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    • 3. 发明授权
    • Antibiotic F-0769, process for its production, and its use as a growth
accelerating and feed efficiency increasing agent and as an antitumour
agent
    • 抗生素F-0769,其生产方法及其作为生长促进剂和饲料效率增加剂和作为抗肿瘤剂的用途
    • US4904470A
    • 1990-02-27
    • US21125
    • 1987-03-03
    • Hideo SugawaraTomonori TakashinaNobuko TakahashiMachiko SugiyamaAkio SeinoYukio Miyazaki
    • Hideo SugawaraTomonori TakashinaNobuko TakahashiMachiko SugiyamaAkio SeinoYukio Miyazaki
    • C07G11/00A23K1/17A23K1/18A61K35/66A61K35/74A61P31/04C12P1/06C12R1/465
    • C12P1/06A23K20/195A23K50/30
    • An antibiotic F-0769 having the following properties:(1) Outer appearance: White or light yellow powder,(2) Melting point: 245.degree.-250.degree. C.,(3) Specific rotation: [.alpha.].sub.D.sup.25 =-37.5.degree. (c=1, methanol),(4) Solubility in solvents: Soluble in methanol, ethanol, acetone, chloroform, ethyl acetate and benzene; and insoluble in water and hexane,(5) Elementary analysis (found %): C:57.53, H:7.36, O:21.17, N:12.97,(6) Ultraviolet absorption spectrum (as measured in methanol: As shown in FIG. 1, .lambda.max(E.sub.1 cm.sup.1%)=213 nm (466), 286 nm (200)(7) Infrared absorption spectrum (as measured by KBr method): As shown in FIG. 2,(8) Nuclear magnetic resonance spectra (as measured in heavy chloroform): .sup.1 H-NMR spectrum is as shown in FIG. 3, and .sup.13 C-NMR spectrum is as shown in FIG. 4,(9) Distinction among basicity, acidity and neutrality: Neutral substance,(10) Amino acid analysis: As a result of the hydrolysis with 6N hydrochloric acid at 110.degree. C. for 18 hours, amino acids i.e. threonine, valine and leucine were detected,(11) Color reactions: Positive in the iodine reaction and in the potassium permanganate reaction; and negative in the ninhydrin reaction and in the ferric chloride reaction,(12) Thin layer chromatography (by means of silica gel, Art, 5715, manufactured by Merck Co.):______________________________________ Solvent system Rf value ______________________________________ Ethyl acetate 0.16 Ethyl acetate-methanol (5:1) 0.33 Chloroform-methanol (10:1) 0.68 Ethyl acetate-acetone (1:1) 0.31 Acetone-benzene (5:1) 0.40 ______________________________________ (13) Molecular weight (as measured by Rast method): About 745
    • 具有以下性质的抗生素F-0769:(1)外观:白色或浅黄色粉末,(2)熔点:245〜-250℃,(3)比旋光度:αD25= -37.5° (c = 1,甲醇),(4)溶剂中的溶解度:溶于甲醇,乙醇,丙酮,氯仿,乙酸乙酯和苯; 并且不溶于水和己烷,(5)元素分析(发现%):C:57.53,H:7.36,O:21.17,N:12.97,(6)紫外吸收光谱(在甲醇中测定: 1,λmax(E1cm1%)= 213nm(466),286nm(200)(7)红外吸收光谱(通过KBr法测定):如图2所示,(8)核磁共振谱 如在重氯仿中测得):1 H-NMR光谱如图3所示,13C-NMR谱如图4所示,(9)碱度,酸度和中性之间的区别:中性物质,(10)氨基 酸分析:由于6N盐酸在110℃水解18小时,检测出氨基酸,即苏氨酸,缬氨酸和亮氨酸,(11)色素反应:碘反应和高锰酸钾反应中呈阳性 ;在茚三酮反应和氯化铁反应中为负,(12)薄层色谱法(通过硅胶,Art,5715,由Merck Co.制造): - 溶剂sy 茎Rf值乙酸乙酯0.16-乙酸乙酯 - 甲醇(5:1)0.33-氯仿 - 甲醇(10:1)0.68乙酸乙酯 - 丙酮(1:1)0.31-乙酮 - 苯(5:1)0.40- (13)分子量(用Rast法测定):约745
    • 5. 发明授权
    • Lactone compound of agricultural utility
    • 内酯农用化合物
    • US5032611A
    • 1991-07-16
    • US320599
    • 1989-03-08
    • Ryusuke TaguchiHideo SugawaraYukio MiyazakiTaku MizunoMasahide NomuraMachiko SugiyamaHideo SaitoGoro YabutaAkiya FuruichiYasuhiko HamazakiKatsuhiro Nakamura
    • Ryusuke TaguchiHideo SugawaraYukio MiyazakiTaku MizunoMasahide NomuraMachiko SugiyamaHideo SaitoGoro YabutaAkiya FuruichiYasuhiko HamazakiKatsuhiro Nakamura
    • C12P1/06A01N43/08A01N63/02C07D307/58C07D307/68C07G99/00C12P17/04C12R1/01
    • A01N43/08C07D307/58Y10S435/911
    • Disclosed in the present invention are: a substance F-0368 or salts thereof having the following structural formula ##STR1## a method for production of the substance F-0368 or salts thereof, wherein an F-0368-substance-producing-microorganism belonging to a genus Kitasatosporia is cultured, and the substance F-0368 is isolated and collected from the cultured substance; a method for production of the substance F-0368 or salts thereof, wherein 3-methyl-4-lower alkoxy carbonyl-2(5H)-furanone represented by the following general formula is subjected to hydrolytic reaction ##STR2## (where: R represents a straight or branched lower alkyl group having 1 to 6 carbon atoms); a composition which consists essentially of the substance F-0368 or salt thereof, a diluent permissible in the agricultural chemicals, and a carrier or an excipient; a preventive agent for plant diseases such as rice blast disease and bacterial leaf blight disease, which consists essentially of an effective amount of the substance F-0368 or salts thereof as the active component, a diluent permissible in the agricultural chemicals, and a carrier or an excipient; a method for preventing plant diseases, wherein plants are treated with the preventive agent; a disinfectant for agricultural use to prevent plant disease such as rice blast disease and bacterial leaf blight disease, which consists essentially of an effective amount of the substance F-0368 or salts thereof, as the active component, a diluent permissible in the agricultural chemicals, and a carrier or an excipient; materials for agricultural use containing therein the substance F-0368 or salts thereof; a method for growing plants, wherein the plants are cultivated by use of the agricultural materials; and an F-0368-substance-producing microorganism (Kitasatosporia sp. F-0368; FERM BP-2259).
    • 在本发明中公开的是具有以下结构式的物质F-0368或其盐:其中产生F-0368物质的微生物属于F-0368或其盐, 培养北海孢属,从培养物中分离收集F-0368物质; 制备物质F-0368或其盐的方法,其中由以下通式表示的3-甲基-4-低级烷氧基羰基-2(5H) - 呋喃酮进行水解反应(其中:R表示 具有1至6个碳原子的直链或支链低级烷基); 基本上由物质F-0368或其盐组成的组合物,农药中允许的稀释剂,以及载体或赋形剂; 用于植物疾病如稻瘟病和细菌性叶枯病的预防剂,其基本上由有效量的F-0368物质或其盐作为活性成分,农药中允许的稀释剂和载体或 赋形剂 预防植物病害的方法,其中用预防剂处理植物; 用于农业用途的消毒剂,以防止植物病害如稻瘟病和细菌性叶枯病,其主要由有效量的作为活性成分的有效量的物质F-0368或其盐,农药中允许的稀释剂, 和载体或赋形剂; 含有物质F-0368或其盐的农业用材料; 一种用于种植植物的方法,其中通过使用农业材料培育植物; 和产生F-0368的微生物(Kitasatosporia sp.F-0368; FERM BP-2259)。