神农架地区五味子科植物成分的研究 II: 五味子酯F的分离与结构研究

从湖北房县中坝采集的南五味子(Kadsura sp. 种名待定)根中, 分得四个新化合物. 本文报道其中之一—五味子酯F(schisantherin F)的分离与结构研究以及在结构研究过程中获得的十一个衍生物的制备方法和理化数据.     

五味子酯J和五内酯F的分离与结构

从长梗南五味子(Kadsura Lorgipedunculata Finet.et Gagnep)种子中分得2个新化合物: 五味子酯(schisantherin)J(1)和五内酯(schisanlactone)F(2); 4个已知物: 五内酯(Schisanlactone)A、schizandronic acid、表安五酸(epianwuweizic acid)和二甲基去当归酰五味子酯F, 抗癌药理筛选表明, 在体外2对白血病P-388细胞有明显抑制作用。     

翼梗五味子的研究 Ⅱ.翼梗五味子酯和翼梗五味子酸的结构

从翼梗五味子(Schisandra henryi Clarke)中分得四种结晶成分,其中两种鉴定为五味子酯乙(1)和南五味子酸(Kadsuric acid,3);另外二种为新化合物,分别命名为翼梗五味子酯(2)和翼梗五味子酸(4),经结构测定,前者为C₇(R)-五味子酯乙,其结构式和构象如2所示;翼梗五味子酸推定为⊿^9,24羊毛甾二烯-3-氧代-22-乙酰氧基-26-酸(4)。除五味子酯乙是已知的降血清谷丙转氨酶有效成分外,经小白鼠四氯化碳中毒性肝炎观察表明,翼梗五味子酯亦有明显的降转氨酶作用,而南五味子酸无效。     

粤北产五味子科植物风沙藤的化学成分研究(II)

本文继续报道从粤北所采集的五味子科植物风沙藤(Schisandra viridis A. C.Sm)根和茎中分得的另外三个木脂素类新化合物, 即五味子酯(schisantherin)K,五脂酮(Schisanlignone)E和异安五脂素(isoanwulignan)。通过光谱分析和化学转变, 确定了它们的结构和构型。     

粤北产五味子科植物风沙藤的化学成分研究(II)

本文继续报道从粤北所采集的五味子科植物风沙藤(Schisandra viridis A. C.Sm)根和茎中分得的另外三个木脂素类新化合物, 即五味子酯(schisantherin)K,五脂酮(Schisanlignone)E和异安五脂素(isoanwulignan)。通过光谱分析和化学转变, 确定了它们的结构和构型。     

粤北产五味子科植物风沙藤的化学成分研究(Ⅱ)

本文继续报道从粤北所采集的五味子科植物风沙藤(Schisandra viridis A.C Sm)的根和茎中分得的另外三个木脂素类新化合物,即五味子酯(schisantherin)K(1),五脂酮(schisanlignone)E(2)和异安五脂素(isoanwulignan)(3)。通过光谱分析和化学转变,确定了它们的结构和构型。     

神农架地区五味子科植物成分的研究 I: 铁箍散茎和根的化学成分研究

用铁箍散的茎和根中分得六个化合物, 其中一个是新化合物, 命名为表恩施辛(1,epienshicine), 在体外具有抗癌活性. 其结构由光谱分析和化学转化确定为1-氧代-2R, 3S-二甲基-4R-(3-甲氧基-4-羟基苯)-6,7-次甲二氧基四氢萘. 其余五个为已知物, 分别鉴定为恩施辛(2,enshicine),isoschizandrolic acid(3), 去氧五味子素, β-谷甾醇和硬脂酸, 其中3系首次自天然界获得.     

神农架地区五味子科植物成分的研究 Ⅰ.铁箍散茎和根的化学成分研究

从铁箍散的茎和根中分得六个化合物.其中一个是新化合物,命名为表恩施辛(1,epienshicine),在体外具有抗癌活性.其结构由光谱分析和化学转化确定为1-氧代-2R,3S-二甲基-4R-(3-甲氧基-4-羟基苯)-6,7-次甲二氧基四氢萘.其余五个为已知物,分别鉴定为恩施辛(2,enshicine),isoschizandrolic acid(3),去氧五味子素,β-谷甾醇和硬脂酸,其中3系首次自天然界获得     

五内酯E和长南酸的分离与结构

从浙江临安产的长梗南五味子(Kadsura longipedunculata Finet. etGagnep.)根皮中分得2个新三萜化合物: 五内酯E(Schisanlactone E, 1)和长南酸(changnanic acid 2)以及3个已知物: 五内酯B(schisanlactone B,3)、meso-二氢愈创木脂酸(meso-dihydoguaiaretic acid,4)和β-谷甾醇(β-sitosterol,5)。1和2在体外对白血病p-388细胞有明显地抑制作用, IC50分别为1μg/mL和10μg/mL。本文报道其分离、鉴定与结构研究。     

粤北产五味子科植物风沙藤的化学成分研究I.

从粤北产五味子科植物风沙藤(Schisandra viridis A. C. Sm.)的根和茎中, 分到三个新的联苯环辛二烯木脂素化合物, 它们的结构和构型通过光谱分析和化学转变得以证实, 并分别命名为: 五脂酮(Schisanlignone)C(1), D(2)和五脂醇(schisan-lignaol)D(3)。     

4-(1,2-亚乙二氧基)环己酮及其2-甲醛和2-羧酸酯的烯胺和烯醇反应的研究

4-(1,2-亚乙二氧基)环己酮及其2-甲醛和2-羧酸酯的烯胺和烯醇与丙烯酸型的和丙二酸型的试剂反应,获得了与6-(1,2-亚乙二氧基)-5,6,7,8-四氢-2(1H)- 喹啉酮很相近的四个化合物(5,11,18,19)和六个其它化合物(4,7,8,9,16,17).探讨了这十个均未见于文献的新化合物的生成机理,并得到一个制备5- 四氢萘胺衍生物的新方法     

Metabolism of terniary compounds. V. Decomposition of diincarbonic acids and hydrocarbons in vivo

10,12-Heneicosadiynoic acid (I), 5,7-hexadecadiynoic acid (IV), and 10,12-docosadiynedioic acid (VI) were fed to rats. As metabolites 4,6-undecadiynedioic acid (II), 5,7-dodecadiynedioic acid (V), and 4,6-decadiynedioic acid (VII) respectively were isolated from the urine. 10,12-Heptadecadiynoic acid (III) also yielded metabolite II. Furthermore 9,11-eicosadiyne (X) and for comparison purposes eicosane (XI), hexadecanedioic acid (VIII), and docosanedioic acid (IX) were fed. X and XI were incorporated into depot fat and liver lipids to a cetain degree. The diynes I, II, IV, and X are new compounds.     

土槿皮新二萜成分的研究 IV: 土槿丁酸和土槿戊酸的分离和结构测定

从土槿皮(Pseudolarix kaempferi, Gord.)中分离到两个新二萜酸, 命名为土槿丁酸(1)和土槿戊酸(2), 经理化性质和对它们的IR、^1H NMR、^1^3C NMR、MS数据的分析, 鉴定1为 18-羟-对映-贝壳杉-15-烯-17-羧酸; 2为对映-贝壳杉-15-烯-17, 18-二羧酸. 1的结构经X衍射得到了证实.     

Two closely related {4‐[(N‐substituted amino)(diethoxyphosphoryl)methyl]phenyl}boronic acids

Organic phosphonic acids and organic phosphonic acid esters have been of much interest due to their applications in the fields of medicine, agriculture and industrial chemistry. Boronic acids can act as synthetic intermediates and building blocks and are used in sensing, protein manipulation, therapeutics, biological labelling and separation. The additional introduction of an aminophosphonic acid group into a boronic acid may give new opportunities for application. To study the structure of such multifunctional compounds, we prepared two new derivatives which can be easily converted to the corresponding phosphonic acids. In the title compounds, {4‐[(butylamino)(diethoxyphosphoryl)methyl]phenyl}boronic acid monohydrate, C₁₅H₂₇BNO₅P·H₂O, (I), and {4‐[(diethoxyphosphoryl)(4‐nitroanilino)methyl]phenyl}boronic acid, C₁₇H₂₂BN₂O₇P, (II), three different substituents are attached to a central C—H group, namely 4‐boronophenyl, diethoxyphosphoryl and amine. Compound (I) crystallizes as a monohydrate and O_B—H…N hydrogen bonds link neighbouring molecules into chains along the [001] direction. The solvent water molecule connects two such chains running in opposite directions. Compound (II) crystallizes as an ansolvate and classical hydrogen bonds result in a layer structure in the (001) plane.     

Cytotoxic and anti-HIV principles from the rhizomes of Begonia nantoensis

Three new compounds: begonanline (1). nantoamide (2). and methyl (S)-glycerate (3). as well as forty-four known compounds have been isolated and characterized from the rhizomes of Begonia nantoensis. The structures of these compounds were determined by spectral analyses and/or X-ray crystallography. Among them, cucurbitacin B (4). dihydrocucurbitacin B (5). cucurbitacin E (6). dihydrocucurbitacin E (7). cucurbitacin I (8). and (-)-auranamide (9). showed cytotoxicity against four human cancer cell lines. 3beta,22alpha-Dihydroxyolean-12-en-29-oic acid (10), indole-3-carboxylic acid (11), 5,7-dihydroxychromone (12), and (-)-catechin (13) demonstrated significant activity against HIV replication in H9 lymphocyte cells.     

N'-取代苯磺酰基N-(4,6-二取代均-三氮苯-2-基)乙二胺的合成

N-芳基磺酰乙二胺与三聚氰氯反应获得三个新缩合产物, 缩合产物再与醇钠反应得到六个N-取代苯磺酰基-N'-取代均三嗪基乙二胺衍生物, 所有化合物都表现出对植物生长的抑制作用, 可用于筛选除草剂.     

Melophlins P, Q, R, and S: four new tetramic acid derivatives, from two Palauan marine sponges of the genus Melophlus

Four new tetramic acid derivatives, named melophlins P, Q, R, and S (1-4), were isolated from two marine sponges of the genus Melophlus collected at Palau, together with seven known melophlins A, D, E, G, H, I, and O. The structures of the new compounds were elucidated on the basis of their spectral data. The absolute stereochemistries at the tetramic acid moieties of the new compounds were determined as 1 : 1 mixtures (racemic) by ESI-LC/MS analysis of derivatives obtained by oxidation and hydrolysis of the respective parent compounds. Melophlins P-S (1-4) showed cytotoxicity against the murine leukemia cell line L1210 with IC(50) values of 20.0, 10.5, 0.85, and 5.13 muM, respectively.     

Oxidation of perfluoroaromatics

3,4,5,6-Tetrafluoro-2-nitroaniline (I), 2,3,5,6-tetrafluoro-4-nitroaniline (IV) and 2,5,6-trifluoro-4-nitro-1,3-phenylenediamine (VI) react with nitrous acid to give 3,4,5-trifluoro-6-nitro-1,2-diazo-oxide (III), 3,5,6-trifluoro-4-nitro-1,2-diazo-oxide and (V) 5-fluoro-6-nitro-bis-1,2:3,4-diazo-oxide (VII), respectively. Reduction of the diazo-oxide (III) with hypophosphorous acid gives 4,5,6-trifluoro-3-nitrophenol (VIII). Treatment of 2,3,4,6-tetrafluoroacetanilide with nitric acid affords trifluoro-p-benzoquinone (X), the reduction of which gives trifluorohydroquinone (XI). Proton and fluorine chemical shifts and coupling constants of the new compounds are reported.