic substituents in position 2 of the pyrrolidine ring are tricarbonyl(cyclopentadienyl)rhenium, α-bicymantrenyl, and β-bicymantrenyl (also the optically active (+)-enantiomer of the latter). The electrochemical and spectroscopic (NMR) properties of the compounds obtained were studied. Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 9, pp. 1932–1934, September, 2008.  相似文献   

15.
α-亚甲基-β-氨基酮类化合物的合成和光谱特征   总被引:1,自引:0,他引:1  
以取代亚苄基丙酮、二级胺盐酸盐为底物, 与多聚甲醛在无水乙醇中反应. 除得到预期的Mannich碱产物外, 还得到一个副产物, 该副产物经IR, MS, 1H NMR光谱及元素分析数据证明, 为新一类结构的Mannich碱(IM). 对影响Mannich反应的条件(如酸度、反应物的浓度、酮和胺盐的配比以及所用溶剂等方面)作了考察, 并对该产物形成的机理作了探讨. 还报道了14个α-亚甲基-β-氨基酮(IM)类化合物的质谱特征裂解方式及双键烯氢的δ值特征, 并对其机理作了研究.  相似文献   

16.
《Journal of Coordination Chemistry》2012,65(16-18):2965-2977
Abstract

Thermal treatment of pyridine-2-ethyl cyclopentadiene (1) with Fe(CO)5 and Ru3(CO)12 gave novel intramolecular C–H activated dinuclear products (3 and 5). In the case of Fe(CO)5, the reaction also afforded the normal bis(cyclopentadienyl) diiron complex (4). However, similar reaction of pyridine-2-methyl cyclopentadiene (2) with Fe(CO)5 and Ru3(CO)12 only afforded the normal bis(cyclopentadienyl) dinuclear metal complexes (7 and 8). For Ru3(CO)12, the reaction also yielded a pendant η1-pyridyl-coordinated product (9). In addition, the reactions of 1 and 2 with Re2(CO)10 formed the corresponding pyridylethyl/pyridylmethyl cyclopentadienyl rhenium tricarbonyl complexes 10 and 11, which further underwent pyridine to rhenium cyclization via photoirradiation to provide the rhenium dicarbonyl complexes 12 and 13. The molecular structures of 3, 5, 6, 7, 8, 9, and 12 were determined by X-ray diffraction.  相似文献   

17.
Two rhenium(I) tricarbonyl complexes, with the monoanionic tridentate NSO type ligand, 4-(imidazolin-2-yl)-3-thiabutanoic acid and 4-(N-ethylimidazolin-2-yl)-3-thiabutanoic acid were synthesized and isolated in pure form. Both complexes were characterized by spectroscopic methods and elemental analysis. The solid-state structure of 4-(imidazolin-2-yl)-3-thiabutanoic acid and of both complexes was established by X-ray crystallography. The geometry about the rhenium is octahedral. The analogous technetium-99m complexes were also prepared quantitatively by the reaction of both ligands with the fac-[99mTc(CO)3(H2O)3]+ synthon and their identity was established by chromatographic comparison to their rhenium congeners.  相似文献   

18.
The photocatalytic reduction of CO2 into fuels offers the prospect for creating a new CO2 economy. Harnessing visible light-driven CO2-to-CO reduction mediated by the long-lived triplet excited state of rhenium(I) tricarbonyl complexes is a challenging approach. We here develop a series of new mononuclear rhenium(I) tricarbonyl complexes ( Re-1 − Re-4 ) based on the imidazole-pyridine skeleton for photo-driven CO2 reduction. These catalysts are featured by combining pyridyl-imidazole with the aromatic ring and different pendant organic groups onto the N1 position of 1,3-imidazole unit, which display phosphorescence under Ar-saturated solution even at ambient conditions. By contrast, {Re[9-(pyren-1-yl)-10-(pyridin-2-yl)-9H-pyreno[4,5-d]imidazole)](CO)3Cl} ( Re-4 ) by introducing pyrene ring at the N1 position of pyrene-fused imidazole unit exhibits superior catalytic performance with a higher turnover number for CO (TONCO=124) and >99.9 % selectivity, primarily ascribed to the strong visible light-harvesting ability, long-lived triplet lifetimes (164.2 μs) and large reductive quenching constant. Moreover, the rhenium(I) tricarbonyl complexes derived from π-extended pyrene chromophore exhibit a long lifetime corresponding to its ligand-localized triplet state (3IL) evidenced from spectroscopic investigations and DFT calculations.  相似文献   

19.
杨冰  杨俊  翁玲玲  郑虎 《有机化学》2006,26(6):835-838
由泼尼松龙(Prednisolone)为原料, 经甲磺酰化、甲基化、脱水、两次1,3-偶极反应以及其后的两次热分解共7步反应, 以23.5%的总收率首次制得了11β-羟基-16β-甲基-16α,17α-环丙烷基-孕甾-1,4-二烯-3,20-二酮这一重要的潜在药物及化学中间体. 实验同时发现, 1,3-偶极反应及其之后的热分解反应具有高度的立体选择性和区域选择性. 这种立体选择性和区域选择性通过1H NMR数据加以了证明.  相似文献   

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