200913891 九、發明說明 【發明所屬之技術領域】 本發明係有關一種以1 6-氧代麴黴亞胺 作爲有效成份之農園藝用殺蟲劑。 相關專利申請參考 本專利申請案同時主張2〇〇7年6月21日 本申請案特願2007- 1 63 582號之優先權，該 文揭示之內容以引用方式倂入本文作爲本申 分。 【先前技術】 過去以來已知有多種農園藝用殺蟲劑， 藥性或安全性等問題，可更有效且安全使用 要。爲農家省力化之目的之農作物害蟲防治 使用對種子或於播種時、育苗期或移植時對 劑之方法，此時，一般使用可自種子或植物 有於植物體內移行而顯示防治效果之浸透移 所謂具有浸透移行性之藥劑，謂之於植物體 使吸汁、攝食該藥劑之害蟲中毒死亡之藥劑 殺蟲劑（參考新版「農藥科學」（文永堂出版 著）之第14頁）。 PF1378物質亦即16-氧代麹黴亞胺爲具 化合物，經報告爲麴黴（Aspergillus)屬生產 (P F 1 3 7 8 物質） 提出申請之曰 曰本申請案全 請揭不之一部 但由於藥劑抗 之藥劑成爲必 方法，係廣泛 植物體施加藥 之根吸收，具 行性之藥劑。 內浸透移行， ，所謂浸透性 ，山下恭平等 有下列結構之 之代謝產物， 200913891 已知作爲對晡乳類之消化管寄生線蟲之捻轉血矛線蟲 (Haemonchus contortus)之3齡幼蟲的驅蟲活性物質（The Journal of Antibiotics, 1 997, 50( 1 0), 840-846)。然而，該 物質對於農業害蟲之活性並未有任何報導。 [化1]BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an agricultural and horticultural insecticide which uses 16-oxo-pyridinium imine as an active ingredient. RELATED APPLICATIONS This application is hereby incorporated by reference in its entirety in its entirety in the entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire entire all all all all all [Prior Art] A variety of agricultural and horticultural insecticides have been known in the past, which are more effective and safe to use, such as medicinal properties or safety. For the control of crop pests for the purpose of saving labor for farmers, the method of using seeds for seeding or at the time of sowing, at the seedling stage or at the time of transplanting is generally used. In this case, it is generally used to migrate from the seeds or plants to show the control effect. The agent having the ability to impregnate and migrate is a plant insecticide that causes the plant to poison and inoculate the poison of the drug (refer to the new edition of "Pesticide Science" (published by Wen Yongtang) on page 14). The PF1378 substance, that is, 16-oxomycin, is a compound, and has been reported to be produced by Aspergillus (PF 1 3 7 8 substance). The application is not disclosed in this application. Since the agent against the drug becomes a necessary method, it is a broad-based plant body that applies the root absorption of the drug, and is a medicinal agent. Internal soaking and migration, the so-called permeability, Yamashita Kyoko equals the metabolites of the following structure, 200913891 known as the deworming of 3rd instar larvae of Haemonchus contortus, a parasitic nematode of the digestive tract Active substances (The Journal of Antibiotics, 1 997, 50 (10), 840-846). However, this substance has not been reported for the activity of agricultural pests. [Chemical 1]
又，Tetrahedron Letters, 1 997，3 8(32)，5 65 5-565 8、 Bioscience,Biotechnology and Biochemistry，2000，64(1), 111-115以及特開平1 0-2453 83號公報中，報導有爲16-氧 代麹黴亞胺之類緣物質之麹黴哌帕啉（asperparaline)類對 於蠶具有麻痺活性或對甜菜夜蛾（Spodoptera exigua)、褐 飛 1¾ (Nilaparuata lugens)及蜚蠊（Blattodea)具有殺蟲活性 ，又有關其浸透移行活性亦未有任何報導。 再者，迄今雖報導有多種具有浸透移行性之農園藝用 殺蟲劑，但任一種藥劑均確認有藥劑抗藥性蟲種或難防治 性蟲種存在，故依然期望開發新的殺蟲劑。 【發明內容】 -6- 200913891 本發明人等如今發現PF1378物質具有顯著之農園藝 用殺蟲活性或浸透移行性殺蟲活性。本發明係基於該等發 現而完成者。 因此，本發明目的在於提供一種有效且安全使用之農 園藝用殺蟲劑或浸透移行性殺蟲劑。 因此，依據本發明之一態樣，係提供一種農園藝用殺 蟲劑，係含有PF 1 3 78物質、其對映異構物、其等之混合 物、或其等之農園藝上可接受之酸加成鹽作爲有效成份。 又，依據本發明另一態樣，係提供一種浸透移行性殺 蟲劑，係含有PF 1 3 78物質、其對映異構物、其等之混合 物、或其等之農園藝上可接受之酸加成鹽作爲有效成份。 再者，依據本發明又另一態樣，係提供一種農園藝上 之害蟲防治方法，包含使有效量之PF 1 3 78物質、其對映 異構物、其等之混合物、或其等之農園藝上可接受之酸加 成鹽適用於選自水面、土壤、於營養液栽培中之營養液、 於營養液栽培之固體培養基、植物種子、根、塊莖、球根 以及根莖所組成組群之對象。 【實施方式】 P F 1 3 7 8物質 PF 1 3 78物質（16-氧代麹黴亞胺）可依據例如 The Journal of Antibiotics, 1997, 50(10)，840-846所記載之方 法，自1 6-氧代麴黴亞胺產生菌之培養物獲得。 本發明中，不僅可利用P F 1 3 7 8物質，亦可利用其對 200913891 映異構物進而利用其等之混合物。 又，本發明中，亦可利用PF1378物質之農園藝上可 接受之酸加成鹽，作爲其例，舉例有鹽酸鹽、硝酸鹽 '硫 酸鹽、磷酸鹽或乙酸鹽等之酸加成鹽。 農園藝用殺蟲劑及浸透移行性殺蟲劑 PF 1378物質爲顯示對害蟲之優異防治效果者。因此’ 依據本發明，提供一種農園藝用殺蟲劑及浸透移行性殺蟲 劑，其含有PF 1 3 78物質、其對映異構物' 或其等之混合 物作爲有效成份。又，PF1378物質、其對映異構物或其等 之混合物亦可以農園藝上可接受之酸加成鹽形態使用。 依據本發明另一態樣，提供一種PF 1 3 78物質、其對 映異構物、其等之混合物、或其等之農園藝上可接受之酸 加成鹽之使用，係作爲農園藝用殺蟲劑。 又，依據本發明另一態樣，提供一種PF 1 3 7 8物質、 其對映異構物、其等之混合物、或其等之農園藝上可接受 之酸加成鹽之使用，係作爲浸透移行性殺蟲劑。 PF 1 3 78物質顯示有除蟲效果之蟲種並無特別限制，但 較好舉例爲鱗翅目害蟲（例如斜紋夜蛾（Spod optera litura) 、甜菜夜蛾（Spodoptera exigua)、粟夜盜（Pseudaletia separata)、夜盜蛾（Mamestra brassicae)、球菜夜蛾 (Agrotis ipsilon)、金翅夜蛾（Trich〇plusia)屬、實夜蛾 (Heliothis)屬、棉鈴蟲（Helicoverpa)屬等之夜蛾科類，二化 螟蛾（Chilo suppressalis)、稻縱卷葉螟蛾（Cnaphalocrocis 200913891 medinalis)、玉米螟（Ostrinia nubilalis)、菜心螟（Hellulla undalis Fabricius)、草坪包蛾（Parapediasia teterrella)、 棉卷葉野螟（Notarcha derogata)、印度谷膜（Plodia interpunctella)等之斑螺蛾（Endotricha)類，紋白蝶（Pieris rapae)等之粉蝶科（Pierinae)類，捲葉蛾屬（Adoxophyes spp·)，梨小實心蟲（Grapholita molesta)、蘋果蠢蛾（Cydia pomonella)等之卷葉蛾（Adoxophyes)類，桃蛀果蛾（Carposina sasakii Matsumura)等之柱果蛾科（Carposinidae)類， Lyonetia 屬等之潛蛾科（Lyonetiidae)類，毒蛾屬（Lymantria) 、茶毒蛾屬（Euprotis)等之毒蛾（Artaxa subflava)類，小菜 蛾（Plutella xylostella)等之巢蛾科（Yp〇nomeutidae)類、棉 紅鈴蟲（？6(^110卩110^£0 8 5丫？丨6 113)等之旋麥蛾科（〇616(^^(136) 類’白蛾（Hyphantria cunea)等之燈蛾科（Arctiidae)類，幕 衣蛾（Tineola bisselliella)等之蕈穀蛾科（Tineidae)類等）， 半翅目害蟲（例如’桃録（Myzus persicae)、種棉^(Aphis gossypii Glover)等之蚜蟲科（Aphididae)類，灰稻蝨 (Delphacodes striatellus)、稻飛蝨（pianth〇pper)、白背飛 蝨（Sogatella furcifera)等之飛蝨科（Delphacidae)類，黑尾 夜蟬（Nephotettix cincti cep s)等之夜蟬科（C 丨cade丨丨idae)類 ，稻葉蟲（Trigonotylus caelestialium)、小珀蝽（Plautia crossota stali Scott)、南青龜蟲（Nezara viridula)、蜂緣幢 (Riptortus clavatus)類等之橡蝽科類，白粉蝨（Trialeur〇des vaporariorum)、煙粉蟲（BemiSia tabaei)等之白粉蝶類，桑 白盾蚧（Pseudaulacaspis pentag〇na Targi〇ni)、康氏粉蚧 200913891 (Pseudococcus comstocki)等之介殼蟲類，網幢科（Tingidae)類 ，木1¾科（Psyllidae)類等），鞘翅目害蟲（例如，玉米象 (S itophiluszeamais)、稻水象甲（Lissorhoptrus oryzophilus)、 綠丑象（Callosobruchus chinensis)等之象蟲科類，黃粉蟲 (Tenebrio molitor Linnaeus)等之粉蟲科類，銅色綠金龜 (Anomala cuprea)、姬金龜（Anomala rufocuprea Motschulsky) 等之金龜科類，黃條葉蚤：（Phyllotreta striolata)、黃守瓜 (Aulacophora femoralis)、金花蟲（Leptinotarsa. decemlineata) 、玉米根螢葉甲（Diabrotica virgifera virgifera)、黃瓜十 —星葉甲（Diabrotica und ecimpunctata howardi)等之金花 蟲類，稻葉蟲、蟻型隱翅蟲（Paederus Fuscipes)、蘋果蠢 蛾（Cydia pomonella)類、節二十八星瓢蟲（Epilachna vigintioctopunctata Fabricius)等之瓢蟲屬（Epilachna)類、 天牛類等），織目（例如，二斑葉輸（Tetranychus urticae Koch)、神澤氏葉觸（Tetranychus kanzawai)、柑梧葉觸 (Panonychus citvi) 、 M etatetrany chus ulmi (蘋果葉· (Panonychus uimi)、荔枝葉蟎屬（Oligonychus)等之蛛蟎類 ，番節刺皮癭觸（Aculops lycopersici)、相·橘録壁蟲 (Aculops pelekassi)、紫錄婢（Calacarus carinatus)等之節 蜱 科 （Eriophyidae) 類，側 多食 跗線蟎 (Polyphagotarsonemus latus)等之細蟎科（Tarsonemidae)類 ’粉蟎（F 1 〇 u r m i t e)類等），膜翅目害蟲（例如，菜葉蜂 (Athalia rosae)等之葉蜂科（Tenthredinidae)類等），直翅目 害蟲（例如，飛蝗類等），雙翅目害蟲（例如，蠅科（Museidae) -10- 200913891 類’庫蚊（Culex)類’瘧蚊（Anopheles)類，搖蚊科 (Chironomidae)類，黑蠅（calliphorini)類，麻蠅科 (Sarcophagidae)類，廁蠅科（Fanniidae)類，花蠅科 (Pegoplata)類，非洲菊斑潛蠅（Liriomyza trifolii Burgess) 、美洲斑潛繩（Liriomyza sativae)、蕃前斑潛繩（Liriomyza bryoniae)等之斑潛蠅類，果實蠅科（Tephritidae)類，蚤蠅科 (Phoridae)類’猩猩蠅科（Drosophilidae)類，蛾蚋科 (Psychodidae)類，蚋科（Simuliidae)類，虻科（Tabanidae)類、 廄刺繩（Stable fly)類），經翅目（Thysanoptera)害蟲（例如 ，南黃薊馬（Thrips palmi)、西方花薊馬（Frankliniella occidentalis Pergande)、蔥薊馬（Thrips tabci Lin deman) 、花薊馬（Thrips hauaiiensis)、小黃薊馬（Scirtothrips dorsalis)、台灣花蘇馬（Frunkliniella intonsa (Trybom)、 加菊蘭馬（Ponticulothrips disospyrosi)等），植物寄生性線 蟲（例如，根節線蟲（Root-knot Nematode)類，根腐線蟲類 ，胞囊線蟲（Heterodera glycines)類，心枯線蟲等之葉芽 線蟲（Aphelenchoides)類’松材線蟲（Bursaphelenchus xylophilus)等）等，更好舉例爲半翅目害蟲、纓翅目害蟲 、雙翅目、鞘翅目害蟲，又更好舉例爲半翅目害蟲。 PF1378物質、其對映異構物、其等之混合物、或其等 之農園藝上可接受之酸加成鹽使用作爲農園藝用殺蟲劑之 有效成份時，可就此使用’亦可與適當固體載體、液體載 體、氣體狀載體、界面活性劑、分散劑、其他製劑用補助 劑混合而做成乳劑、液劑 '懸浮劑、水合劑、粉劑、粒劑 -11 - 200913891 、錠劑、油劑、氣溶膠、可流動劑等之任意劑型而使用。 作爲固體載體舉例有例如滑石、膨潤土、黏土、高嶺 土、矽藻土、蛭石、白碳、碳酸鈣等。 又，作爲液體載體，舉例有例如甲醇、正己醇、乙二 醇等之醇類，丙酮、甲基乙基酮、環己酮等之酮類，正己 烷、煤油、燈油等之脂肪族烴類，甲苯、二甲苯、甲基萘 等之芳香族烴類，二乙醚、二噁烷、四氫呋喃等醚類，乙 酸乙酯等的酯類，乙腈、異丙腈等腈類，二甲基甲醯胺、 二甲基乙醯胺等醯胺類，大豆油、棉子油等之植物油類， 二甲基亞颯、水等。 再者，氣體載體可舉例有LPG、空氣、氮氣、二氧化 碳、二甲基醚等。 又，用以乳化、分散、延展之界面活性劑、分散劑可 爲例如烷基硫酸酯類、烷基（芳基）磺酸鹽類、聚氧烯烷基 (芳基）醚類、多元醇酯類、木質磺酸鹽等。 再者，作爲用以改善製劑性狀之補助劑可使用例如羧 甲基纖維素、阿拉伯膠、聚乙二醇、硬脂酸鈣等。 上述載體、界面活性劑、分散劑以及補助劑可依據必 要單獨或組合使用。 該等製劑中有效成份之含量並無特別限制’但較好於 乳劑時爲1-75重量％，於粉劑時爲0.3-25重量％，於水合劑 時爲1 - 9 0重量％，於粒劑時爲〇 · 5 -1 0重量％。 又’依據本發明另一態樣，係提供一種農園藝上之害 虫防治方法，包含將有效量之P F 1 3 7 8物質、其對映異構 -12- 200913891 物、其等之混合物、或其等之農園藝上 使用於水面、土壤、於營養液栽培中之 栽培之固體培養基、植物種子、根、塊 〇 至於將有效量之PF 1 3 7 8物質、其 之混合物、或其等之農園藝上可接受之 物或土壤之方法，較好舉例爲撒佈處理 處理（混入、灌注等）、育苗箱處理、_ 衣、被覆）或薰蒸處理等，更好爲水面 育苗箱處理或表面處理。 藉撒佈處理使用於植物時之處理I 、其對映異構物、其等之混合物、或其 受之酸加成鹽作爲有效成份計，每 O.lg〜10kg，更好使用lg〜lkg。 又，使用於植物種子、根、塊莖、 ，有例如對種子浸漬法、粉衣法、塗沫 法、皮膜法或薰蒸法。 浸漬法爲將種子浸漬於液狀藥劑液 法有將粉狀藥劑附著在乾燥狀種子之乾 於水中之種子附著粉狀藥劑之濕粉衣法 劑於混合機內塗佈於種子表面之塗沬法 之吹附法。再者，舉例有將種子與塡充 大小、形狀時，將藥劑混合入塡充劑中 含藥劑之薄膜塗佈於種子上之塗覆法； 可接受之酸加成鹽 營養液、於營養液 莖、球根或根莖上 對映異構物、其等 酸加成鹽使用於植 、水面處理、土壤 I面處理（塗佈、粉 處理、土壤處理、 t，以 P F 1 3 7 8物質 等之農園藝上可接 1 〇畝耕地宜使用 球根或根莖之方法 法、吹附法、造粒 中之方法，而粉衣 粉衣法以及對輕浸 。又有將懸浮狀藥 、吹附於種子表面 劑一起造粒成一定 處理之造粒法、將 於密閉容器內藉由 -13- 200913891 氣化之藥劑對種子消毒之薰蒸法。 本發明之浸透移行性殺蟲劑之使用方法並無特別限制 ，較好爲浸漬法、粉衣法、塗沬法、吹附法、造粒法、皮 膜法。 又，除種子以外，亦可施用於發芽後或自土壤萌芽後 移植、發芽之植物及幼苗植物。藉由浸漬對全體或一部份 進行處理，可保護移植前之該等植物。 使用於植物種子時之處理量並無特別限制，但較好對 每100kg種子，使用PF 13 78物質、其對映異構物、其等之 混合物、或其等之農園藝上可接受之酸加成鹽lg〜l〇kg， 更好100g〜lkg 。 又，本發明之農園藝用殺蟲劑或浸透用移行性殺蟲劑 之土壤施用方法並無特別限制，但較好爲以下舉例方法。 舉例有將含PF 1 3 78物質之粒劑使用於土壤中或土壤 上之方法，尤其較佳之土壤施用方法爲撒佈、帶、溝及附 植穴法。 又，藉由將P F 1 3 7 8物質乳化或溶解於水中之溶液灌 入於土壤中而使用亦爲較佳之土壤施用方法。 除此之外，較佳之土壤施用方法之例’舉例有：爲了 生產野菜及花木類而使用於如水耕栽培及沙耕、NFT (營 養膜技術（Nutrient Film Technique))、石棉耕法等之固形 培養基土耕栽培中之營養液培養系統中之營養液中’以及 稻育苗用之對育苗箱施用（苗床土混合等）方法。又’亦可 直接使用於含蛭石之人工培養土以及含育苗用人工墊片之 -14- 200913891 固形培養基中。 對水面、育苗箱或土壤之PF1378物質、其對映異構 物、其等之混合物、或其等之農園藝上可接受之酸加成鹽 處理量並無特別限制，較好作爲有效成份，每1 0公畝耕地 爲O.lg〜10kg，更好爲ig〜ikg。 本發明之農園藝用殺蟲劑或浸透移行性殺蟲劑可直接 使用或稀釋後使用。又，本發明之農園藝用殺蟲劑或浸透 移行性殺蟲劑可與其他殺菌劑、殺蟲劑、殺蟎劑、除草劑 、植物生長調節劑、肥料等混合使用。作爲可混合之其他 有害生物防治劑舉例有殺菌劑、殺蟎劑、除草劑、植物生 長調節劑。具體言之，舉例有於殺蟲劑手冊（The Pesticide Manual，第 13 版，The Crop Protection Council 發行）以及 涉谷索引（SHIBUYA INDEX，第 10 版，2 00 5 年，SHIBUYA INDEX RESEARCH GROUP發行）中所記載者。 所用之殺蟲劑並無特別限制，但較好爲歐殺松 (acephate)、二氯松（dichlorvos)、EPN、撲滅松（fenitothion) 、益多松（fenamifos)、普硫松（prothiofos)、佈飛松（profenofos) 、白克松（pyraclofos)、甲基陶斯松（chlorpyrifos-methyl)、 殺螟威（chlorfenvinphos)、滅賜松（demeton)、愛殺松 (ethion)、馬拉松（malathion)、繩毒憐（coumaphos)、加福 松（isoxathion)、芬殺松（fenthion)、大利松（diazinon)、硫 敵克（thiodicarb)、得滅克（aldicarb)、歐殺滅（oxamyl)、 安丹（propoxur)、加保利（carbaryl)、丁基滅必蝨（fenobucarb) 、艾芬克（ethiofencarb)、芬硫克（fenothiocarb)、比加普 -15- 200913891 (pirimiearb)、加保扶（carbofuran)、丁基加保扶（carbosulfan) 、肤線威（furathiocarb)、害快威（hyquincarb)、棉鈴威 (alanycarb)、納乃得（methomyl)、免扶克（benfuracarb)、 培丹（cartap)、硫賜安（thiocyclam)、免速達（bensultap)、 大克觸（dicofol)、得脫織（tetradifon)、阿納寧（acrinathrin) 、畢芬寧（bifenthrin)、乙氰菊酯（cycloprothrin)、賽扶寧 (cyfluthrin)、四氟甲醚菊醋（dimefluthrin)、炔戊菊醋 (empenthrin)、五氟菊酯（fenfluthrin)、芬普寧（fenpropathrin) 、炔咪菊酯（imiprothrin)、甲氧节氟菊酯（metofluthrin)、百 滅寧（permethrin)、速滅靈（phenothrin)、異列滅寧 (resmethrin)、七氟菊酯（tefluthrin)、治滅寧（tetramethrin)、 泰滅寧（tralomethrin)、四氧苯菊酯（transfluthrin)、賽滅寧 (cypermethrin)、亞滅寧（deltamethrin)、賽洛寧（cyhalothrin) 、芬瓦特納（fenvalerate)、福化利（fluvalinate)、醚菊酯 (ethofenprox)、三氟酸菊醋（flufenprox)、合芬寧（halfenprox) 、氟矽菊酯（silafluofen)、賽滅淨（cyromazine)、二福隆 (diflubenzuron)、伏蟲脲（teflubenzuron)、氣彌脲（flucycloxuron) 、氟芬隆（flufenoxuron)、六伏隆（hexaflumuron)、祿芬隆 (lufenuron)、諾伐隆（novaluron)、氟幼尿（penfluron)、殺蟲脲 (triflumuron)、克福隆（chlorfluazuron)、汰芬諾克（diafenthiuron) 、稀蟲醋（methoprene)、芬諾克（fenoxycarb) '百利普芬 (pyriproxyfen)、氯蟲醯肼（halofenozide)、得芬諾（tebufenozide) 、滅芬諾（methoxyfenozide)、可芬諾（chromafenozide)、 環蟲腈（dicyclanil)、布芬淨（buprofezin)、合賽多（hexythiazox) -16- 200913891 、三亞輸（amitraz)、殺蟎脒（chlordimeform)、畢達本 (pyridaben)、芬普虫葙（fenpyroxymate)、（flufenerim)、畢汰 芬（pyrimidifen)、D比觸胺（tebufenpyrad)、哩蟲醯胺（tolfenpyrad) 、喃觸醋（fluacrypyrim)' 亞酿觸（acequinocyl)、賽芬織 (cyflumetofen)、氟蟲醢胺（flubendiamide)、乙蟲清（ethiprole)、 芬普尼（fipronil)、乙嚼哩（ethoxazole) ' D比蟲啉（imidacloprid)、 稀陡蟲胺（nitenpyram)、可尼丁（elothianidin)、亞滅培 (acetamiprid)、達特南（dinotefuran)、噻蟲啉（thiacloprid)、阿克 泰（thiamethoxam)、派滅淨（pymetrozine)、聯苯菊醋（bifenazate) 、螺酯（spirodiclofen)、螺甲觸酯（spiromesifen)、氟尼胺 (flonicamid)、溴蟲腈(chlorfenapyr)、(pyriproxyfene)、 因得克（indoxacarb)、啶蟲丙醚（pyridalyl)、賜諾殺 (spinosad)、伊維菌素（avermectin)、絲蟲黴素（milbemycin)、印 楝素（azadirachtin)、尼古丁（nicotine)、魚藤酮（rotenone)、 BT劑、昆蟲病原病毒劑、甲胺基阿維菌素苯甲酸鹽 (emamectinbenzoate)、旋耐妥蘭（spinetoram)、U比氟唾腙 (pyrifluquinazon)、氯蟲醯胺（chlorantraniliprole)、 (cyenopyrafen)、螺蟲乙酯（spirotetramat)、利啦美汀（lepimectin) 、美氟米腙（metaflumizone)、啦拉氟普（pyrafluprole)、卩仕普 (pyriprole)、四氟甲醚菊酯（dimefluthrin)、抗彌哩（fenazaflor)、 伏犠腙（hydramethylnon)、嗖极威（triazamate)。 作爲使用之殺菌劑並無特別限定，但較好舉例爲例如 亞托敏（azoxystrobin)、克收欣（kresoxym-methyl)、三氟 敏（trifloxystrobin)時醚菌胺（orysastrobin)、Π定氧菌酯 -17- 200913891 (picoxystrobin)、（fuoxastrobin)等之甲氧基丙烯酸酯系化 合物；如滅派林（mepanipyrim)、嘧黴胺（pyrimethanil)賽 普洛（cyprodinil)之苯胺基嘧啶系化合物；如三泰芬 (triadimefon)、比多農（bitertanol)、賽福座（triflumizole) 、乙環哩（etaconazole)、普克利（propiconazole)、平克座 (penconazole)、護砂得（flusilazole)、邁克尼（myclobutanil) ' 環 克座（cyproconazole)、得克利（tebuconazole)、菲克利 (hexaconazole)、撲克拉（prochloraz)、砂氟哩（simeconazole)之 π坐系化合物；如滅觸猛（quinomethionate)之嗤Π坐咐系化合物 ;如代森锰（maneb)、代森鋅（zineb)、代森猛鋅（mancozeb)、代 森福美鋅（polycarbamate)、甲基鋅乃浦（propineb)之二硫 代胺基甲酸酯系化合物；如乙黴威（diethofencarb)之苯基 胺基甲酸酯系化合物；如四氯異苯（chlorothalonil)、五氯 硝基苯（quintozene)之有機氯系化合物；如苯菌靈 (benomyl)、甲基硫菌靈（thiophanate-methyl)、卡苯達口坐 (carbendazole)之苯并咪唑系化合物；如甲霜靈（metalaxyl)、惡 霜靈（oxadixyl)、歐護酶（ofurase)本達樂（benalaxyl)、咲 霜靈（furalaxyl)、酯菌胺（cyprofuram)之苯基醯胺系化合 物：如益發靈（dichlofluanid)之次磺酸系化合物；如氫氧 化銅（copper hydroxide)、快得寧銅（oxine-copper)之銅系 化合物；如經基異U惡哩（h y d r ο X y i s ο X a ζ ο 1 e)之異H惡嗖系化 合物；如福賽得（fosetyl-aluminium)、脫克松（tolclofos-methyl)之有基磷系化合物；如勉菌丹（captan)、敵菌丹 (captafol)、滅菌丹（f〇lpet)之N-幽代硫代烷基系化合物； -18- 200913891 如撲滅寧（procymidone)、依普同（iprodione)、維氯嗖寧 (vinchlozolin)之二羧基醯亞胺系化合物；如福多寧 (flutolanil)、滅普寧（mepronil)之苯并苯醯胺系化合物； 如芬普福（fenpropimorph)、達滅芬（dimethomorph)之嗎咐 系化合物；如氫氧化三苯錫（fenthin hydroxide)、乙酸三 苯錫（fenthin acetate)之有機錫系化合物；如略菌腈 (f 1 u d i ο X ο n i 1)、拌種略（f e n p i c 1 ο n i 1)之醯基D比略系化合物； 其他之四氯苯酞（fthalide)、撲殺熱（probenazole)、苯并噻 二哩（acibenzolar-S-methyl)、噻醯菌胺（tiadinil)、（isotianil)、 環丙酸菌胺（carpropamid)、雙氯氰菌胺（diclocymet)、稻 癒醒胺（fenoxanil)、三環哩（tricyclazole)、百快隆（pyroquilon) 、富米綜（ferimzone)、扶吉胺（fluazinam)、克絕 (cymoxanil)、賽福寧（triforine)、比芬諾（pyrifenox)、芬 瑞莫（fenarimol)、苯鏡 D定（fenpropidin)、賓得克利（pencycuron) 、賽座滅（cyazofamid)、環氟菌胺（cyflufenamid)、白克列 (boscalid)、Π比噻菌胺（penthiopyrad)、丙氧喹啉（proquinazid)、 快諾芬（quinoxyfen)、凡殺同（famoxadone)、味哩菌酮 (fenamidone)、異丙菌胺（iprovalicarb)、苯嚷菌胺 (benthiavalicarb-isopropyl)、氟 Π比菌胺（fluopicolide)、必 苯扶（pyribencarb)、嘉賜黴素（kasugamycin)或維達黴素 (validamycin)。 實施例 以下舉例實施例具體說明本發明，但本發明並不限定 -19- 200913891 於該等實施例。 (製劑例） 製劑例1(粒劑） P F 1 3 7 8物質 5重量％ 膨潤土 4 0重量％ 滑石 10重量％ 黏土 4 3重量％ 木質磺酸鈣 2電量％ 使上述成份均一粉碎混合，添加水混練後，造粒乾燥 獲得粒劑。 製劑例2(水合劑） P F 1 3 7 8物質 滑石 白碳 石夕藻土 木質磺酸鈣 月桂基硫酸鈉 將上述成份均一混合 製劑例3 (顆粒水合劑） P F 1 3 7 8物質 滑石 3 0重量％ 5 0重量％ 2重量％ 1 3重量％ 4重量％ 1重量％ 粉碎後獲得水合劑。 3 0重量％ 6 0雷量％ -20- 200913891 糊精 5重量％ 烷基馬來酸共聚物 4重量％ 月桂基硫酸鈉 1重量％ 將上述成份均一粉碎混合’添加水混練後，造粒乾燥 獲得顆粒水合劑。 製劑例4(可流動劑） P F 1 3 7 8物質 2 5重量％ ΡΕΟ聚苯乙烯苯基醚硫酸鹽 5重量％ 丙二醇 6重量％ 膨潤土 1重量％ 黃耆膠1 %水溶液 3重量％ PRONAL EX-3 00(東邦化學工業股份有限公司）0.05 重量％ ADDAC827(KI化成股份有限公司） 0.02 重量％ 水 加至1 0 〇重量％ 上述配方中除黃耆膠1 %水溶液與適當量水以外之全 囂預先混合後，於濕式粉碎機中粉碎。之後’添加黃耆膠 1 %水溶液與剩餘水使成1 〇〇重量％ ’獲得可流動劑。 製劑例5(乳劑） P F 1 3 7 8物質 1 5重量％ Ν,Ν-二甲基甲醯胺 20重量％ -21 - 200913891 5 5重量％ 1 0重量％ 2重量％ 6 0重量％ 3 7重量％ 1重量％ 2重量％ 9 4.5重量％ 2重量％ 1重量％ 〇 . 5重量％Also, in Tetrahedron Letters, 1 997, 3 8 (32), 5 65 5-565 8, Bioscience, Biotechnology and Biochemistry, 2000, 64(1), 111-115 and JP-A-10-2-2 83, report Asperparaline, which is a substance of the genus 16-oxomycin, is paralyzed to silkworms or to Spodoptera exigua, Nilaparuata lugens and alfalfa ( Blattodea) has insecticidal activity and has not been reported for its permeation and migration activity. Further, although various agricultural and horticultural insecticides having permeation and migration properties have been reported so far, it has been confirmed that any of the pharmaceutical agents is resistant to insecticides or difficult-to-control insects, and it is still desired to develop new insecticides. SUMMARY OF THE INVENTION -6-200913891 The present inventors have now found that the PF1378 substance has remarkable insecticidal activity against agricultural or horticultural activity or impregnation of migratory insecticidal activity. The present invention has been completed based on these findings. Accordingly, it is an object of the present invention to provide an agricultural or horticultural insecticide or an infiltrating transitional insecticide which is effective and safe to use. Therefore, according to one aspect of the present invention, there is provided an agricultural and horticultural insecticide comprising a PF 1 3 78 substance, an enantiomer thereof, a mixture thereof, or the like, which is agriculturally and horticulturally acceptable. An acid addition salt is used as an active ingredient. Further, according to another aspect of the present invention, there is provided a method of impregnating a transitional insecticide comprising a PF 1 3 78 substance, an enantiomer thereof, a mixture thereof, or the like, which is agriculturally acceptable An acid addition salt is used as an active ingredient. Furthermore, according to still another aspect of the present invention, there is provided a method for controlling pests in agriculture and horticulture comprising comprising an effective amount of a substance of PF 1 3 78, an enantiomer thereof, a mixture thereof, or the like The acid addition salt acceptable for agriculture and horticulture is suitable for the group consisting of water surface, soil, nutrient solution in nutrient solution cultivation, solid medium cultured in nutrient solution, plant seeds, roots, tubers, bulbs and rhizomes. Object. [Embodiment] The PF 1 3 7 8 substance PF 1 3 78 substance (16-oxoindolizine) can be obtained according to, for example, the method described in The Journal of Antibiotics, 1997, 50(10), 840-846. A culture of 6-oxomycin-imiding bacteria producing bacteria was obtained. In the present invention, not only P F 1 3 7 8 may be used, but also a mixture of the same may be used for the 200913891 image. Further, in the present invention, a horticulturally acceptable acid addition salt of a substance of PF1378 may be used, and as an example thereof, an acid addition salt of a hydrochloride, a nitrate 'sulfate, a phosphate or an acetate is exemplified. . Insecticides for agricultural and horticultural use and impregnated transitional insecticides PF 1378 substances are excellent for controlling pests. Therefore, according to the present invention, there is provided an agricultural and horticultural insecticide and a permeating transitional insecticide comprising a mixture of a PF 1 3 78 substance, an enantiomer thereof or the like as an active ingredient. Further, the PF1378 substance, its enantiomer or a mixture thereof can also be used in the form of a horticulturally acceptable acid addition salt. According to another aspect of the present invention, there is provided a use of a PF 1 3 78 substance, an enantiomer thereof, a mixture thereof, or the like, and a horticulturally acceptable acid addition salt thereof, for use as agricultural and horticultural Insecticides. Further, according to another aspect of the present invention, there is provided a use of a PF 1 3 7 8 substance, an enantiomer thereof, a mixture thereof, or the like, or a horticulturally acceptable acid addition salt thereof, as Soaking the transitional insecticide. The PF 1 3 78 substance exhibiting the insecticidal effect is not particularly limited, but is preferably a lepidopteran pest (for example, Spodo optera litura, Spodoptera exigua, and Pseudaletia). Separata), Mamestra brassicae, Agrotis ipsilon, Trich〇plusia genus, Heliothis genus, Helicoverpa genus Class, Chilo suppressalis, Cnaphalocrocis 200913891 medinalis, Ostrinia nubilalis, Hellulla undalis Fabricius, Parapediasia teterrella, Cotton leaf The genus Endotricha, such as Notarcha derogata, Plodia interpunctella, Pierinae, Pieris rapae, Adoxophyes spp, P. (Grapholita molesta), Adoxophyes, such as the genus Cydia pomonella, and Carposinidae, such as Carposina sasakii Matsumura. Of the genus Lyonetiidae, the genus Lyonetiidae, the genus Artaxa subflava, the genus Euprotis, and the genus Plutella xylostella (Yp〇nomeutidae) ), cotton red bollworm (?6 (^110卩110^£0 8 5丫?丨6 113), etc., 〇616 (^^(136) 'Hyphantria cunea, etc. Arctiidae, Tineola bisselliella, etc., Hemiptera pests (eg 'Myzus persicae, cotton> (Aphis gossypii Glover) ) Aphididae, Delphacodes striatellus, pianth〇pper, Sogatella furcifera, Delphacidae, Black-tailed Nightingale Nephotettix cincti cep s), such as C 丨cade丨丨idae, Trigonotylus caelestialium, Plautia crossota stali Scott, Nezara viridula, and bee sting ( Riptortus clavatus), such as the oak family, Trialeur〇des vaporari Orum), white powder butterfly such as BemiSia tabaei, scale insects such as Pseudaulacaspis pentag〇na Targi〇ni and Pseudococcus comstocki, Tingidae ), the family of the genus Psyllidae, etc., a coleopteran pest (for example, the genus of the genus Sitophilus zeamais, Lisorhoptrus oryzophilus, Callosobruchus chinensis, etc., yellow Beetles such as Tenebrio molitor Linnaeus, Anomala cuprea, Anomala rufocuprea Motschulsky, etc., and the genus (Phyllotreta striolata) and yellow squash ( Aulacophora femoralis, Leptinotarsa. decemlineata, Diabrotica virgifera virgifera, Diabrotica und ecimpunctata howardi, etc., rice leaf worm, ant type occult Lady (Paederus Fuscipes), Cydia pomonella, and Epilachna vigintioctopunctata Fabricius (Epil) (achna), celestial, etc., woven (eg, Tetranychus urticae Koch, Tetranychus kanzawai, Panonychus citvi, Metatetrany chus ulmi (Apple) Leaves (Panonychus uimi), lychee genus Oligonychus, etc., Aculops lycopersici, Aculops pelekassi, Calacarus carinatus, etc. In the Eriophyidae class, the genus Tarsonemidae, such as Polyphagotarsonemus latus, is a genus of the genus Hymenoptera (F1 〇urmite). Bee (Athalia rosae) and other species of the genus Tenthredinidae, etc., Orthoptera pests (eg, planthoppers, etc.), Diptera pests (eg, Museidae -10- 200913891 class 'Culex ( Culex) 'Anopheles', Chironomidae, calliphorini, Sarcophagidae, Fanniidae, Pegoplata, Africa Liriomyza trifolii Bu Rgess), Liriomyza sativae, Liriomyza bryoniae, and other species of the genus Tephritidae, Phoridae, Drosophilidae Classes, Psychodidae, Simuliidae, Tabanidae, Stable fly, Thysanoptera (eg, Southern Yellow Horse (Thrips) Palmi), Frankliniella occidentalis Pergande, Thrips tabci Lin deman, Thrips hauaiiensis, Scirtothrips dorsalis, and Frunkliniella intonsa (Trybom) , Ponticulothrips disospyrosi, etc., plant parasitic nematodes (for example, Root-knot Nematode, root rot nematodes, Heterodera glycines, heart buds such as Neisseria gonorrhoeae) Aphelenchoides, such as Bursaphelenchus xylophilus, etc., are more preferably exemplified by Hemiptera pests, Thysanoptera pests, Diptera, Coleoptera pests, and even better An example is a Hemipteran pest. When the PF1378 substance, its enantiomer, a mixture thereof, or the like, or a horticulturally acceptable acid addition salt thereof, is used as an active ingredient of an agricultural and horticultural insecticide, it may be used as appropriate. A solid carrier, a liquid carrier, a gaseous carrier, a surfactant, a dispersing agent, and other preparations are mixed with an auxiliary agent to form an emulsion, a liquid agent, a suspension agent, a hydrating agent, a powder, and a granule-11 - 200913891, a tablet, an oil It can be used in any dosage form such as a dose, an aerosol, a flowable agent or the like. Examples of the solid carrier include talc, bentonite, clay, kaolin, diatomaceous earth, vermiculite, white carbon, calcium carbonate and the like. Further, examples of the liquid carrier include alcohols such as methanol, n-hexanol and ethylene glycol; ketones such as acetone, methyl ethyl ketone and cyclohexanone; and aliphatic hydrocarbons such as n-hexane, kerosene and kerosene. An aromatic hydrocarbon such as toluene, xylene or methylnaphthalene; an ether such as diethyl ether, dioxane or tetrahydrofuran; an ester such as ethyl acetate; a nitrile such as acetonitrile or isopropionitrile; and dimethylformamidine. Amidoxime such as amine or dimethylacetamide, vegetable oil such as soybean oil or cottonseed oil, dimethyl hydrazine, water, and the like. Further, the gas carrier may, for example, be LPG, air, nitrogen, carbon dioxide, dimethyl ether or the like. Further, the surfactant, dispersant used for emulsifying, dispersing, and stretching may be, for example, an alkyl sulfate, an alkyl (aryl) sulfonate, a polyoxyalkylene (aryl) ether, or a polyhydric alcohol. Esters, lignosulfonates, and the like. Further, as the auxiliary agent for improving the properties of the preparation, for example, carboxymethylcellulose, gum arabic, polyethylene glycol, calcium stearate or the like can be used. The above carriers, surfactants, dispersing agents and auxiliary agents may be used singly or in combination as necessary. The content of the active ingredient in the preparations is not particularly limited 'but preferably from 1 to 75% by weight in the case of the emulsion, from 0.3 to 25% by weight in the case of the powder, and from 1 to 90% by weight in the case of the hydrating agent. When the agent is 〇·5 -10% by weight. Further, according to another aspect of the present invention, there is provided a method for controlling pests in agriculture and horticulture comprising comprising an effective amount of a PF 1 37 8 substance, an enantiomer thereof -12-200913891, a mixture thereof, or The solid medium, plant seeds, roots, and lumps used in the cultivation of water, soil, and nutrient solution for agricultural and horticultural purposes, such as an effective amount of PF 1 378 substance, a mixture thereof, or the like The method for horticulturally acceptable things or soil is preferably, for example, a sprinkling treatment (mixing, infusion, etc.), a nursery box treatment, a garment, a coating, or a fumigation treatment, and is preferably treated as a water surface nursery box or Surface treatment. The treatment of the plant I, its enantiomers, mixtures thereof, or the acid addition salts thereof as an active ingredient by sprinkling, per lg~10 kg, preferably lg~lkg . Further, it is used in plant seeds, roots, tubers, and, for example, a seed dipping method, a powder coating method, a coating method, a film method, or a fumigation method. The dipping method is a method in which a seed is immersed in a liquid chemical solution, and a wet powder coating agent in which a powdery drug is adhered to a dry seed in a dry state, and a powdery drug is applied to a surface of a seed in a mixer. The method of blowing the law. Further, for example, when the seed and the size and shape are filled, the coating method in which the drug is mixed into the medicated drug-containing film is applied to the seed; the acceptable acid addition salt nutrient solution and the nutrient solution Enantiomers on stems, bulbs or rhizomes, and their acid addition salts are used in planting, surface treatment, soil surface treatment (coating, powder treatment, soil treatment, t, PF 1 3 7 8 substances, etc.) For agricultural and horticultural use, it is advisable to use bulbs or rhizomes, method of blowing, or granulation, and powder coating method and light immersion. The granulation method in which the surface agent is granulated together into a certain treatment, and the fumigation method for sterilizing the seeds by the gasification of the gasification in the sealed container by -13-200913891. The use method of the immersed transition insecticide of the present invention is not used. In particular, it is preferably a dipping method, a powder coating method, a coating method, a blowing method, a granulation method, or a film method. Further, in addition to the seed, it may be applied to a plant which is transplanted or germinated after germination or after germination from the soil. And seedling plants. by impregnation for the whole or one The treatment is carried out to protect the plants before transplantation. The amount of treatment used in the plant seeds is not particularly limited, but it is preferred to use PF 13 78 substance, its enantiomer, etc. per 100 kg of seed. a mixture, or a horticulturally acceptable acid addition salt of the mixture, lg~l〇kg, more preferably 100g~lkg. Further, the agricultural application of the agricultural and horticultural insecticide or the infiltration insecticide of the present invention The method is not particularly limited, but is preferably exemplified by the following examples. Examples of methods for using granules containing PF 1 3 78 in soil or on soil, particularly preferred methods of soil application are spreading, belt, ditch and Further, a method of applying soil by using a solution in which a PF 1 37 substance is emulsified or dissolved in water is preferably used. In addition, a preferred example of a soil application method is used. 'Examples include: in the nutrient solution culture system in the solid culture medium cultivation such as hydroponic cultivation and sanding, NFT (Nutrient Film Technique), asbestos cultivation, etc., for the production of wild vegetables and flowers. Nutrient solution 'And rice seedlings for seedling box application (seed bed soil mixing, etc.) method. Also 'can also be directly used in vermiculite-containing artificial culture soil and artificial seedlings containing artificial seedlings -14-200913891 solid medium. The amount of the PF1378 substance, the enantiomer, the mixture thereof, or the like, and the horticulturally acceptable acid addition salt of the seedling box or the soil are not particularly limited, and are preferably used as an active ingredient. The 0-acre arable land is O.lg~10kg, more preferably ig~ikg. The agricultural and horticultural insecticide or the impregnated transitional insecticide of the present invention can be used directly or diluted. Further, the agricultural and horticultural use of the present invention Insecticides or impregnated transitional insecticides can be used in combination with other fungicides, insecticides, acaricides, herbicides, plant growth regulators, fertilizers, and the like. Examples of other pest control agents that can be mixed include fungicides, acaricides, herbicides, and plant growth regulators. Specifically, examples are given in the Pesticide Manual (13th edition, The Crop Protection Council) and Shibuya Index (SHIBUYA INDEX, 10th edition, 2005, SHIBUYA INDEX RESEARCH GROUP). Recorded. The insecticide to be used is not particularly limited, but is preferably acephate, dichlorvos, EPN, fenitothion, fenamifos, prothiofos, Profenofos, pyraclofos, chlorpyrifos-methyl, chlorfenvinphos, demeton, ethion, malathion, rope poison ( Coumaphos), isoxathion, fenthion, diazinon, thiodicarb, aldicarb, oxamyl, propoxur, plus Carbaryl, fenobucarb, ethiofencarb, fenothiocarb, Bizap-15-200913891 (pirimiearb), carbofuran, butyl plus Carbosulfan, furathiocarb, hyquincarb, alanycarb, methomyl, benfuracarb, cartap, thiocyclam ), speed-free (bensultap), big grams Dicofol), tetradifon, acrinathrin, bifenthrin, cycloprothrin, cyfluthrin, dimefluthrin, acetylacetonate (empenthrin), fenfluthrin, fenpropathrin, imiprothrin, metofluthrin, permethrin, phenothrin, Resmethrin, tefluthrin, tetramethrin, tralmethrin, transfluthrin, cypermethrin, arsenin Deltamethrin), cyhalothrin, fenvalerate, fluvalinate, ethofenprox, flufenprox, halfenprox, valerian Ester (silafluofen), cyromazine, diflubenzuron, teflubenzuron, flucycloxuron, flufenoxuron, hexaflumuron, lufenlong (lufenuron), Norvaron (novaluron), penfluron, penfluron, triflumuron, chlorfluazuron, diafenthiuron, metoprene, fenoxycarb Pyriproxyfen, halofenozide, tebufenozide, methoxyfenozide, chromafenozide, dicyclanil, buprofezin, co-race (hexythiazox) -16- 200913891 , amitraz, chlordimeform, pyridaben, fenpyroxymate, flufenerim, pyrimidifen, D ratio Tebufenpyrad, tolfenpyrad, fluacrypyrim's acequinocyl, cyflumetofen, flubendiamide, ethiprole, Fipronil, ethoxazole 'D than imidacloprid, nitenpyram, elothianidin, acetamiprid, dinotefuran , thiacloprid, arbo Thiamethoxam, pymetrozine, bifenazate, spirodiclofen, spiromesifen, flonicamid, chlorfenapyr, Pyriproxyfene), indoxacarb, pyridalyl, spinosad, avermectin, milbemycin, azadirachtin, nicotine Nicotine), rotenone, BT agent, entomopathogenic virus agent, emamectinbenzoate, spinetoram, U-pyrefluquinazon, chlorella Chlorantraniliprole, (cyenopyrafen), spirotetramat, lepimectin, metaflumizone, pyrafluprole, pyriprole, IV Dimethfluthrin, fenazaflor, hydramethylnon, triazamate. The fungicide to be used is not particularly limited, but is preferably exemplified by, for example, azoxystrobin, kresoxym-methyl, triflamine (trifloxystrobin), oryzastrobin, and oxytocin a methoxy acrylate compound such as ester-17-200913891 (picoxystrobin) or (fuoxastrobin); an anilinopyrimidine compound such as mepanipyrim or pyrimethanil cyprodinil; Triadimefon, bitertanol, triflumizole, etaconazole, propiconazole, penconazole, flusilazole, McAfee (myclobutanil) ' cyproconazole, tebuconazole, hexaconazole, prochloraz, simeconazole π-sit compounds; such as quinomethionate Sputum lanthanide compounds; such as maneb, zineb, mancozeb, polycarbamate, propionb dithioamine a formate compound; a phenyl carbamate compound such as diehofencarb; an organochlorine compound such as chlorothalonil or quintozene; Benomyl, thiophanate-methyl, carbendazole benzimidazole-based compounds; such as metalaxyl, oxadixyl, European enzymes ( Ofurase) Benalaxyl, furalaxyl, cyprofuram phenylamine compound: such as chlorinated compounds of dichlofluanid; such as copper hydroxide ), a copper compound of oxine-copper; such as a humic compound of the hydr X ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; fo fo fo fo fo fo fo fo fo fo fo fo fo fo fo fo -aluminium), tolclofos-methyl based phosphorus compounds; such as captan, captafol, sterilized dan (f〇lpet) N-perithioalkyl Line compound; -18- 200913891 such as procymidone, iprodione, vitamin a dicarboxy quinone imine compound of vinchlozolin; such as flutolanil, mepronil benzophenamide compound; such as fenpropimorph, dimethomorph a lanthanide compound; an organotin-based compound such as fenthin hydroxide or fenthin acetate; such as sputum nitrile (f 1 udi ο X ο ni 1), seed dressing (fenpic) 1 ο ni 1) thiol D ratio slightly compound; other fthalide, probenazole, acibenzolar-S-methyl, tiadinil , (isotianil), carpropamid, diclocymet, fenoxanil, tricyclazole, pyroquilon, fermizone ), fluazinam, cymoxanil, triforine, pyrifenox, fenarimol, fenpropidin, pencycuron, Cyazofamid, cyflufenamid, Boscalid, penthiopyrad, proquinazid, quinoxyfen, famoxadone, fenamidone, isopropylprocarb ), benthiavalicarb-isopropyl, fluopicolide, pyribencarb, kasugamycin or validamycin. EXAMPLES Hereinafter, the present invention will be specifically described by way of examples, but the present invention is not limited to the examples. (Formulation Example) Formulation Example 1 (granules) PF 1 3 7 8 substance 5% by weight Bentonite 40% by weight Talc 10% by weight Clay 4 3 % by weight Calcium lignosulfonate 2 Electric % The above ingredients were uniformly pulverized and mixed, and water was added. After the kneading, granulation is dried to obtain granules. Formulation Example 2 (Hydrating Agent) PF 1 3 7 8 Substance talc White Carbonate 藻 土 Soil Calcium sulfonate Lauryl Sodium Sulfate The above ingredients are uniformly mixed. Example 3 (Particle Hydrating Agent) PF 1 3 7 8 Substance talc 3 0 Weight% 50% by weight 2% by weight 13% by weight 4% by weight 1% by weight A hydrating agent is obtained after pulverization. 30% by weight 6 0 ray % -20- 200913891 dextrins 5 weight % alkyl maleic acid copolymer 4 weight % sodium lauryl sulfate 1% by weight The above ingredients are uniformly pulverized and mixed 'added water and mixed, granulated and dried A particulate hydrating agent is obtained. Formulation Example 4 (flowable agent) PF 1 3 7 8 substance 2 5 wt% ΡΕΟ polystyrene phenyl ether sulfate 5 wt% propylene glycol 6 wt% bentonite 1 wt% xanthan gum 1% aqueous solution 3 wt% PRONAL EX- 3 00 (Dongbang Chemical Industry Co., Ltd.) 0.05% by weight ADDAC827 (KI Chemical Co., Ltd.) 0.02% by weight Water added to 10% by weight of the above formula except for 1% aqueous solution of xanthan gum and appropriate amount of water After premixing, it was pulverized in a wet pulverizer. Thereafter, a 1% aqueous solution of xanthan gum and 1% by weight of residual water were added to obtain a flowable agent. Formulation Example 5 (emulsion) PF 1 3 7 8 substance 15 wt% Ν, Ν-dimethylformamide 20% by weight -21 - 200913891 5 5 wt% 1 0 wt% 2 wt% 6 0 wt% 3 7 Weight% 1% by weight 2% by weight 9 4.5% by weight 2% by weight 1% by weight 〇. 5% by weight
Solvesso 150(ExxonMobil 有限公司） 聚氧乙釀院基方基酸 將上述成份均一混合，溶解後獲得乳劑。 製劑例6(粉劑） P F 1 3 7 8物質 黏土 滑石 硬脂酸鈣 將上述成份均一混合或得粉劑。 製劑例7[DL粉劑] P F 1 3 7 8物質 DL滑石 白碳 硬脂酸鈣 輕質流動石躐 將上述成份均一混合獲得粉劑。 製劑例8(微粒劑F) P F 1 3 7 8物質 載體 白碳Solvesso 150 (ExxonMobil Co., Ltd.) Polyoxyethylene base acid The above ingredients are uniformly mixed and dissolved to obtain an emulsion. Formulation Example 6 (powder) P F 1 3 7 8 Material Clay Talc Calcium Stearate The above ingredients are uniformly mixed or powdered. Formulation Example 7 [DL powder] P F 1 3 7 8 substance DL talc White carbon Calcium stearate Light mobile stone 躐 The above ingredients were uniformly mixed to obtain a powder. Formulation Example 8 (Particle F) P F 1 3 7 8 Substance Carrier White carbon
Hysol SAS-296 2重量％ 9 4重量％ 2重量％ 2重量％ 22- 200913891 上述成份均一混合獲得粉劑。 (試驗例） <浸根處理試驗> 試驗例 1灰稻 1¾ (Smaller Brown Planthopper)防治試驗 於水耕栽培之小麥苗根部以於1 0 %丙酮-水中調製成特 定濃度之藥液處理。由根部吸收藥劑3天後，於其中放養 灰稻蝨2齡幼蟲1 0隻。隨後，放置於2 5 °C恆溫室（1 6小時明 亮期-8小時黑暗期）中。觀察放養3天後蟲的生死，以下式 算出死蟲率。試驗係以2連制進行。 死蟲率（％) = ·{死亡蟲數/(生存蟲數+死亡蟲數）}χ100 如表1所示，可看出P F 1 3 7 8物質之浸透移行殺蟲活性 相對於對照化合物麴黴哌帕胺Α顯現極高活性。 又於本試驗中使用之PF1378物質及麴黴哌帕胺A係 依據 The Journal of Antibiotics, 1997，50( 1 0), 840-846戶斤 記載之方法獲得。以下試驗例中亦相同。 表1各藥劑處理量相關之死蟲率（％) 藥劑名 藥量㈣/苗） 0.5 PF1378物質 100 麴黴哌帕胺A 0 試驗例2稻葉蟲（Trig〇notylus caelestialium)防治試驗 -23- 200913891 於水耕栽培之小麥苗根部以於1 〇 %丙酮-水中調製成特 定濃度之藥液處理。由根部吸收藥劑3天後，於其中放養2 齡幼蟲。隨後，放置於2 5 °C恆溫室（1 6小時明亮期-8小時黑 暗期）中。觀察放養3天後蟲的生死，以下式算出死蟲率。 試驗係以2連制進行。 死蟲率（％)={死亡蟲數/ (生存蟲數+死亡蟲數）}χ1〇〇 如表2所示’可看出PF1378物質對於稻葉蟲具有高的 浸透移行殺蟲活性。 <土壤灌注處理試驗> 試驗例3灰稻蝨防治試驗 於盆栽栽培之稻苗’以於1 0 %丙酮-水中調製成特定濃 度之藥液進行土壤灌注處理。放置3天後，於其中放養2齡 幼蟲。隨後’放置於2 5 °C恆溫室（1 6小時明亮期· 8小時黑 暗期）中。觀察放養3天後蟲的生死，以下式算出死蟲率。 試驗係以2連制進行。 死蟲率（％) = {死亡蟲數/(生存蟲數+死亡蟲數）}xl00 如表3所示’顯示PF1378物質對灰稻蝨之高浸透移行 殺蟲活性。 -24- 200913891 試驗例4褐飛^(Nilaparuata lugens)防治試驗 藉由與試驗例3同樣之試驗方法，算出對褐飛蝨2齡幼 蟲之死蟲率。如表3所示，顯示PF 1 3 7 8物質對褐飛蝨有高 浸透移行殺蟲活性。 試驗例5白背飛|^(Sogatella furcifera)防治試驗 藉由與試驗例3同樣之試驗方法，算出對白背飛蝨2齡 幼蟲之死蟲率。如表3所示，顯示PF 1 3 78物質對白背飛蝨 有高浸透移行殺蟲活性。 試驗例6黑尾夜禪（Nephotettix cincticeps)防治試驗 藉由與試驗例3同樣之試驗方法，算出對黑尾夜禪2齡 幼蟲之死蟲率。如表3所示，顯示PF 1 3 7 8物質對黑尾夜禪 有高浸透移行殺蟲活性。 試驗例7西方花薊馬（Frankliniella occidentalis)防治試驗 於盆栽栽培之胡瓜苗，以於1 〇 %丙酮-水中調製成特定 濃度之藥液進行土壤灌注處理。放置4天後，自胡瓜苗切 除直徑2.8 cm之葉盤’於其上放養1齡幼蟲。隨後，放置 於2 5 °C恆溫室（1 6小時明亮期-8小時黑暗期）中。觀察放養 6天後蟲的生死，以下式算出死蟲率。試驗係以2連制進行 〇 死蟲率（％) = {死亡蟲數/(生存蟲數+死亡蟲數）}>〇00 -25- 200913891 如表3所示，顯示PF1378物質對西方花薊馬之高浸透 移行殺蟲活性。 <食葉撒佈試驗> 試驗例8灰稻蝨防治試驗 於盆栽栽培之稻苗，以於10%丙酮-水中調製成50ppm 之藥液進行莖葉撒佈處理。風乾後，於其中放養2齢幼蟲 。隨後，放置於25°C恆溫室（16小時明亮期-8小時黑暗期） 中。觀察放養3天後蟲的生死，以下式算出死蟲率。試驗 係以2連制進行。 死蟲率（％) = {死亡蟲數/(生存蟲數+死亡蟲數）}xl〇〇 如表4所示，顯示P F 1 3 7 8物質對灰稻蝨亦顯示莖葉撒 佈處理之殺蟲活性。 試驗例9褐飛蝨防治試驗 藉由與試驗例8同樣之試驗方法，算出對褐飛蝨2齡幼 蟲之死蟲率。如表4所示，顯示PF 1 3 78物質對褐飛蝨亦顯 示莖葉撒佈處理之殺蟲活性。 試驗例10白背飛蝨防治試驗 藉由與試驗例8同樣之試驗方法，算出對白背飛蝨2齡 -26- 200913891 幼蟲之死蟲率。如表4所示，顯示PF 1 3 7 8物質對白背飛蝨 亦顯示莖葉撒佈處理之殺蟲活性。 試驗例1 1黑尾夜禪防治試驗 藉由與試驗例8同樣之試驗方法，算出對黑尾夜禪2齡 幼蟲之死蟲率。如表4所示，顯示PF 1 3 7 8物質對黑尾夜禪 亦顯示莖葉撒佈處理之殺蟲活性。 試驗例12 種棉$牙（Aphis gossypii Glover)防治試驗 自盆栽栽培之胡瓜切除直徑2.0cm之葉盤’於其上撒 佈成爲50%丙酮-水（加用〇·〇5% Tween20)般調製之特定濃 度之藥液。風乾後，於其中放養1齡幼蟲。隨後，放置於 2 5 t恆溫室（1 6小時明亮期-8小時黑暗期）中。觀察放養3 天後蟲的生死，以下式算出死蟲率。試驗係以2連制進行 死蟲率（％) = ·{死亡蟲數/(生存蟲數+死亡蟲數）}xl〇〇 如表4所示，顯示PF 1 3 78物質對種棉蚜亦顯示莖葉撒 佈處理之殺蟲活性。 試驗例1 3西方花萷馬防治試驗 自盆栽栽培之菜豆切除直徑2.8cm之葉盤’於其上撒 佈成爲5 0 %丙酮-水（加用〇 · 〇 5 % T w e e η 2 0 )般調製之特定濃 -27- 200913891 度之藥液。風乾後，於其中放養1齢幼蟲。隨後，放置於 25 °C恆溫室（1 6小時明亮期-8小時黑暗期）中。觀察放養3 天後蟲的生死，以下式算出死蟲率。試驗係以2連制進行 死蟲率（％) = {死亡蟲數/(生存蟲數+死亡蟲數）}xl〇〇 如表4所示，顯示PF 1 3 7 8物質對西方花薊馬亦顯示莖 葉撒佈處理之殺蟲活性。 表 2 PF 1 3 78S 丨勿質對稻葉蟲 之殺蟲效果 蟲種 處理濃度&g/苗） 死蟲率(％) 稻葉蟲 0.5 100 表3 PF 1 3 78物質對各種害蟲之殺蟲效果 蟲種 處理濃度(mg/苗） 死蟲率(％) 灰稻蝨 1.0 100 白背飛蝨 1.0 100 褐飛1¾ 1.0 100 黑尾夜禪 1.0 100 西方花薊馬 2.0 100 -28 - 200913891 表4 PF 1 3 78物質對各種害蟲之殺蟲效果 蟲種 處理濃度(ppm) 死蟲率(％) 灰稻蝨 100 100 白背飛1¾ 100 100 褐飛蟲 100 100 黑尾夜禪 100 100 西方花薊馬 100 100 種棉蚜 100 100 -29-Hysol SAS-296 2% by weight 9.4% by weight 2% by weight 2% by weight 22-200913891 The above ingredients are uniformly mixed to obtain a powder. (Test Example) <Immersion Root Treatment Test> Test Example 1 Smaller Brown Planthopper Control Test The roots of wheat seedlings in hydroponic cultivation were treated with a chemical solution of a specific concentration in 10% acetone-water. After the agent was absorbed from the root for 3 days, 10 of the 2nd instar larvae of the gray rice cultivars were stocked therein. Subsequently, it was placed in a constant temperature room at 25 ° C (1 6 hours bright period - 8 hours dark period). The life and death of the insects were observed after 3 days of stocking, and the mortality rate was calculated by the following formula. The test was carried out in two-piece system. Dead insect rate (%) = · {Number of dead insects / (number of living insects + number of dead insects)} χ 100 As shown in Table 1, it can be seen that the immersing and insecticidal activity of PF 1 3 7 8 relative to the control compound 麴Mold piperazine quinones exhibit extremely high activity. The PF1378 substance and the ciprofloxacin A used in this test were obtained according to the method described in The Journal of Antibiotics, 1997, 50 (10), 840-846. The same is true in the following test examples. Table 1 Insecticide rate (%) related to the amount of each treatment agent Pharmacy name (four) / seedlings 0.5 PF1378 substance 100 麴Mimper piperacamine A 0 Test Example 2 Test of control of rice worm (Trig〇notylus caelestialium)-23- 200913891 The roots of the wheat seedlings cultivated in the hydroponic cultivation are treated with a specific concentration of the chemical solution in 1% acetone-water. After the agent was absorbed from the root for 3 days, the 2nd instar larvae were stocked therein. Subsequently, it was placed in a constant temperature room at 25 ° C (1 6 hours bright period - 8 hours dark period). The life and death of the insects after 3 days of stocking were observed, and the mortality rate was calculated by the following formula. The test was carried out in two-piece system. Dead insect rate (%) = {number of dead insects / (number of living insects + number of dead insects)} χ 1 〇〇 As shown in Table 2, it can be seen that PF1378 substance has high permeation and insecticidal activity against rice leaf worms. <Soil perfusion treatment test> Test Example 3 Control experiment of gray rice bran The rice seedlings cultivated in pot culture were subjected to soil infusion treatment by preparing a chemical liquid having a specific concentration in 10% acetone-water. After 3 days of placement, 2nd instar larvae were stocked therein. Subsequently, it was placed in a constant temperature room at 25 ° C (1 6 hours bright period · 8 hours dark period). The life and death of the insects after 3 days of stocking were observed, and the mortality rate was calculated by the following formula. The test was carried out in two-piece system. Dead insect rate (%) = {number of dead insects / (number of living insects + number of dead insects)} xl00 As shown in Table 3, 'the PBS1378 substance showed high insecticidal activity against gray rice blast. -24- 200913891 Test Example 4 Nilaparuata lugens control test The mortality rate of the 2nd instar larvae of the brown planthopper was calculated by the same test method as in Test Example 3. As shown in Table 3, it was shown that the PF 1 3 7 8 substance had high soaking and insecticidal activity against brown planthopper. Test Example 5: Sogatella furcifera control test The mortality rate of the 2nd instar larvae of the whitebacked planthopper was calculated by the same test method as in Test Example 3. As shown in Table 3, it was shown that the PF 1 3 78 substance had high soaking and insecticidal activity against the whitebacked planthopper. Test Example 6 Nephotettix cincticeps control test By the same test method as in Test Example 3, the mortality rate of the 2nd instar larvae of the black-tailed bud was calculated. As shown in Table 3, it was shown that the PF 1 3 7 8 substance had high soaking and insecticidal activity against the black tail zen. Test Example 7 Frankliniella occidentalis control test The potted cultivar was planted in a 1 〇% acetone-water solution to a specific concentration of the chemical solution for soil infusion treatment. After 4 days of storage, the leaf discs of 2.8 cm in diameter were cut from the squash seedlings and the 1st instar larvae were stocked thereon. Subsequently, it was placed in a constant temperature room at 25 ° C (1 6 hours bright period - 8 hours dark period). The life and death of the insects were observed after 6 days of stocking, and the mortality rate was calculated by the following formula. The test system was carried out in a two-line system (%) = {number of dead insects / (number of living insects + number of dead insects)} > 〇 00 -25- 200913891 As shown in Table 3, showing PF1378 substance against western flowers Hummer's high soaking and migration insecticidal activity. <Foliage spread test> Test Example 8 Gray rice bran test The potted seedling was planted in a 10% acetone-water mixture to prepare a 50 ppm chemical solution for stem and leaf spreading treatment. After air drying, 2 larvae are stocked therein. Subsequently, it was placed in a constant temperature room at 25 ° C (16 hours bright period - 8 hours dark period). The life and death of the insects after 3 days of stocking were observed, and the mortality rate was calculated by the following formula. The test was carried out in two-piece system. Dead insect rate (%) = {number of dead insects / (number of living insects + number of dead insects)} xl 〇〇 as shown in Table 4, showing that PF 1 3 7 8 substances also showed the handling of stems and leaves Insecticidal activity. Test Example 9 Brown planthopper control test The mortality rate of the 2nd instar larvae of the brown planthopper was calculated by the same test method as in Test Example 8. As shown in Table 4, it was shown that the PF 1 3 78 substance also showed the insecticidal activity of the stem and leaf spreading treatment on the brown planthopper. Test Example 10 Whitebacked planthopper control test The mortality rate of the 2nd instar -26-200913891 larvae of the whitebacked planthopper was calculated by the same test method as in Test Example 8. As shown in Table 4, it was shown that the PF 1 3 7 8 substance also showed insecticidal activity against the white-backed planthopper. Test Example 1 1 Black-tailed meditation prevention test The mortality rate of the 2nd instar larvae of the black-tailed bud was calculated by the same test method as in Test Example 8. As shown in Table 4, it was shown that the PF 1 3 7 8 substance also showed the insecticidal activity of the stem and leaf spreading treatment. Test Example 12 Aphis gossypii Glover control test was prepared from a potted cultivated courgette cut off a 2.0 cm diameter leaf disc onto which 50% acetone-water (plus 〇·〇 5% Tween20) was prepared. a specific concentration of the drug solution. After air drying, the 1st instar larvae were stocked therein. Subsequently, it was placed in a 25 t constant temperature chamber (16 hours bright period - 8 hours dark period). The life and death of the insects were observed after 3 days of stocking, and the mortality rate was calculated by the following formula. The test system uses the two-line system to carry out the mortality rate (%) = · {number of dead insects / (number of living insects + number of dead insects)} xl 〇〇 as shown in Table 4, showing that PF 1 3 78 substances are also Shows the insecticidal activity of stem and leaf spreading treatment. Test Example 1 3 Western flower thrip horse control test The pot leaf of the 2.8 cm diameter cut from the potted cultivated bean was sprinkled thereon to become 50% acetone-water (plus 〇·〇5 % T wee η 2 0 ) Modulate the specific concentrated -27-200913891 degree liquid. After air drying, stock one larvae. Subsequently, it was placed in a constant temperature room at 25 °C (1 6 hours bright period - 8 hours dark period). The life and death of the insects were observed after 3 days of stocking, and the mortality rate was calculated by the following formula. The test system used the two-line system to carry out the mortality rate (%) = {number of dead insects / (number of living insects + number of dead insects)} xl 〇〇 as shown in Table 4, showing PF 1 3 7 8 substances against western flower hummer It also shows the insecticidal activity of stem and leaf spreading treatment. Table 2 PF 1 3 78S 杀 质 对 对 对 对 对 对 对 & & & & & & & & & & & & & & & 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 Insect treatment concentration (mg/苗) Dead insect rate (%) Gray rice 虱 1.0 100 White backed cockroach 1.0 100 Brown fly 13⁄4 1.0 100 Black tailed zen 1.0 100 Western flower 蓟 horse 2.0 100 -28 - 200913891 Table 4 PF 1 3 78 insecticidal effects of various insect pests (ppm) dead insect rate (%) gray rice blast 100 100 white back fly 13⁄4 100 100 brown fly 100 100 black tail night zen 100 100 western flower 蓟 horse 100 100 cotton quilts 100 100 -29-