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  • Suguru TAKATSUTO, Kiyomi KOBAYASHI, Tsuyoshi WATANABE, Hiroki KURIYAMA, Tokuo FURUSE
    Agricultural and Biological Chemistry
    1988年 52 巻 12 号 3217-3218
    発行日: 1988年
    公開日: 2006/04/05
    ジャーナル フリー
  • R.G. WAN, P.J. GUO
    地盤工学会論文報告集
    1999年 39 巻 6 号 1-11
    発行日: 1999/12/15
    公開日: 2008/02/29
    ジャーナル フリー
    This paper outlines a mathematical description of the stress dilatancy behaviour of granular materials which accounts for stress level and void ratio dependencies. The consideration of these aspects has important implications in the modelling of granular material behaviour. In fact, granular material mechanical response is largely dominated by the evolution of dilatancy, fabric and void ratio histories. The starting point in this study is the well established Rowe's theory which is revisited and ultimately modified by introducing a factor linked to governing state parameters in order to describe the complete behaviour of granular materials during deformation. Numerical simulations of triaxial tests on granular materials at different void ratios and stress levels are herein presented to illustrate the model.
  • Tsuyoshi WATANABE, Hiroki KURIYAMA, Tokuo FURUSE, Kiyomi KOBAYASHI, Suguru TAKATSUTO
    Agricultural and Biological Chemistry
    1988年 52 巻 8 号 2117-2118
    発行日: 1988年
    公開日: 2006/04/05
    ジャーナル フリー
  • 若生 達夫
    地理学評論
    1958年 31 巻 5 号 309-312
    発行日: 1958/05/01
    公開日: 2008/12/24
    ジャーナル フリー
    Having made a reconnaisance in this area, the writer classified it into several geomorpholoical surfaces, concerning about the nature and the time of the formation of each surface.
    (1) Those surfaces are termed, from the lower to the upper, A to G, and mountains; and
    B
    is subdivided into
    Ba
    and
    Bb
    . The relative height of A to G is about 250 meters.
    (2) A•
    B
    •C•
    D
    are river terraces, while
    E
    has characters of the rock bench or the partial pediment (by Ben A. Tator, 1952-1953). F may be the same with
    E
    , and a part of
    D
    resembles
    E
    .
    Above identification depends on the structures of the superficial layers underlying those surfaces and on the forms of those surfaces. G is the surface of the inselberg-like isolated hill, relating to
    E
    and F.
    (
    3
    ) The rocks forming mountains are ancient ones of Hidaka Belt, and the rock underlying G is liparite, while the rest on which the large part of each surface-A-F-lie is loose tuffaceous sandstone.
    (
    4
    ) Among the materials (gravels or finer materials) underlying
    Bb
    and C, various paleolithic. stone implements have been discovered by Shôichi Yoshizaki, archaeologist.
    (
    5
    ) The writer takes a view that such stone implements must be embedded in the material underlying
    Ba
    . The reason is that
    Ba
    and
    Bb
    are supporsed to be the protected terraces, owing to the presence of the gorge of the hard rock of Hidaka Belt downstream, and the time of those formation supposed to have been in the same cycle.
    But an alternative interpretation would be possible, that is, the time of the formation of the graded reach emerged as
    Ba
    later belongs to the alluvial epock, but the time of the accident by which
    Ba
    was formed belongs to the dilluvial epock.
    (
    6
    ) Geologist Kiyoshi Hasegawa has studied the area and, from the gravels underlying each surface, concluded that the time of the formation of the volcano Tengudake corresponds to the time of the formation of C, and that of the present peak of the volcano is later than that of
    B
    and earlier than A.
    The lava flows of the volcano might affect the drainage systems of this area, and they might also affect the agencies to form those surfaces.
    (7) In addition to the facts above mentioned, there exist another characteristics, that is, each surface has different pedological character.
    So, the writer supposes that such surfaces could be classified corresponding to the geological age, from the view point of geomorphology, geology, archaeology and pedology. And the conditions, especially climatic ones, under which each surface was formed could be estimated.
  • 佐藤 敬之輔
    デザイン学研究
    1970年 1970 巻 11 号 45-55
    発行日: 1970/03/30
    公開日: 2017/07/25
    ジャーナル フリー
    [1] The purpose of this reserch is to make clear what type of design can give good effects to win the high readership score. At the begining I had to know what factors decide the readership score, and how to change the quality of the desing into numerical value. I have used the method of multi-dimentional analysis with the help of a computer, and got the estimation formula, with 7 kinds of factors, as follows ; A^^〜=
    B
    +C+
    D
    +K+aE+
    bF
    +cG. A^^〜=estimated values of the readership score. 1)
    B
    , C,
    D
    , K : these four factors are given as category values (so we call them); each factor is classified into several categories.
    B
    =week day, classified into 7 categories. C=pages of a newspaper, which are characterized by the kinds of articles, news, and the other reading matters, classified into
    22
    categories.
    D
    =kinds of goods and trades of the advertizement, classified into 14 catedories. K=constants, given to each 13 surveys. 2)
    E
    , F, G : these factors are given as numerical values. G=area of advertizement, measured by the unit of column in the whole page length, being classified into
    6
    kinds of area (2.
    5
    ,
    3
    .
    5
    ,
    5
    , 7, 10, 15) and 15 column means a whole page, about 2,000cm^2.
    E
    , F are the marks obtained in the design of advertizements.
    E
    =sum of the marks obtained in each design element on the advertizement. F=the marks obtained on the whole effect of the design.
    3
    ) a,
    b
    , c : coefficients Using the above formula with the category values and the coefficients, we can obtain the naked design effect from the actual value A of readership score: aE+
    bF
    =A-(
    B
    +C+
    D
    +K+cG). In this research, I used 1,829 data of readership score from 1960 to 1968, being obtained by 13 survevs, spring and autumn twice a year. The sample of size each survey was
    3
    ,541, 2,251, or 200 in the other 11 surveys. Multiple correlation coefficient between the estimated value A^^〜 and the actual value A is 0.951. The table 2^* shows the contribution indexes of each factor by
    3
    kinds of expression-(1) Range : the absolute difference between the maximum and the minimum category values, (2) Standard deviations of the category values, (
    3
    ) Partial correlation coefficient : the relationship between the actual values A and each factors. *see the table 2 in the thesis in Japanese. [2] The important point was in the determination of the values of
    E
    , F.
    E
    is the sum of the marks obtained in each design element, classified into four kinds :
    E
    =
    E
    _1+
    E
    _2+
    E
    _
    3
    +
    E
    _
    4
    . design elements [table]
    E
    _1,
    E
    _2,
    E
    _
    3
    ,
    E
    _
    4
    , these values have the
    5
    grades, as 0, 1, 2,
    3
    ,
    4
    and 0 is given to the design that has no attractive effect or no applicable element. And
    E
    obtain the marks of 0 to
    9
    grades as the sum of them. The values of F have also
    5
    grades, 0 to
    4
    . The principles to determine the values of
    E
    , F are as follows : a) The marks obtained of
    E
    , F must be the relative values among the each survey, and at the same time, they must have constancy within the same survey-the same elements of design must win the same marks obtained.
    b
    ) They must be determined as to win the highest multiple correlation coefficient, when they are put into the estimation formula. c) They must be reasonable. In order to justify them, we must carry many researches on the actual condition. The frequency of accurence of each grade of
    E
    , F values, as the table
    5
    -
    4
    , and
    5
    -
    5
    in the thesis in Japanese.
  • 末次 康将
    マリンエンジニアリング
    2021年 56 巻 5 号 680-687
    発行日: 2021/09/01
    公開日: 2021/10/12
    ジャーナル フリー
  • Keishi Hata, Fuyuki Sugawara, Naganori Ohisa, Saori Takahashi, Kazuyuki Hori
    Biological and Pharmaceutical Bulletin
    2002年 25 巻 8 号 1040-1044
    発行日: 2002年
    公開日: 2002/08/01
    ジャーナル フリー
    We screened the differentiation-inducing activities of 39 mushroom extracts from Akita prefecture, Japan, on the mouse osteoblastic cell line, MC
    3
    T
    3
    -
    E
    1. Sixteen phosphate buffered saline (PBS), 8 boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MC
    3
    T
    3
    -
    E
    1 cell differentiation. The enzyme activities were markedly induced by extracts of Tricholoma auratum, and we isolated the active compound from methanol extracts of this mushroom. Physical data for the isolated active compound were identical to those for (
    22E
    ,24R)-ergosta-7,
    22
    -diene-
    ,
    ,
    -triol (1). 1 induced ALP activities of MC
    3
    T
    3
    -
    E
    1 cells and promoted cell proliferation. To investigate the relationships between the chemical structure and differentiation-inducing activity of the compound, ALP-inducing activities of MC
    3
    T
    3
    -
    E
    1 cells by 1, ergosterol (2), ergocalciferol (
    3
    ), cholesta-
    ,
    ,
    -triol (
    4
    ), 7-dehydrocholesterol (
    5
    ) and cholecalciferol (
    6
    ) were tested. The enzyme activities of MC
    3
    T
    3
    -
    E
    1 cells were increased
    3
    .0-fold by 10 μM 1 and 2.
    4
    -fold by 10 μM
    4
    . However, 2,
    3
    ,
    5
    and
    6
    did not induce MC
    3
    T
    3
    -
    E
    1 cell ALP activity at 0.1—10 μM. These results suggested that the OH groups at C-
    5
    and/or C-
    6
    of 1 and
    4
    played an important role in their differentiation-inducing activities on MC
    3
    T
    3
    -
    E
    1 cells. Furthermore, 1 suppressed induction of MC
    3
    T
    3
    -
    E
    1 cell apoptosis by serum starvation.
  • /, 三浦 哲彦, NORIHIKO MIURA
    地盤工学会論文報告集
    1996年 36 巻 4 号 11-22
    発行日: 1996/12/15
    公開日: 2008/02/29
    ジャーナル フリー
    A new analytical method is proposed for determining the inextensible grid reinforcement pullout resistance and pullout force/pullout displacement curve by using basic backfill soil and grid reinforcement properties. The pullout skin friction resistance/pullout displacement relationship is simulated by linear elastic-perfectly plastic model. A hyperbolic model has been proposed to represent the pullout bearing resistance/pullout displacement relationship in which the maximum bearing resistance of a single bearing member is determined using a new bearing capacity equation proposed in this paper. The influences of the grid bearing member spacing ratio, S/
    D
    , the bearing member deflection rigidity, and the pullout softening behavior on the mobilization of pullout bearing resistance are explicitly included in the proposed model. Good agreement has been obtained between calculated values and laboratory test results.
  • Kiyofumi Ninomiya, Kanae Shibatani, Mayumi Sueyoshi, Saowanee Chaipech, Yutana Pongpiriyadacha, Takao Hayakawa, Osamu Muraoka, Toshio Morikawa
    Chemical and Pharmaceutical Bulletin
    2016年 64 巻 7 号 880-885
    発行日: 2016/07/01
    公開日: 2016/07/01
    ジャーナル フリー HTML
    A methanol extract of the flowers of Mammea siamensis (Calophyllaceae) was found to inhibit enzymatic activity against aromatase (IC50=16.
    5
     µg/mL). From the extract, two new geranylated coumarins, mammeasins C (1) and
    D
    (2), were isolated together with seven coumarins: 8-hydroxy-
    5
    -methyl-7-(
    3
    ,7-dimethyl-octa-2,
    6
    -dienyl)-
    9
    -(2-methyl-1-oxobutyl)-
    4
    ,
    5
    -dihydropyrano[
    4
    ,
    3
    ,2-de]chromen-2-one (
    9
    ), 8-hydroxy-
    5
    -methyl-7-(
    3
    ,7-dimethyl-octa-2,
    6
    -dienyl)-
    9
    -(
    3
    -methyl-1-oxobutyl)-
    4
    ,
    5
    -dihydropyrano[
    4
    ,
    3
    ,2-de]chromen-2-one (10), mammeas A/AA (14), A/AB (15), A/AA cyclo
    D
    (18),
    E
    /
    BA
    (23), and
    E
    /BC cyclo
    D
    (25). The structures of 1 and 2 were elucidated on the basis of spectroscopic evidence. Among the isolates including 17 previously reported coumarins, 1 (IC50=2.7 µM), 2 (
    3
    .
    6
     µM), and mammea
    B
    /AB cyclo
    D
    (21,
    3
    .1 µM) showed relatively strong inhibitory activities comparable to the activity of the synthetic nonsteroidal aromatase inhibitor aminoglutethimide (2.0 µM).
  • 小田切 孝人, 田代 眞人
    ウイルス
    2013年 63 巻 2 号 233-240
    発行日: 2013/12/25
    公開日: 2014/10/31
    ジャーナル フリー
  • ASHRAF GHALY, ADEL HANNA, MIKHAIL HANNA
    土質工学会論文報告集
    1991年 31 巻 2 号 77-92
    発行日: 1991/06/15
    公開日: 2008/02/29
    ジャーナル フリー
    The performance of single pitch and multi pitch screw anchors during the application of installation torque is presented. An experimental testing program was conducted using five models of screw anchors with different geometry. The effect of the shape of the screw element, sand properties, and installation depth on the required installation torque value was examined. A theoretical model was developed from which the required installation torque value can be calculated in terms of the influencing factors. The required installation torque can be determined in terms of the ultimate uplift resistance calculated from any of the available theories. Based on the actual installation torque value measured in the field, the anticipated pullout capacity can be back calculated from the present theory. A comparison between theoretical and experimental results showed good agreement. Also, good agreement was observed when the present theoretical results were compared with the available field results reported in the literature.
  • 榎 明潔, 八木 則男, 矢田部 龍一, 一本 英三郎
    土質工学会論文報告集
    1991年 31 巻 2 号 1-13
    発行日: 1991/06/15
    公開日: 2008/02/29
    ジャーナル フリー
    It has been shown after mathematical and mechanical investigation that Limit Equilibrium Method (LEM) can be considered as a method to obtain the necessary condition of Slip Line Method (SLM), and that the solution can be obtained under the condition that Fs=1 and ∂Fs/∂θ=O, where Fs is the safety factor and θ is the inclination of the plane on which the safety factor is defined. Next, the generalized LEM (GLEM) is proposed, dealing with the following points : (1) Triangular or quadrangular blocks can be treated; (2) Safety factors are defined also on interblock planes; and (
    3
    ) All types of plastic problems, slope stability, bearing capacity, and earth pressure are identically formulated. Two situations regarding treatment of the moment equilibrium condition are discussed. GLEM is applied to well-known problems. The results agree well with those obtained by theoretical methods. GLEM can be used to obtain the distribution of earth pressure or bearing capacity. GLEM, Iike ordinary LEM, is very effective for the practical problems, but GLEM is more theoretical and it can result in more accurate solutions.
  • *Yoshihiro TAKAHASHI, Kenta SAITOH, Yasuhiko BENINO, Takumi FUJIWARA, Takayuki KOMATSU
    日本セラミックス協会 年会・秋季シンポジウム 講演予稿集
    2003年 2003F 巻 17-O-11
    発行日: 2003年
    公開日: 2005/08/25
    会議録・要旨集 フリー
    This paper presents a review for the crystallization of nonlinear optical crystals such as
    LaBGeO5
    ,
    LiBGeO4
    , fresnoite-type
    Ba2TiGe2O8
    and several langasite-type crystals in glasses and for the second order optical nonlinearities of those crystals. In this study, transparent surface crystallized glasses consisting of
    LaBGeO5
    ,
    LiBGeO4
    and
    Ba2TiGe2O8
    crystals were successfully fabricated from the corresponding glasses. Second order nonlinear optical coefficients,
    d33
    , were evaluated by Maker fringe technique for those surface crystallized glasses. As a result, it was demonstrated that the
    LiBGeO4
    and the
    Ba2TiGe2O8
    crystals indicated large
    d33
    values, i.
    e
    ., – 1.
    3
    pm/V and –
    22
    pm/V, respectively. In particular,
    d33
    of the
    Ba2TiGe2O8
    crystal is comparable to that of
    LiNbO3
    single crystal. Moreover, we confirmed for the first time that the langasite-type crystals, which are promising materials for SAW device, are formed by crystallization in the corresponding glasses.
  • Özkan ASLANTAŞ, Ebru Şebnem YILMAZ
    Journal of Veterinary Medical Science
    2017年 79 巻 6 号 1024-1030
    発行日: 2017年
    公開日: 2017/06/16
    [早期公開] 公開日: 2017/04/27
    ジャーナル フリー

    This study aimed to determine the prevalence of fecal carriage of extended spectrum β-lactamase (ESBL) and/or plasmidic AmpC β-lactamase (pAmpC) producing Escherichia coli among dogs (n=428) in Turkey. Polymerase chain reaction (PCR) and sequencing were used to characterize genes encoding β-lactamase and plasmid mediated quinolone resistance (PMQR). Antimicrobial susceptibility testing and PCRs for virulence genes and phylogenetic groups were also performed. Cefotaxime resistant

    E
    . coli isolates were detected in 95 (
    22
    .2%) of the swab samples. Sequencing analysis results showed occurrence of various β-lactamase genes: blaCTX-M-15 (62), blaTEM-
    1b
    (42), blaCMY-2 (
    22
    ), blaCTX-M-
    3
    (16), blaCTX-M-1 (15), blaOXA-1 (
    9
    ) and blaSHV-12 (
    3
    ) alone or in combination. The most frequently encountered phylogenetic group was group A1 (35.8%), followed by group
    D2
    (
    22
    .1%),
    B
    1 (15.8%),
    D1
    (
    9
    .
    5
    %), A0 (7.
    4
    %),
    B22
    (
    5
    .
    3
    %) and
    B23
    (
    4
    .2%), respectively. PMQR genes, aac(
    6
    ’)-Ib-cr, qnr
    S1 and qnrB10 were detected in 25.
    3
    , 10.
    5
    and 1.1% of the isolates, respectively. While all isolates were susceptible to imipenem and amikacin, resistance rates to non-β-lactam antibiotics ranged from 20.0% for tobramycin to 56.8% for tetracycline. The virulence genes were only detected in 34 (36.2%) of the isolates and this isolates carried single or various combination of virulence genes of iucD, papC, papE, f17a-A and eaeA. Four isolates were identified as human virulent pandemic CTX-M-15 producing
    E
    . coli
    clone O25
    b
    :ST131/
    B
    2. To the best of our knowledge, this is the first study to show fecal carriage of ESBL/pAmpC type β-lactamase producing
    E
    . coli
    isolates among dogs in Turkey.

  • Suguru TAKATSUTO
    Agricultural and Biological Chemistry
    1988年 52 巻 9 号 2361-2363
    発行日: 1988年
    公開日: 2006/04/05
    ジャーナル フリー
  • 堀 幹夫, 片岡 貞, 清水 洋, 小野木 和弘
    YAKUGAKU ZASSHI
    1978年 98 巻 9 号 1189-1197
    発行日: 1978/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    As a fundamental study on dibenzothiepins, reaction of 11-phenyl-
    6
    , 11-dihydrodibenzo [
    b
    ,
    e
    ] thiepin-11-ol (10) or 11-chloro-11-phenyl-
    6
    , 11-dihydrodibenzo [
    b
    ,
    e
    ] thiepin (14) with triphenylmethyl cation or
    SbCl5
    was examined under various conditions. 11-Phenyl-
    6
    , 11-dihydrodibenzo [
    b
    ,
    e
    ] thiepin-11-ylium salt (8) was isolated as a black powder (perchlorate) and a green powder (hexachloroantimonate), but
    BF4
    salt was obtained only as a solution. Treatment of the hexachloroantimonate with excess of
    SbCl5
    was found to result in a novel dehydrocyclization reaction to give selectively
    9
    , 13
    b
    -dihydrofluoreno [1,
    9
    a,
    9
    -c,
    d
    ] [2]-benzothiepin-13
    b
    -ylium hexachloroantimonate (19). Some discussions were made on the mechanism of the formation of 19.
  • Masakazu SHIRAIWA, Kyuya HARADA, Kazuyoshi OKUBO
    Agricultural and Biological Chemistry
    1991年 55 巻 4 号 911-917
    発行日: 1991年
    公開日: 2006/04/05
    ジャーナル フリー
    The composition of "group
    B
    saponin" in soybean seed was analyzed by HPLC, and six kinds of "group
    B
    saponin, " named
    Ba
    ,
    Bb
    ,
    Bb
    ', Be, Bd and Be according to elution order from HPLC, were detected. Of these saponins,
    Ba
    ,
    Bb
    ,
    Bb
    ' and Be were identified with soyasaponin V, I, III and II, respectively. Bd and Be were novel saponins possessing soyasapogenol
    E
    as the aglycone and the same sugar chain as
    Ba
    and
    Bb
    , respectively. These saponins were very unstable in the isolated state and had a tendency to form
    Ba
    and
    Bb
    , respectively. From these results, Bd and Be are presumed to be the precursors of
    Ba
    and
    Bb
    in soybean seed.
  • M. K. Banerjee, P. S. Banerjee, S. Datta
    ISIJ International
    2001年 41 巻 3 号 257-261
    発行日: 2001/03/15
    公開日: 2007/05/31
    ジャーナル フリー
    A boron treated copper bearing HSLA steel containing austenite formers like manganese and nickel, somewhat lower in amount than that in HSLA 100 variety of steel is chosen for the study. The role of thermomechanical processing on the microstructure and mechanical properties of the above steel has been investigated. Differential scanning calorimetric study is carried out for understanding the precipitation behaviour of copper in HSLA steel under the influence of boron. The microstructure of the experimental steel is found to consist of laths of martensites and bainite. MA constituents of ribbon like morphology are observed at the lath boundaries. Higher strength properties of the steel are attributed to the presence of finely distributed precipitates of copper and microalloy carbides.
  • 今野 博行, 青山 幸代, 武林 陽子
    天然有機化合物討論会講演要旨集
    2003年 45 巻 86/P-8
    発行日: 2003/09/01
    公開日: 2017/08/18
    会議録・要旨集 フリー
    Callipeltin A (1) is a cyclodepsipeptide from water sponge collected at New Caledonia. This compound shows anti-HIV and cytotoxic activities against KB and P388 cells and contains three new amino acid residues. β-methoxytyrosine (β-MeOTyr) (
    4
    ), (2R,
    3
    R,
    4
    S)-
    4
    -amino-7-guanidino-2,-
    3
    -dihydroxyheptanoic acid (AGDHE) (
    5
    ), (
    3
    S,
    4
    R)-
    3
    ,
    4
    -dimethyl-L-glutamine (diMeGln) (
    6
    ). In addition, two new truncated open-chain derivatives of Callipeltin A (1), named Callipeltin
    D
    (2) and
    E
    (
    3
    ) were isolated. The unique structure and intriguing biological activities of this compound led us to explore total synthesis of Callipeltin A (1) and to elucidate stereochemistry of β-MeOTyr (
    4
    ). We started to synthesize Callipeltin
    E
    (
    3
    ) which contains β-MeOTyr (
    4
    ). In order to synthesize four stereoisomer of β-MeOTyr (
    4
    ), we attempted Evans anti or syn-Aldol reaction as a key step. Evans direct anti-aldol reaction with chiral benzyloxazolidinones (8) and p-hydroxy benzaldehyde (
    9
    ) promoted by catalytic amounts of MgCl_2 in the presence of triethylamine and chlorotrimethylsilane. This proceder provide
    3
    :1 diastereoselelctivity and 70% yield of isolated anti-aldol product (10). And Enolizalion of isocyanate oxazolidinone (13) with di-n-butylboryl trifrate and diisopropylethylamine followed by treatment with aldehyde 8 afford syn-aldol product 14 affording
    88
    % yield and 1:
    5
    anti: sin diastereomeric ratio. On the other hand, we tried Sharpless Asymmetric dihydroxylation (AD) and Aminohydroxylation (AA) to give all four stereoisomers of β-MeOTyr. Treatment of olefin (18) with AD-mix α provided diol (19) and the α position alcohol of 19 was converted to sulfone regioselectively followed by azidation and treatment of 20 with PPh_
    3
    to afford aziridine (21). Addition of aziridine (21) and
    BF
    _
    3
    ・Et_2O in methanol produced α-amino β-methoxy adduct (
    22
    ). AA reaction protocol with t-butylcarbamate was successfully applied to afford desired
    22
    in single step. Now we construct Callipeltin
    E
    to determine absolute stereochemistry of β-MeOTyr (
    4
    ). In addition, we report the synthesis of diMeGln (
    6
    ) and (2R,
    3
    R,
    4
    S)-
    3
    -hydroxy-2-
    4
    -
    6
    -trimethyl hepanoic acid (7).
  • 伊東 常男, 富井 保雄, 内藤 貴之, 山村 美奈子, 石川 一郎, 川原 徳夫, 水野 義久, 小倉 治夫
    Chemical and Pharmaceutical Bulletin
    1989年 37 巻 8 号 2197-2199
    発行日: 1989/08/25
    公開日: 2008/03/31
    ジャーナル フリー
    5
    -Amino-
    6
    -mercapto-1,
    3
    -dimethyluracil (2) was prepared by the treatment of
    5
    ,
    6
    -diamino-1,
    3
    -dimethyluracil (1) with liquid H2S and pyridine in a sealed steel tube at 60°C for 20 h. Thiazolo[
    5
    ,
    4
    -
    d
    ]pyrimidinediones
    3
    a,
    b
    were obtained from 2 by cyclization with HCO2H and AcOH.Under stringent conditions, however, 1 was converted into the
    5
    ,
    9
    -dihydrodipyrimido[
    4
    ,
    5
    -
    b
    :
    5
    ',
    4
    '-
    e
    ][1,
    4
    ]thiazine derivtive
    4
    a.The structure of
    4
    a was confirmed by spectral (nuclear magnetic resonance and mass spectra) data and by comparison with a sample which was prepared from 2 and
    5
    -hydroxy-1,
    3
    -dimethyluracil.Benzylation of
    4
    a gave 1,
    3
    , 7,
    9
    -tetramethyl-
    5
    -benzyl (or p-bromobenzyl)-
    5
    ,
    9
    -dihydrodipyrimido[
    4
    ,
    5
    -
    b
    :
    5
    ',
    4
    '-
    e
    ][1,
    4
    ]thiazine-2,
    4
    ,
    6
    , 8-(1H,
    3
    H, 7H)-tetrone (
    4
    b
    , c) and 1,
    3
    , 7,
    9
    -tetramethyl-
    5
    -benzyl (or p-bromobenzyl)-
    5
    ,
    9
    -dihydropyrrolo[
    3
    , 2-
    d
    :
    4
    ,
    5
    -
    d
    ']dipyrimidine-2,
    4
    ,
    6
    , 8-(1H,
    3
    H, 7H)-tetrone (
    6
    a,
    b
    ).
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