TWI809148B - Composition comprising eutectic mixture of boscalid and a strobilurin fungicide, preparing method thereof, and combating or controlling fungi method - Google Patents

Composition comprising eutectic mixture of boscalid and a strobilurin fungicide, preparing method thereof, and combating or controlling fungi method Download PDF

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TWI809148B
TWI809148B TW108124806A TW108124806A TWI809148B TW I809148 B TWI809148 B TW I809148B TW 108124806 A TW108124806 A TW 108124806A TW 108124806 A TW108124806 A TW 108124806A TW I809148 B TWI809148 B TW I809148B
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eutectic mixture
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fungicide
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fluoxastrobin
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蘇嘉塔 東迪拉姆 德賽
帕瑞許 維塔爾達斯 塔拉堤
嘉戴夫 拉尼肯特 夏洛夫
維克蘭 拉尼肯特 夏洛夫
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印度商Upl有限公司
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    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/541,3-Diazines; Hydrogenated 1,3-diazines
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/88Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms six-membered rings with three ring hetero atoms
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/12Powders or granules
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/44Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids
    • A01N37/50Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids the nitrogen atom being doubly bound to the carbon skeleton

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  • Plant Pathology (AREA)
  • Engineering & Computer Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Agronomy & Crop Science (AREA)
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Abstract

The present invention relates to a eutectic mixture of boscalid and strobilurin fungicide. Agrochemical compositions comprising a eutectic mixture of boscalid and a strobilurin fungicide and a method of controlling phytopathogenic fungi using said compositions are also provided.

Description

包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物、 其製備程序及對抗或控制真菌方法 Compositions comprising eutectic mixtures of bakleyl and strobilurin fungicides, Its preparation procedure and method for combating or controlling fungi

本發明係關於一種組成物,其包含白克列(boscalid)及嗜球果傘素(strobilurin)殺真菌劑之共熔混合物。本發明進一步關於一種用於配製包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物之程序,以及關於一種使用該等組成物控制植物病原性真菌之方法。 The present invention relates to a composition comprising a eutectic mixture of boscalid and strobilurin fungicides. The present invention further relates to a process for formulating a composition comprising a eutectic mixture of bacrine and strobilurin fungicides, and to a method of using such compositions for controlling phytopathogenic fungi.

白克列係一種已知為琥珀酸去氫酶抑制劑的殺真菌劑。其係一種殺真菌劑,在植物葉內具有透層(translaminar)及向頂(acropetal)移動,提供預防性及某些情況下的治療作用。其抑制孢子發芽、發芽管伸長,並且亦有效地抑制真菌發育的所有其他階段。白克列係用以控制交鏈胞枯萎病(Alternaria blight)、葡萄胞病(Botrytis)、白粉病(Powdery mildew)、紫斑病(Purple blotch)、銹病(Rust)、葉斑病(Leaf spot)、圓盾斑點病(Target spot)、灰黴菌(Grey module),及莖腐病(Stem rot)。 Bakret is a family of fungicides known as succinate dehydrogenase inhibitors. It is a fungicide that has translaminar and acropetal migration within plant leaves, providing preventive and in some cases curative action. It inhibits spore germination, germination tube elongation, and also effectively inhibits all other stages of fungal development. Baccarat series are used to control Alternaria blight, Botrytis, Powdery mildew, Purple blotch, Rust, Leaf spot, Target spot, Gray module, and Stem rot.

為了擴大活性範圍以及增強殺真菌控制的有效性,通常將琥珀酸去氫酶抑制劑諸如白克列與其他類別的殺真菌活性成分組合。其中一類重要的殺真菌劑係醌外抑制劑(QoI)。 In order to broaden the spectrum of activity and enhance the effectiveness of fungicidal control, succinate dehydrogenase inhibitors, such as bacilli, are often combined with other classes of fungicidally active ingredients. One of the important class of fungicides is quinone exo-inhibitors (Q o I).

嗜球果傘素係QoI抑制殺真菌劑,並藉由與粒線體呼吸中之QoI位點之細胞色素bc1複合體結合來抑制真菌呼吸。這些殺真菌劑係藉由抑制真菌進行正常呼吸的能力而作用。該等嗜球果傘素雙化學物質具有非常特定的標靶位點或作用模式(mode-of-action,MOA)。已知嗜球果傘素係用以控制真菌,諸如:溫帶穀物上的小麥白粉病菌(Erysiphe graminis)、鏽病菌屬病菌(Puccinia spp.)、穎枯殼小球腔菌(Leptosphaeria nodorum)、小麥殼針孢(Septoria tritici)及圓核腔菌(Pyrenophora teres),稻米上的稻瘟病菌(Pyricularia oryzae)及立枯絲核菌(Rhizoctonia solani);葡萄藤蔓上的葡萄露菌病菌(Plasmopara viticola)及葡萄鉤絲殼菌(Uncinula necator);葫蘆科上的蒼耳單絲殼菌(Sphaerotheca fuliginea)、及南瓜假霜黴(Pseudoperonospora cubensis);馬鈴薯及番茄上的馬鈴薯腐疫菌(Phytophthora infestans)及番茄夏疫病菌(Alternaria solani);花生上的花生球腔菌(Mycosphaerella arachidis)、立枯絲核菌(Rhizoctonia solani)及小核菌(Sclerotium rolfsii);桃子上的鏈核盤菌屬(Monilinia spp.)及黑星病菌(Cladosporium carpophilum);草皮上的腐黴屬(Pythium spp.)及立枯絲核菌(Rhizoctonia solani);香蕉上的球腔菌屬(Mycosphaerella spp.);美洲胡桃上的卡利金冷枝孢菌(Cladosporium caryigenum);柑橘上的柑桔痂囊腔菌(Elsinoe fawcettii)、炭疽菌屬(Colletotrichum spp.)及柑桔球座菌(Guignardia citricarpa);咖啡上的炭疽刺盤孢菌屬病菌(Colletotrichum spp.)及咖啡駝孢銹菌(Hemileia vastatrix)。 Strobilurins are Q o I inhibitory fungicides and inhibit fungal respiration by binding to the cytochrome bc 1 complex at the Q o I site in mitochondrial respiration. These fungicides work by inhibiting the ability of fungi to perform normal respiration. These strobilurin dual chemicals have very specific target sites or mode-of-action (MOA). The strobilurins are known to control fungi such as: Erysiphe graminis on temperate cereals, Puccinia spp., Leptosphaeria nodorum, wheat Septoria tritici and Pyrenophora teres, Pyricularia oryzae and Rhizoctonia solani on rice; Plasmopara viticola on grape vines and Uncinula necator; Sphaerotheca fuliginea and Pseudoperonospora cubensis on Cucurbitaceae; Phytophthora infestans and Alternaria solani on tomato; Mycosphaerella arachidis, Rhizoctonia solani and Sclerotium rolfsii on peanuts; Monilinia spp on peaches .) and Cladosporium carpophilum; Pythium spp. and Rhizoctonia solani on turf; Mycosphaerella spp. on bananas; Cladosporium caryigenum; Elsinoe fawcettii, Colletotrichum spp. and Guignardia citricarpa on citrus; Anthrax stinger on coffee Colletotrichum spp. and Hemileia vastatrix.

鑑於藉由將琥珀酸去氫酶抑制劑與嗜球果傘素殺真菌劑組合可預期到有效控制植物病原性真菌的改善,因此需要探索並發展來自這些族群之活性成分的穩定組成物。 Given that improvements in the effective control of phytopathogenic fungi can be expected by combining succinate dehydrogenase inhibitors with strobilurin fungicides, there is a need to explore and develop stable compositions of active ingredients from these groups.

值得注意的是,當與水或溶劑接觸時,白克列經歷不可抑制的形態變化。進一步觀察到,通常需要特定的技術、繁瑣且昂貴的程序來製作適合商 業生產以及預期應用的白克列配方。此類配方長時間儲存時也會產生穩定性問題。 Notably, becryl undergoes irrepressible morphological changes when in contact with water or solvents. It was further observed that technically specific, tedious and expensive procedures are often required to produce commercially formulations of bacillit as produced commercially and for the intended application. Stability issues can also arise with such formulations when stored for extended periods of time.

因此,需要開發白克列與嗜球果傘素殺真菌劑一起的穩定組成物來消除已知製劑的缺點。 Therefore, there is a need to develop stable compositions of bcclidin together with strobilurin fungicides to eliminate the disadvantages of known formulations.

令人驚訝地,本發明之發明人發現,可以製備包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物,其不經歷任何形態變化、穩定且非常適合於控制植物病原性真菌的預期應用。 Surprisingly, the inventors of the present invention have found that it is possible to prepare compositions comprising eutectic mixtures of bacrine and strobilurin fungicides which do not undergo any morphological changes, are stable and are very suitable for controlling phytopathogens Anticipated applications for sexual fungi.

本發明之目的:Purpose of the present invention:

本發明之目的係提供包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物。 It is an object of the present invention to provide a composition comprising a eutectic mixture of bacrine and strobilurin fungicides.

本發明之另一目的係提供包含白克列及亞托敏之共熔混合物的組成物。 Another object of the present invention is to provide a composition comprising a eutectic mixture of bakleyl and yatormin.

本發明之另一目的係提供包含白克列及氟嘧菌酯之共熔混合物的組成物。 Another object of the present invention is to provide a composition comprising a eutectic mixture of bakleyl and fluoxastrobin.

本發明之又另一目的係提供一種用於製備白克列及嗜球果傘素殺真菌劑之共熔混合物的程序。 Yet another object of the present invention is to provide a procedure for the preparation of eutectic mixtures of bacrine and strobilurin fungicides.

本發明之另一目的係提供一種用於製備殺真菌組成物之程序,該等組成物包含白克列及嗜球果傘素殺真菌劑之共熔混合物。 Another object of the present invention is to provide a procedure for the preparation of fungicidal compositions comprising eutectic mixtures of bacrine and strobilurin fungicides.

一種共熔混合物,其包含白克列及嗜球果傘素殺真菌劑。 A eutectic mixture comprising buclide and strobilurin fungicides.

本發明提供一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物。 The present invention provides an agricultural chemical composition comprising a eutectic mixture of bacrine and strobilurin fungicides.

本發明提供一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物,其中該組成物包含以重量計10至90%之間的白克列及90至10%之間的嗜球果傘素殺真菌劑。 The present invention provides an agrochemical composition comprising a eutectic mixture of buccalidine and a strobilurin fungicide, wherein the composition comprises between 10 and 90% by weight of buccalidine and between 90 and 10 % between strobilurin fungicides.

一種共熔混合物,其包含白克列及亞托敏。 A eutectic mixture comprising bakleyl and yatormin.

本發明進一步提供一種農業化學組成物,其包含白克列及亞托敏之共熔混合物。 The present invention further provides an agricultural chemical composition, which comprises a eutectic mixture of becryl and yatomin.

本發明進一步提供一種農業化學組成物,其包含白克列及亞托敏之共熔混合物,其中該組成物包含以重量計10至90%之間的白克列及90至10%之間的亞托敏。 The present invention further provides an agricultural chemical composition comprising a eutectic mixture of becryl and yatormine, wherein the composition comprises between 10 and 90% by weight of becryl and between 90 and 10% of Tomin.

一種白克列及亞托敏之共熔混合物,其中該共熔混合物的特徵在於DSC具有100±3℃的起始溫度及103.5±3℃的吸熱峰。 A eutectic mixture of becryl and yatormin, wherein the eutectic mixture is characterized by a DSC onset temperature of 100±3°C and an endothermic peak of 103.5±3°C.

本發明進一步提供一種農業化學組成物,其包含白克列及亞托敏之共熔混合物,其中該共熔混合物的特徵在於DSC具有100±3℃的起始溫度及103.5±3℃的吸熱峰。 The present invention further provides an agrochemical composition comprising a eutectic mixture of bectilide and yatormin, wherein the eutectic mixture is characterized by a DSC onset temperature of 100±3°C and an endothermic peak of 103.5±3°C.

一種共熔混合物,其包含白克列及氟嘧菌酯。 A eutectic mixture comprising bakleyl and fluoxastrobin.

本發明進一步提供一種農業化學組成物,其包含白克列及氟嘧菌酯之共熔混合物。 The present invention further provides an agricultural chemical composition, which comprises a eutectic mixture of bakleyl and fluoxastrobin.

本發明進一步提供一種農業化學組成物,其包含白克列及氟嘧菌酯之共熔混合物,其中該組成物包含以重量計10至90%之間的白克列及90至10%之間的氟嘧菌酯。 The present invention further provides an agrochemical composition comprising a eutectic mixture of buccolidine and fluoxastrobin, wherein the composition comprises between 10 and 90% by weight of bucrine and between 90 and 10% fluoxastrobin.

一種白克列及氟嘧菌酯之共熔混合物,其中該共熔混合物的特徵在於DSC具有92±3℃的起始溫度及97±3℃的吸熱峰。 A eutectic mixture of bakleyl and fluoxastrobin, wherein the eutectic mixture is characterized in that DSC has an onset temperature of 92±3°C and an endothermic peak of 97±3°C.

本發明進一步提供一種農業化學組成物,其包含白克列及氟嘧菌酯之共熔混合物,其中該共熔混合物的特徵在於DSC具有92±3℃的起始溫度及97±3℃的吸熱峰。 The present invention further provides an agrochemical composition comprising a eutectic mixture of bakleyl and fluoxastrobin, wherein the eutectic mixture is characterized in that DSC has an onset temperature of 92±3°C and an endotherm of 97±3°C peak.

一種白克列及氟嘧菌酯之共熔混合物,其中該共熔混合物的特徵在於DSC具有100±3℃的起始溫度及107±3℃的吸熱峰。 A eutectic mixture of bakleyl and fluoxastrobin, wherein the eutectic mixture is characterized in that DSC has an onset temperature of 100±3°C and an endothermic peak of 107±3°C.

本發明進一步提供一種農業化學組成物,其包含白克列及氟嘧菌酯之共熔混合物,其中該共熔混合物的特徵在於DSC具有100±3℃的起始溫度及107±3℃的吸熱峰。 The present invention further provides an agrochemical composition comprising a eutectic mixture of bakleyl and fluoxastrobin, wherein the eutectic mixture is characterized in that DSC has an onset temperature of 100±3°C and an endotherm of 107±3°C peak.

本發明係關於一種用於配製農業化學組成物之程序,該農業化學組成物包含白克列及嗜球果傘素殺真菌劑之共熔混合物。 The present invention relates to a process for formulating an agrochemical composition comprising a eutectic mixture of bacrine and strobilurin fungicides.

進一步地,其係關於一種用於製備白克列及嗜球果傘素殺真菌劑之共熔混合物之製程。 Further, it relates to a process for preparing a eutectic mixture of bacrine and strobilurin fungicides.

本發明進一步提供一種控制植物病原性真菌之方法,該方法包含對植物或其棲地、植物種子或土壤施用殺真菌有效量之包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物。 The present invention further provides a method of controlling phytopathogenic fungi, the method comprising applying to plants or their habitat, plant seeds or soil a fungicidally effective amount of a eutectic mixture comprising buccalide and strobilurin fungicides composition.

本發明可藉由參照下列圖式來理解:第1圖:白克列之DSC熱分析圖。 The present invention can be understood by referring to the following figures: Figure 1: DSC thermogram of Bekley.

第2圖:亞托敏之DSC熱分析圖。 Figure 2: DSC thermogram of yatormin.

第3圖:白克列及亞托敏之DSC熱分析圖,其比率%為60:40。 Figure 3: DSC thermograms of Bakleyl and Yatomin, the ratio of which is 60:40.

第4圖:白克列及亞托敏之共熔混合物的相圖。 Figure 4: The phase diagram of the eutectic mixture of bekleyl and yatormin.

第5圖:實例2之DSC熱分析圖。 Figure 5: DSC thermogram of Example 2.

第6圖:實例3之DSC熱分析圖。 Fig. 6: DSC thermogram of Example 3.

第7圖:實例8之DSC熱分析圖。 Fig. 7: DSC thermogram of Example 8.

第8圖:實例2儲存9個月後之DSC熱分析圖。 Figure 8: DSC thermogram of Example 2 after storage for 9 months.

第9圖:氟嘧菌酯之DSC熱分析圖。 Figure 9: DSC thermogram of fluoxastrobin.

第10圖:白克列及氟嘧菌酯混合物比率為30:70(實例9)之DSC熱分析圖。 Fig. 10: The DSC thermogram of the mixture of bakleyl and fluoxastrobin at a ratio of 30:70 (Example 9).

第11圖:白克列及氟嘧菌酯混合物比率為25:75(實例10)之DSC熱分析圖。 Fig. 11: The DSC thermogram of the mixture of bakleyl and fluoxastrobin at a ratio of 25:75 (Example 10).

本發明之發明人驚訝地發現,可成功地製備白克列及嗜球果傘素化合物之共熔混合物,其對於控制植物病原性真菌的預期用途係穩定的且非常適合的。 The inventors of the present invention have surprisingly found that it is possible to successfully prepare eutectic mixtures of bacrine and strobilurin compounds which are stable and very suitable for their intended use in the control of phytopathogenic fungi.

此外,本發明之發明人已觀察到,包含白克列及嗜球果傘素化合物之共熔混合物的組成物在製備此類組成物時,不會遭受不受控制的形態變化,並且進一步注意到該等組成物在長期儲存期間保持穩定。 Furthermore, the inventors of the present invention have observed that compositions comprising eutectic mixtures of bakleyl and strobilurin compounds do not suffer from uncontrolled morphological changes in the preparation of such compositions, and further noted These compositions remain stable during long-term storage.

關於本發明,白克列係指2-氯-N-(4'-氯聯苯-2-基)菸鹼醯胺、其鹽類及衍生物及多形體。在整個說明書中,用語「白克列(boscalid)」包括分子之已知多形體形式,亦即白克列無水物修飾I、白克列無水物修飾II及白克列水合物形式。 With regard to the present invention, Bakret refers to 2-chloro-N-(4'-chlorobiphenyl-2-yl)nicotinamide, its salts and derivatives and polymorphs. Throughout the specification, the term "boscalid" includes the known polymorphic forms of the molecule, ie, the anhydrate I, anhydrate II and hydrate forms of boscalid.

用語「共熔混合物(eutectic mixture)」係定義為二或更多種組分之混合物,其通常不會相互作用形成新的化合物,但是在一定比例下,抑制彼此的結晶程序,造成具有比該等組分之任一者更低的熔點之系統。描繪共熔混合物之起始熔融溫度(使用微差掃描熱量法-DSC熱分析圖)及兩種組分之不同%的過 量組分的相圖,說明根據本發明之組成物的熔化模式。混合物中所有組分處於平衡狀態的點稱為共熔點。 The term "eutectic mixture" is defined as a mixture of two or more components which do not normally interact to form new compounds, but which, in certain proportions, inhibit the crystallization process of each other, resulting in A system with a lower melting point of either of the components. Plot the onset melting temperature of the eutectic mixture (using Differential Scanning Calorimetry - DSC thermogram) and the difference % transition of the two components The phase diagram of the quantitative components, illustrating the melting mode of the composition according to the invention. The point at which all components in a mixture are in equilibrium is called the eutectic point.

用語共熔混合物亦應理解為包括兩種組分的比率之根據本發明之混合物,其中熔點在該比率降低至最小值。然而,其亦應包括熔點高於該共熔混合物之熔點的其他比率,儘管低於各別組分的熔點,其中至少一部分混合的活性成分係處於共熔點。 The term eutectic mixture is also understood to include mixtures according to the invention of the ratio of the two components in which the melting point is reduced to a minimum. However, it shall also include other ratios having a melting point higher than that of the eutectic mixture, although lower than that of the individual components, at which at least a portion of the active ingredients mixed are at the eutectic point.

在一實施例中,本發明提供一種共熔混合物,其包含白克列及嗜球果傘素殺真菌劑。 In one embodiment, the present invention provides a eutectic mixture comprising bacrine and a strobilurin fungicide.

在一實施例中,本發明提供一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物。 In one embodiment, the present invention provides an agrochemical composition comprising a eutectic mixture of bacrine and a strobilurin fungicide.

在本發明之一實施例中,提供一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物;以及至少一種農業化學上可接受的賦形劑,其中該共熔混合物的形成抑制白克列及嗜球果傘素殺真菌劑的結晶程序。 In one embodiment of the present invention, there is provided an agrochemical composition comprising a eutectic mixture of bacrine and strobilurin fungicides; and at least one agrochemically acceptable excipient, wherein the The formation of eutectic mixtures inhibits the crystallization process of the buclide and strobilurin fungicides.

在一實施例中,該組成物包含選自包含下列者之群組的形式之白克列:白克列無水物修飾I、白克列無水物修飾II,及白克列水合物形式。 In one embodiment, the composition comprises Bacrine in a form selected from the group comprising: Bacrine Anhydrate Modified I, Bacclelide Anhydrate Modified II, and Bacrine Hydrate Form.

在一實施例中,根據本發明之組成物包含選自包含下列群組之嗜球果傘素殺真菌劑:亞托敏(azoxystrobin)、百克敏(pyraclostrobin)、三氟敏(trifloxystrobin)、啶氧菌酯(picoxystrobin)、氟嘧菌酯(fluoxastrobin)、甲氧基乙醯胺類菌酯(mandestrobin)、吡菌苯威(pyribencarb)、丁香菌酯(coumoxystrobin)、烯肟菌酯(enoxastrobin)、氟菌蟎酯(flufenoxystrobin)、唑菌酯(pyraoxystrobin)、唑胺菌酯(pyrametostrobin)、氯啶菌酯(triclopyricarb)、醚菌胺(dimoxystrobin)、芬胺司唑賓(fenaminstrobin)、苯氧菌胺(metominostrobin)、肟醚菌胺(orysastrobin),及克收欣(Kresoxim-methyl)。 In one embodiment, the composition according to the invention comprises a strobilurin fungicide selected from the group comprising: azoxystrobin, pyraclostrobin, trifluroxystrobin, pyridine Picoxystrobin, fluoxastrobin, mandestrobin, pyribencarb, coumoxystrobin, enoxastrobin , flufenoxystrobin, pyraoxystrobin, pyramethstrobin, triclopyricarb, dimoxystrobin, fenaminstrobin, phenoxy Metominostrobin, orysastrobin, and Kresoxim-methyl.

在一較佳實施例中,根據本發明之組成物包含選自下列群組的殺真菌劑,其包含:亞托敏、百克敏、三氟敏、氟嘧菌酯及啶氧菌酯。 In a preferred embodiment, the composition according to the present invention comprises a fungicide selected from the following group, which includes: ytropamine, becclomin, trifluramine, fluoxastrobin and picoxystrobin.

在本發明之一實施例中,該組成物包含以重量計10至90%之間的白克列及90至10%之間的嗜球果傘素殺真菌劑。 In one embodiment of the present invention, the composition comprises 10 to 90% by weight of buccalidine and 90 to 10% of strobilurin fungicide.

在本發明之一實施例中,該組成物包含以重量計50至80%的白克列及約50至20%的嗜球果傘素殺真菌劑。 In one embodiment of the present invention, the composition comprises 50 to 80% by weight of buccalidine and about 50 to 20% of strobilurin fungicide.

在本發明之一實施例中,該組成物包含以活性成分之重量計50至80%之間的白克列及50至20%之間的嗜球果傘素殺真菌劑。 In one embodiment of the present invention, the composition comprises, by weight of the active ingredient, between 50 and 80% of the buccalidine and between 50 and 20% of the strobilurin fungicide.

在一實施例中,本發明提供一種白克列及亞托敏之共熔混合物。 In one embodiment, the present invention provides a eutectic mixture of bakleyl and yatormin.

在一實施例中,本發明提供一種包含白克列及亞托敏之共熔混合物,其莫耳比為1.5:1。 In one embodiment, the present invention provides a eutectic mixture comprising bakleyl and yatormine, the molar ratio of which is 1.5:1.

在本發明之一實施例中,提供一種包含白克列及亞托敏之共熔混合物的農業化學組成物。 In one embodiment of the present invention, there is provided an agrochemical composition comprising a eutectic mixture of bakleyl and yatormin.

在本發明之一實施例中,該組成物包含以重量計10至90%之間的白克列及90至10%之間的亞托敏。 In one embodiment of the present invention, the composition comprises 10 to 90% of bacilli and 90 to 10% of atropamine by weight.

在本發明之某些實施例中,該組成物包含以重量計50至80%之間的白克列及50至20%之間的亞托敏。 In some embodiments of the present invention, the composition comprises between 50 and 80% by weight of bacilli and between 50 and 20% of atropamine.

在本發明之某些實施例中,該組成物包含以活性成分之重量計50至80%之間的白克列及50至20%之間的亞托敏。 In some embodiments of the present invention, the composition comprises, by weight of the active ingredient, between 50 and 80% of bacilli and between 50 and 20% of atropamine.

在一實施例中,本發明提供一種共熔混合物,其包含以活性成分之重量計約60%的白克列及約40%的亞托敏。 In one embodiment, the present invention provides a eutectic mixture comprising, by weight of the active ingredient, about 60% of bacilli and about 40% of atropamine.

在一實施例中,該組成物包含以活性成分之重量計約60%的白克列及約40%的亞托敏。 In one embodiment, the composition comprises, by weight of the active ingredient, about 60% bacilli and about 40% atropamine.

在一實施例中,該組成物包含白克列及亞托敏,其莫耳比為1:9至9:1。 In one embodiment, the composition comprises bacclelid and yatormin at a molar ratio of 1:9 to 9:1.

在一實施例中,該組成物包含白克列及亞托敏,其莫耳比為1:5至5:1。 In one embodiment, the composition comprises bacclelid and yatormin at a molar ratio of 1:5 to 5:1.

在一實施例中,該組成物包含白克列及亞托敏,其莫耳比為以1:3至3:1。 In one embodiment, the composition includes bacrine and yatormin in a molar ratio of 1:3 to 3:1.

在一較佳實施例中,該組成物包含白克列及亞托敏,其莫耳比為1.5:1。 In a preferred embodiment, the composition comprises bacrine and yatormin at a molar ratio of 1.5:1.

在一實施例中,本發明提供一種包含白克列及亞托敏之共熔混合物,其莫耳比為1.5:1。 In one embodiment, the present invention provides a eutectic mixture comprising bakleyl and yatormine, the molar ratio of which is 1.5:1.

在一實施例中,包含白克列及亞托敏之共熔混合物之組成物的特徵在於DSC具有100±3℃的起始溫度及103℃±3℃的吸熱峰。 In one embodiment, a composition comprising a eutectic mixture of bakleyl and tropamine is characterized by a DSC onset temperature of 100±3°C and an endothermic peak of 103°C±3°C.

在一實施例中,本發明提供一種包含白克列及亞托敏之共熔混合物,其特徵在於DSC具有100±3℃的起始溫度及103℃±3℃的吸熱峰。 In one embodiment, the present invention provides a eutectic mixture comprising bakleyl and tropamine, characterized in that DSC has an onset temperature of 100±3°C and an endothermic peak of 103°C±3°C.

在一實施例中,包含白克列及亞托敏之共熔混合物之組成物的特徵在於DSC具有100±3℃的起始溫度及103℃與106℃之間的吸熱峰。 In one embodiment, a composition comprising a eutectic mixture of bakleyl and tropamine is characterized by a DSC onset temperature of 100±3°C and an endothermic peak between 103°C and 106°C.

在一實施例中,本發明提供一種包含白克列及亞托敏之共熔混合物,其特徵在於DSC具有100±3℃的起始溫度及103℃與106℃之間的吸熱峰。 In one embodiment, the present invention provides a eutectic mixture comprising bakleyl and tropamine, characterized in that DSC has an onset temperature of 100±3°C and an endothermic peak between 103°C and 106°C.

在一較佳實施例中,包含白克列及亞托敏之共熔混合物之組成物的特徵在於DSC具有100±3℃的起始溫度及103.5℃的吸熱峰。 In a preferred embodiment, the composition comprising the eutectic mixture of bacletide and tropamine is characterized by a DSC onset temperature of 100±3°C and an endothermic peak of 103.5°C.

在一實施例中,本發明提供一種包含白克列及亞托敏之共熔混合物,其特徵在於DSC具有100±3℃的起始溫度及103.5℃的吸熱峰。 In one embodiment, the present invention provides a eutectic mixture comprising bakleyl and tropamine, characterized in that DSC has an onset temperature of 100±3°C and an endothermic peak of 103.5°C.

在一實施例中,本發明提供一種白克列及氟嘧菌酯之共熔混合物。 In one embodiment, the present invention provides a eutectic mixture of bacilli and fluoxastrobin.

在本發明之一實施例中,提供一種包含白克列及氟嘧菌酯之共熔混合物的農業化學組成物。 In one embodiment of the present invention, there is provided an agrochemical composition comprising a eutectic mixture of bakleyl and fluoxastrobin.

在本發明之一實施例中,該組成物包含以重量計10至90%之間的白克列及90至10%之間的氟嘧菌酯。 In one embodiment of the present invention, the composition comprises 10 to 90% by weight of buclide and 90 to 10% of fluoxastrobin.

在本發明之某些實施例中,該組成物包含以重量計50至80%之間的白克列及50至20%之間的氟嘧菌酯。 In some embodiments of the present invention, the composition comprises between 50 and 80% by weight of bacilli and between 50 and 20% of fluoxastrobin.

在本發明之某些實施例中,該組成物包含以活性成分之重量計50至80%之間的白克列及50至20%之間的氟嘧菌酯。 In certain embodiments of the present invention, the composition comprises, by weight of the active ingredient, between 50 and 80% of buccalidine and between 50 and 20% of fluoxastrobin.

在一實施例中,本發明提供一種共熔混合物,其包含以活性成分之重量計約60%的白克列及約40%的氟嘧菌酯。 In one embodiment, the present invention provides a eutectic mixture comprising, by weight of the active ingredient, about 60% bacilli and about 40% fluoxastrobin.

在一實施例中,該組成物包含以活性成分之重量計約60%的白克列及約40%的氟嘧菌酯。 In one embodiment, the composition comprises, by weight of the active ingredient, about 60% bacilli and about 40% fluoxastrobin.

在一實施例中,該組成物包含白克列及氟嘧菌酯,其莫耳比為1:9至9:1。 In one embodiment, the composition comprises bakleyl and fluoxastrobin in a molar ratio of 1:9 to 9:1.

在一實施例中,該組成物包含白克列及氟嘧菌酯,其莫耳比為1:5至5:1。 In one embodiment, the composition comprises bakleyl and fluoxastrobin in a molar ratio of 1:5 to 5:1.

在一實施例中,該組成物包含白克列及氟嘧菌酯,其莫耳比為以1:3至3:1。 In one embodiment, the composition includes bakleyl and fluoxastrobin in a molar ratio of 1:3 to 3:1.

在一實施例中,該組成物包含白克列及氟嘧菌酯,其莫耳比為1.5:1。 In one embodiment, the composition comprises bakleyl and fluoxastrobin at a molar ratio of 1.5:1.

在一實施例中,本發明提供一種包含白克列及氟嘧菌酯之共熔混合物,其莫耳比為1:3。 In one embodiment, the present invention provides a eutectic mixture comprising bakleyl and fluoxastrobin, the molar ratio of which is 1:3.

在一實施例中,包含白克列及氟嘧菌酯之共熔混合物之組成物的特徵在於DSC具有92±3℃的起始溫度及97±3℃的吸熱峰。 In one embodiment, a composition comprising a eutectic mixture of bakleyl and fluoxastrobin is characterized by a DSC onset temperature of 92±3°C and an endothermic peak of 97±3°C.

在一實施例中,本發明提供一種包含白克列及氟嘧菌酯之共熔混合物,其特徵在於DSC具有100±3℃的起始溫度及107℃±3℃的吸熱峰。 In one embodiment, the present invention provides a eutectic mixture comprising bakleyl and fluoxastrobin, characterized in that DSC has an onset temperature of 100±3°C and an endothermic peak of 107°C±3°C.

在一較佳實施例中,包含白克列及氟嘧菌酯之共熔混合物之組成物的特徵在於DSC具有92±3℃的起始溫度及97至100℃的吸熱峰。 In a preferred embodiment, the composition comprising the eutectic mixture of bakleyl and fluoxastrobin is characterized by a DSC onset temperature of 92±3°C and an endothermic peak of 97 to 100°C.

在一較佳實施例中,包含白克列及氟嘧菌酯之共熔混合物之組成物的特徵在於DSC具有100±3℃的起始溫度107至109℃的吸熱峰。 In a preferred embodiment, the composition comprising the eutectic mixture of bakleyl and fluoxastrobin is characterized by DSC having an endothermic peak with an onset temperature of 107 to 109°C at 100±3°C.

在一實施例中,本發明提供一種製備白克列及嗜球果傘素殺真菌劑之共熔混合物的程序。 In one embodiment, the present invention provides a process for preparing a eutectic mixture of bacrine and strobilurin fungicides.

在一實施例中,本發明提供一種製備白克列及嗜球果傘素殺真菌劑之共熔混合物的程序,該程序包含使白克列及嗜球果傘素殺真菌劑經受溶液結晶、乾式研磨、溶劑滴式研磨技術,或噴霧乾燥技術。 In one embodiment, the present invention provides a process for preparing a eutectic mixture of buccalidine and a strobilurin fungicide, the process comprising subjecting the buccalidine and strobilurin fungicide to solution crystallization, Dry milling, solvent drop milling techniques, or spray drying techniques.

在一實施例中,本發明提供一種用於製備白克列及嗜球果傘素之共熔混合物的程序,該程序包含下列步驟:a.在一或多種溶劑中製備白克列及嗜球果傘素殺真菌劑之濃縮溶液;b.可選地將該溶劑蒸發;以及c.用反溶劑研製或沉澱以獲得共熔混合物。 In one embodiment, the present invention provides a process for preparing a eutectic mixture of buccalidine and strobilurin, the process comprising the following steps: a. preparing buccalidine and strobilurin in one or more solvents a concentrated solution of the strobilurin fungicide; b. optionally evaporating the solvent; and c. trituration or precipitation with an anti-solvent to obtain a eutectic mixture.

在一實施例中,本發明提供一種用於製備白克列及嗜球果傘素之共熔混合物的程序,該程序包含下列步驟:a.在一或多種溶劑中製備白克列及嗜球果傘素殺真菌劑之濃縮溶液;b.將該溶劑蒸發來引起結晶以獲得共熔混合物。 In one embodiment, the present invention provides a process for preparing a eutectic mixture of buccalidine and strobilurin, the process comprising the following steps: a. preparing buccalidine and strobilurin in one or more solvents A concentrated solution of the strobilurin fungicide; b. evaporation of the solvent to induce crystallization to obtain a eutectic mixture.

在一實施例中,步驟a)之溶劑係選自脂族醇、酮、酯、醚、極性質子性溶劑、極性非質子性溶劑、鹵化溶劑、脂族烴、或芳族烴。 In one embodiment, the solvent of step a) is selected from aliphatic alcohols, ketones, esters, ethers, polar protic solvents, polar aprotic solvents, halogenated solvents, aliphatic hydrocarbons, or aromatic hydrocarbons.

在本發明之一實施例中,該反溶劑可為係脂族烴或芳族烴。 In one embodiment of the present invention, the anti-solvent can be aliphatic hydrocarbon or aromatic hydrocarbon.

在步驟(b)之一實施例中,該溶劑係經部分蒸發。 In one embodiment of step (b), the solvent is partially evaporated.

在步驟(b)之一實施例中,該溶劑係經完全蒸發。 In one embodiment of step (b), the solvent is completely evaporated.

在本發明之一實施例中,步驟c)中之反溶劑係選自脂族或芳族烴溶劑。 In one embodiment of the present invention, the anti-solvent in step c) is selected from aliphatic or aromatic hydrocarbon solvents.

在一實施例中,本發明提供一種製備白克列及嗜球果傘素殺真菌劑之共熔混合物的程序,該程序包含下列步驟:a.將白克列與嗜球果傘素殺真菌劑摻和;b.可選地將溶劑摻和至該摻合物中;以及c.研磨(grind)或壓碎(crush)或碾磨(mill)該摻和物以獲得該共熔混合物。 In one embodiment, the present invention provides a process for preparing a eutectic mixture of buccalidine and strobilurin fungicides, the process comprising the following steps: a. b. optionally blending a solvent into the blend; and c. grinding or crushing or milling the blend to obtain the eutectic mixture.

在一實施例中,進行該程序之步驟(a)、步驟(b)或步驟(c)的溫度係沒有限制的。 In one embodiment, the temperature at which step (a), step (b) or step (c) of the process is carried out is not limited.

在另一實施例中,該程序之步驟(a)、步驟(b)或步驟(c)係在低於白克列及嗜球果傘素殺真菌劑之熔點的溫度下進行。 In another embodiment, step (a), step (b) or step (c) of the procedure is carried out at a temperature below the melting point of the buccalide and strobilurin fungicides.

本發明進一步提供一種用於製備組成物之程序,該組成物包含白克列及嗜球果傘素殺真菌劑之共熔混合物。 The present invention further provides a procedure for the preparation of a composition comprising a eutectic mixture of bacilli and strobilurin fungicides.

在一實施例中,提供一種用於製備包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物之程序,該程序包含在添加或不添加農業化學上可接受的賦形劑的情況下製備白克列及嗜球果傘素殺真菌劑之共熔混合物,並且將該混合物進一步加工成適合的形式。 In one embodiment, there is provided a process for preparing a composition comprising a eutectic mixture of bacrine and strobilurin fungicides, the process comprising adding or not adding an agrochemically acceptable excipient A eutectic mixture of the buccalidine and strobilurin fungicides is prepared in the case of a fungicide, and the mixture is further processed into a suitable form.

在一實施例中,提供一種用於製備粒狀組成物之程序,該粒狀組成物包含白克列及嗜球果傘素殺真菌劑之共熔混合物。 In one embodiment, a process is provided for preparing a granular composition comprising a eutectic mixture of bacrine and a strobilurin fungicide.

在本發明之一實施例中,藉由包含下列步驟之程序來製備包含白克列及嗜球果傘素殺真菌劑之共熔混合物的粒狀組成物:(a)製備白克列及嗜球果傘素殺真菌劑之共熔混合物,其可選地具有農業化學上可接受的賦形劑; (b)可選地添加一或多種其他農業化學品;(c)可選地研磨及粉碎;及(d)將該混合物造粒以獲得粒狀組成物。 In one embodiment of the present invention, a granular composition comprising a eutectic mixture of bacrine and strobilurin fungicides is prepared by a procedure comprising the following steps: (a) preparing bacrine and strobilurin fungicides A eutectic mixture of strobilurin fungicides, optionally with agrochemically acceptable excipients; (b) optionally adding one or more other agrochemicals; (c) optionally grinding and pulverizing; and (d) granulating the mixture to obtain a granular composition.

在本發明之一實施例中,藉由包含下列步驟之程序來製備包含白克列及嗜球果傘素殺真菌劑之共熔混合物的粒狀組成物:(a)製備白克列及嗜球果傘素殺真菌劑之共熔混合物,其具有至少一種農業化學上可接受的賦形劑;(b)可選地添加一或多種其他農業化學品;(c)研磨及粉碎;及(d)將該混合物造粒以獲得粒狀組成物。 In one embodiment of the present invention, a granular composition comprising a eutectic mixture of bacrine and strobilurin fungicides is prepared by a procedure comprising the following steps: (a) preparing bacrine and strobilurin fungicides A eutectic mixture of a strobilurin fungicide having at least one agrochemically acceptable excipient; (b) optionally with the addition of one or more other agrochemicals; (c) ground and comminuted; and ( d) Granulating the mixture to obtain a granular composition.

將該混合物造粒的步驟並沒有特別限制。適當的造粒程序係在造粒技術中描述的習知程序,例如噴霧乾燥、流化床造粒、黏聚、盤式造粒、及特別是擠壓造粒。 The step of granulating the mixture is not particularly limited. Suitable granulation procedures are the customary procedures described in granulation technology, such as spray drying, fluid bed granulation, agglomeration, pan granulation, and especially extrusion granulation.

在本發明之一實施例中,藉由包含下列步驟之程序來製備包含白克列及嗜球果傘素殺真菌劑之共熔混合物的粒狀組成物:(a)將白克列及嗜球果傘素殺真菌劑與至少一種促進化學上可接受的賦形劑混合;(b)研磨及粉碎;及(c)將該混合物造粒以獲得粒狀組成物。 In one embodiment of the present invention, a granular composition comprising a eutectic mixture of bacrine and strobilurin fungicides is prepared by a procedure comprising: (a) mixing bacrine and strobilurin fungicides mixing the strobilurin fungicide with at least one facilitating chemically acceptable excipient; (b) grinding and pulverizing; and (c) granulating the mixture to obtain a granular composition.

在一實施例中,步驟(a)之混合包括研磨。 In one embodiment, the mixing of step (a) includes grinding.

在本發明之一實施例中,該共熔混合物係藉由將白克列與嗜球果傘素殺真菌劑一起研磨來製備。 In one embodiment of the present invention, the eutectic mixture is prepared by grinding bakleyl with a strobilurin fungicide.

在一實施例中,該共熔混合物係藉由將白克列與嗜球果傘素殺真菌劑一起碾磨來製備。 In one embodiment, the eutectic mixture is prepared by co-milling bacrine with a strobilurin fungicide.

在一實施例中,該共熔混合物係藉由將白克列與嗜球果傘素殺真菌劑一起熔化來製備。 In one embodiment, the eutectic mixture is prepared by melting the bacilli and strobilurin fungicides together.

在一實施例中,該共熔混合物係藉由將白克列及嗜球果傘素殺真菌劑從一或多種合適的溶劑中結晶來製備。 In one embodiment, the eutectic mixture is prepared by crystallizing the buccalidine and strobilurin fungicides from one or more suitable solvents.

在一實施例中,用於製備白克列及嗜球果傘素殺真菌劑之共熔混合物的合適溶劑係選自醇、酯、醚、酮、醛、鹵化烴、芳族烴、脂族烴、醯胺、及水或其混合物。 In one embodiment, suitable solvents for the preparation of eutectic mixtures of bucaria and strobilurin fungicides are selected from alcohols, esters, ethers, ketones, aldehydes, halogenated hydrocarbons, aromatic hydrocarbons, aliphatic Hydrocarbons, amides, and water or mixtures thereof.

在一實施例中,該共熔混合物係藉由將白克列及嗜球果傘素殺真菌劑之混合物造粒來製備。 In one embodiment, the eutectic mixture is prepared by granulating a mixture of bacilli and strobilurin fungicides.

在一實施例中,造粒程序並沒有特別限制,並且可藉由噴霧乾燥、流化床造粒、黏聚、盤式造粒及擠壓造粒來進行。 In one embodiment, the granulation procedure is not particularly limited, and can be performed by spray drying, fluidized bed granulation, agglomeration, pan granulation, and extrusion granulation.

在一實施例中,該共熔混合物係藉由將白克列及嗜球果傘素殺真菌劑之混合物造粒來製備,其中該嗜球果傘素殺真菌劑係選自:亞托敏、百克敏、三氟敏、三氟嘧菌酯、啶氧菌酯、氟嘧菌酯、甲氧基乙醯胺類菌酯、吡菌苯威、丁香菌酯、烯肟菌酯、氟菌蟎酯、唑菌酯、唑胺菌酯、氯啶菌酯、醚菌胺、芬胺司唑賓、苯氧菌胺、肟醚菌胺或克收欣。 In one embodiment, the eutectic mixture is prepared by granulating a mixture of bacilli and a strobilurin fungicide, wherein the strobilurin fungicide is selected from the group consisting of: strobilurin , bacmin, trifluramine, trifluoxystrobin, picoxystrobin, fluoxastrobin, methoxyacetamidostrobin, pyribencarb, syringstrobin, cylostrobin, fluoxin Micarid, pyraclostrobin, pyraclostrobin, cloxastrobin, kysastrobin, fentil-stazobine, fenoxystrobin, orysastrobin, or cloxastrobin.

在一實施例中,該共熔混合物係藉由將白克列及亞托敏之混合物造粒來製備。 In one embodiment, the eutectic mixture is prepared by granulating a mixture of becryl and yatormin.

根據本發明之殺真菌組成物可進一步包含其他農業化學合適的賦形劑,諸如輔助佐劑/界面活性劑,諸如潤濕劑擴散劑、助滲透劑、分散劑、載劑、黏著劑(sticking agent)及黏合劑、惰性成分、pH改質劑、懸浮劑、噴霧液滴改質劑、顏料、抗氧化劑、UV保護劑、相容劑(compatibilizing agent)、消泡劑、螯合劑(sequestering agent)、中和劑、腐蝕抑制劑、染料、氣味劑、肥料、微量營養劑、軟化劑(emollient)、潤滑劑,及類似者。 The fungicidal composition according to the present invention may further comprise other agrochemically suitable excipients, such as auxiliary adjuvants/surfactants, such as wetting agent diffusing agents, penetration aids, dispersants, carriers, sticking agents (sticking agent) and binders, inert ingredients, pH modifiers, suspending agents, spray droplet modifiers, pigments, antioxidants, UV protectants, compatibilizing agents, defoamers, sequestering agents ), neutralizers, corrosion inhibitors, dyes, odorants, fertilizers, micronutrients, emollients, lubricants, and the like.

包含白克列及嗜球果傘素殺真菌劑之共熔混合物的農業化學組成物可製備為分散性粒劑、可濕性粉劑、乾懸浮劑(dry flowable)、乳劑、分散劑、懸浮濃縮物、聚合性材料之封裝、油分散劑、可乳化濃縮物、微乳劑、可流動濃縮物,或懸浮乳劑(suspo-emulsion)。 Agrochemical compositions comprising eutectic mixtures of buclide and strobilurin fungicides can be prepared as dispersible granules, wettable powders, dry flowables, emulsions, dispersions, suspension concentrates Encapsulation of polymeric materials, oil dispersions, emulsifiable concentrates, microemulsions, flowable concentrates, or suspo-emulsions.

根據本發明之組成物可進一步包含一或多種其他活性成分。其他活性成分可選自殺真菌劑、殺蟲劑或除草劑。 The composition according to the present invention may further comprise one or more other active ingredients. Other active ingredients may be fungicides, insecticides or herbicides.

在一實施例中,該額外的活性成分係殺真菌劑。在此實施例中,本發明之組成物包含第三殺真菌劑。 In one embodiment, the additional active ingredient is a fungicide. In this embodiment, the composition of the present invention includes a third fungicide.

在一實施例中,該額外的殺真菌劑可係二或更多種額外殺真菌劑之組合。在此實施例中,本發明之組成物包含第三及第四殺真菌劑。 In one embodiment, the additional fungicide may be a combination of two or more additional fungicides. In this embodiment, the composition of the present invention includes a third and a fourth fungicide.

在一實施例中,本發明之組成物包含第三及第四殺真菌劑,其係選自多點(multisite)接觸殺真菌劑、唑(conazole)殺真菌劑及琥珀酸去氫酶抑制劑。 In one embodiment, the composition of the present invention comprises a third and a fourth fungicide selected from the group consisting of multisite contact fungicides, conazole fungicides and succinate dehydrogenase inhibitors .

在一實施例中,該第三殺真菌劑可係多點接觸殺真菌劑。 In one embodiment, the third fungicide may be a multi-point contact fungicide.

在一實施例中,該多點接觸殺真菌劑可係選自由下列所組成之群組:(i)銅殺真菌劑,其係選自氧氯化銅(copper oxychloride)、硫酸銅、氫氧化銅及三元硫酸銅(tribasic copper sulfate)(波爾多(Bordeaux)混合物);(ii)元素硫;(iii)二硫胺甲酸酯類殺真菌劑,選自代森銨(amobam)、福美砷(asomate)、氧化福美雙(azithiram)、嗎菌威(carbamorph)、銅合浦單劑(cufraneb)、福美銅氯(cuprobam)、二硫龍(disulfiram)、富爾邦(ferbam)、斯美地(metam)、代森鈉(nabam)、福美雙聯(tecoram)、得恩地(thiram)、福美甲胂(urbacide)、福美鋅(ziram)、邁隆(dazomet)、益地安(etem)、代森環(milneb)、代森錳銅(mancopper)、鋅錳乃浦(mancozeb)、錳乃浦 (maneb)、免得爛(metiram)、聚胺基甲酸酯(polycarbamate)、甲基鋅乃浦(propineb)及鋅乃浦(zineb);(iv)苯二醯亞胺類殺真菌劑,選自氟爾培(folpet)、蓋普丹(captan)及四氯丹(captafol);(v)四氯異苯(chlorothalonil);(vi)硫醯胺類殺真菌劑,選自益發靈dichlofluanid)及甲苯基氟寧得(tolylfluanid);(vii)胍類殺真菌劑,選自多寧(dodine)、雙胍辛(guazantine)及克熱淨(iminoctaadine);(viii)敵菌靈(anilazine);(ix)腈硫醌(dithianon);及(x)其組合。 In one embodiment, the multi-point contact fungicide may be selected from the group consisting of: (i) copper fungicide selected from copper oxychloride, copper sulfate, hydroxide Copper and tribasic copper sulfate (Bordeaux mixture); (ii) elemental sulfur; (iii) dithicarbamic ester fungicides selected from amobam, thiram ( asomate), azithiram oxide, carbamorph, cufraneb, cuprobam, disulfiram, ferbam, smeide ( Metam), nabam, tecoram, thiram, urbacide, ziram, dazomet, etem, generation Sen ring (milneb), mancopper (mancopper), zinc manganese Naipu (mancozeb), manganese Naipu (maneb), metiram, polycarbamate, methyl zinc Naipu (propineb) and zinc Naipu (zineb); (iv) Phthalimide fungicides, selected from folpet, captan and captafol; (v) chlorothalonil; (vi) sulfamide fungicides from dichlorofluanid) and tolylfluanid; (vii) guanidine fungicides selected from dodine, guazantine and iminoctaadine; (viii) anilazine; (ix) dithianon; and (x) combinations thereof.

在一實施例中,該第三殺真菌劑係鋅錳乃浦(mancozeb)。 In one embodiment, the third fungicide is mancozeb.

在一實施例中,該第三殺真菌劑鋅錳乃浦對田地提供的使用量係0.5kg/ha至5.0kg/ha。 In one embodiment, the dosage of the third fungicide zinc manganese Naipu on the field is 0.5kg/ha to 5.0kg/ha.

在一實施例中,該第三殺真菌劑鋅錳乃浦對田地提供的使用量係1.0kg/ha至3.0kg/ha。 In one embodiment, the dosage of the third fungicide zinc manganese Naipu on the field is 1.0kg/ha to 3.0kg/ha.

在一實施例中,該多點殺真菌劑係四氯異苯。 In one embodiment, the multi-site fungicide is tetrachloroisobenzene.

在一實施例中,該第三殺真菌劑可係選自由下列所組成之群組的唑菌殺真菌劑:甘寶素、克黴唑、依滅列、

Figure 108124806-A0305-02-0017-12
咪唑、撲克拉、撲克拉-錳、賽福座、阿扎康唑、比多農、溴克座、環克座、苄氯三唑醇、待克利、戴尼唑、達克利、依普座、乙環唑、芬克座、三氟苯唑、氟喹唑、護矽得、護汰芬、呋菌唑、呋醚唑、菲克利、易胺座、種菌唑、滅特座、邁克尼、平克座、普克利、丙硫菌 唑、奎因克座、矽氟唑、得克利、四克利、三泰芬、三泰隆、滅菌唑、單克素、稻瘋酯及單克素-P。 In one embodiment, the third fungicide may be an azole fungicide selected from the group consisting of: campanola, clotrimazole, examidate,
Figure 108124806-A0305-02-0017-12
Imidazole, Pokra, Pokra-Manganese, Saifuzuo, Azaconazole, Bidronon, Bromogram, Cyclogram, Benzylclotriazole, Taikeli, Danizole, Dacley, Ipzu , Etoconazole, Funkza, Triflubenazole, Fluquinazole, Husilide, Hutifen, Fuconazole, Fufeconazole, Fickley, Yiminzuo, Buconazole, Metezuo, McNee , Pink, Pukley, Prothioconazole, Quinque, Silfluazole, Decley, Four Keli, San Taifen, San Tyrone, Fenconazole, Monograms, Padrazil and Monograms- p.

在一實施例中,該第三殺真菌劑可係選自由下列所組成之群組的第二琥珀酸去氫酶抑制劑:麥鏽靈(benodanil)、福多寧(flutolanil)、滅普寧(mepronil)、氟吡菌醯胺(fluopyram)、甲呋醯胺(fenfuram)、萎鏽靈(carboxin)、喜保信(oxycarboxin)、賽氟滅(thifluzamide)、聯苯吡菌胺(bixafen)、氟唑菌醯胺(fluxapyroxad)、福拉比(furametpyr)、吡唑萘菌胺(isopyrazam)、氟唑菌苯胺(penflufen)、吡噻菌胺(penthiopyrad)及環苯吡菌胺(sedaxane)。 In one embodiment, the third fungicide may be a second succinate dehydrogenase inhibitor selected from the group consisting of: benodanil, flutolanil, mepronin ( mepronil), fluopyram, fenfuram, carboxin, oxycarboxin, thifluzamide, bixafen, fluoride Fluxapyroxad, furametpyr, isopyrazam, penflufen, penthiopyrad, and sedaxane.

在一實施例中,該第三殺真菌劑係多點接觸殺真菌劑,且該第四殺真菌劑可係選自由下列所組成之群組的唑殺真菌劑:甘寶素(climbazole)、克黴唑(clotrimazole)、依滅列(imazalil)、

Figure 108124806-A0305-02-0018-13
咪唑(oxpoconazole)、撲克拉(prochloraz)、撲克拉-錳(prochloraz-manganese)、賽福座(triflumizole)、阿扎康唑(azaconazole)、比多農(bitertanol)、溴克座(bromuconazole)、環克座(cyproconazo1e)、苄氯三唑醇(diclobutrazol)、待克利(difenoconazole)、戴尼唑(diniconazole)、達克利(diniconazole-M)、依普座(epoxiconazole)、乙環唑(etaconazole)、芬克座(fenbuconazole)、三氟苯唑(fluotrimazole)、氟喹唑(fluquinconazole)、護矽得(flusilazole)、護汰芬(flutriafol)、呋菌唑(furconazole)、呋醚唑(furconazole-cis)、菲克利(hexaconazole)、易胺座(imibenconazole)、種菌唑(ipconazole)、滅特座(metconazole)、邁克尼(myclobutanil)、平克座(pencoconazole)、普克利(propiconazole)、丙硫菌唑(prothioconazole)、奎因克座(quinconazole)、矽氟唑(simeconazole)、得克利(tebuconazole)、四克利(tetraconazole)、三泰芬(triadimefon)、三泰隆(triadimenol)、滅菌唑(triticonazole)、單克素(uniconazole)、稻瘋酯(perfurazoate)及單克素-P(uniconazole-P)。 In one embodiment, the third fungicide is a multi-point contact fungicide, and the fourth fungicide may be an azole fungicide selected from the group consisting of climbazole, clarithromycin Clotrimazole, imazalil,
Figure 108124806-A0305-02-0018-13
Imidazole (oxpoconazole), pokla (prochloraz), pokla-manganese (prochloraz-manganese), triflumizole, azaconazole, bitertanol, bromuconazole, Cyproconazole, diclobutrazol, difenoconazole, diniconazole, diniconazole-M, epoxiconazole, etaconazole , fenbuconazole, fluotrimazole, fluquinconazole, flusilazole, flutriafol, furconazole, furconazole- cis), hexaconazole, imibenconazole, ipconazole, metconazole, myclobutanil, pencoconazole, propiconazole, propylthio Prothioconazole, quinconazole, simeconazole, tebuconazole, tetraconazole, triadimefon, triadimenol, triticonazole ), uniconazole, perfurazoate and uniconazole-P.

在一實施例中,該第三殺真菌劑可係選自由下列所組成之群組的唑菌殺真菌劑:甘寶素、克黴唑、依滅列、

Figure 108124806-A0305-02-0019-14
咪唑、撲克拉、撲克拉-錳、賽福座、阿扎康唑、比多農、溴克座、環克座、苄氯三唑醇、待克利、戴尼唑、達克利、依普座、乙環唑、芬克座、三氟苯唑、氟喹唑、護矽得、護汰芬、呋菌唑、呋醚唑、菲克利、易胺座、種菌唑、滅特座、邁克尼、平克座、普克利、丙硫菌唑、奎因克座、矽氟唑、得克利、四克利、三泰芬、三泰隆、滅菌唑、單克素、稻瘋酯及單克素-P。 In one embodiment, the third fungicide may be an azole fungicide selected from the group consisting of: campanola, clotrimazole, examidate,
Figure 108124806-A0305-02-0019-14
Imidazole, Pokra, Pokra-Manganese, Saifuzuo, Azaconazole, Bidronon, Bromogram, Cyclogram, Benzylclotriazole, Taikeli, Danizole, Dacley, Ipzu , Etoconazole, Funkza, Triflubenazole, Fluquinazole, Husilide, Hutifen, Fuconazole, Fufeconazole, Fickley, Yiminzuo, Buconazole, Metezuo, McNee , Pink, Pukley, Prothioconazole, Quinque, Silfluazole, Decley, Four Keli, San Taifen, San Tyrone, Fenconazole, Monograms, Padrazil and Monograms- p.

在一實施例中,該第三殺真菌劑可係多點接觸殺真菌劑,且該第四殺真菌劑可係選自由下列所組成之群組的第二琥珀酸去氫酶抑制劑:麥鏽靈、福多寧、滅普寧、氟吡菌醯胺、甲呋醯胺、萎鏽靈、喜保信、賽氟滅、聯苯吡菌胺、氟唑菌醯胺、福拉比、吡唑萘菌胺、氟唑菌苯胺、吡噻菌胺,及環苯吡菌胺。 In one embodiment, the third fungicide can be a multi-point contact fungicide, and the fourth fungicide can be a second succinate dehydrogenase inhibitor selected from the group consisting of: Rupifen, fuduonin, methpronin, fluopyram, forfamide, wilting, xibaoxin, seflumet, bixafen, flufenpyramide, furabi, pyrazole Naprofen, penflufen, penthiopyrad, and cycloflufen.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦(mancozeb),且該第四殺真菌劑可係選自由下列所組成之群組的第二琥珀酸去氫酶抑制劑:麥鏽靈、福多寧、滅普寧、氟吡菌醯胺、甲呋醯胺、萎鏽靈、喜保信、賽氟滅、聯苯吡菌胺、氟唑菌醯胺、福拉比、吡唑萘菌胺、氟唑菌苯胺、吡噻菌胺,及環苯吡菌胺。 In one embodiment, the third fungicide may be mancozeb and the fourth fungicide may be a second succinate dehydrogenase inhibitor selected from the group consisting of: Maiguanin, fuduonin, methpronin, fluopyram, forfamide, wilting, xibaoxin, seflumet, bixafen, flufenpyramide, furabi, pyrimidine pyraclostrobin, flufenadin, penthiopyrad, and cycloflufen.

在一實施例中,第三殺真菌劑可係鋅錳乃浦,且第四殺真菌劑可係氟吡菌醯胺。 In one embodiment, the third fungicide may be zinc manganese, and the fourth fungicide may be fluopyram.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係賽氟滅。 In one embodiment, the third fungicide can be zinc manganese Naipur, and the fourth fungicide can be salfluramide.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係聯苯吡菌胺。 In one embodiment, the third fungicide can be Zinc manganese Naipur, and the fourth fungicide can be bixafen.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係氟唑菌醯胺。 In one embodiment, the third fungicide may be zinc manganese Naipur, and the fourth fungicide may be flucloxam.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係吡唑萘菌。 In one embodiment, the third fungicide can be Naipur, and the fourth fungicide can be Pyrazonium.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係吡噻菌胺。 In one embodiment, the third fungicide can be Zinc manganese Naipur, and the fourth fungicide can be penthiopyrad.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係環苯吡菌胺。 In one embodiment, the third fungicide may be Zinc manganese Naipur, and the fourth fungicide may be Cyclofen.

在一實施例中,該第三殺真菌劑係多點接觸殺真菌劑,且該第四殺真菌劑係選自下列之唑殺真菌劑:丙硫菌唑、得克利、環克座、依普座、滅特座及得克利。 In one embodiment, the third fungicide is a multi-point contact fungicide, and the fourth fungicide is an azole fungicide selected from the group consisting of prothioconazole, declel, cyclomethicone, and The general seat, the special seat and the Dekley.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係丙硫菌唑。 In one embodiment, the third fungicide can be zinc manganese, and the fourth fungicide can be prothioconazole.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係得克利。 In one embodiment, the third fungicide can be ZnMn Naipur, and the fourth fungicide can be Declair.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係環克座。 In one embodiment, the third fungicide can be zinc manganese Naipur, and the fourth fungicide can be cyclomethicone.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係依普座。 In one embodiment, the third fungicide can be ZnMn Naipur, and the fourth fungicide can be Ipza.

在一實施例中,該第三殺真菌劑可係鋅錳乃浦,且該第四殺真菌劑可係滅特座。 In one embodiment, the third fungicide can be ZnMn Naipur, and the fourth fungicide can be ZnMn.

根據本發明之組成物可製備為預混物(pre-mix),或藉由與其他活性物進行槽混合,或替代地可作為套組部分出售,該套組部分含有白克列及嗜球果傘素殺真菌劑之共熔混合物以及其他成分,可在噴霧之前混合,或在一個部分中係含有白克列及嗜球果傘素殺真菌劑之共熔混合物的預先混合套組,而在另一部分中係其他活性物或合適的農業化學賦形劑。 Compositions according to the present invention may be prepared as pre-mixes, or by tank mixing with other actives, or alternatively may be sold as part of a kit containing bacrine and globulina Eutectic mixtures of strobilurin fungicides, together with other ingredients, may be mixed prior to spraying or in one part as pre-mixed kits containing eutectic mixtures of strobilurin and strobilurin fungicides, and In another part are other active substances or suitable agrochemical excipients.

包含白克列及嗜球果傘素殺真菌劑之共熔混合物之本發明組成物適合用於對抗或控制真菌。 Compositions of the present invention comprising eutectic mixtures of buccalide and strobilurin fungicides are suitable for combating or controlling fungi.

本發明提供一種控制植物病原性真菌之方法,該方法包含對植物或其棲地、植物種子或土壤施用殺真菌有效量之包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物。 The present invention provides a method of controlling phytopathogenic fungi, the method comprising applying to plants or their habitat, plant seeds or soil a fungicidally effective amount of a eutectic mixture of buccalide and strobilurin fungicides. Composition.

因此,提供一種對抗或控制真菌之方法,該方法包含對植物或其棲地、植物種子或土壤施用殺真菌有效量之包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物。 Accordingly, there is provided a method of combating or controlling fungi, the method comprising applying to a plant or its habitat, plant seeds or soil a fungicidally effective amount of a composition comprising a eutectic mixture of buccalide and strobilurin fungicides things.

在一實施例中,提供一種對抗或控制真菌之方法,該方法包含對植物或其棲地、植物種子或土壤施用殺真菌有效量之包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物,其中該嗜球果傘素殺真菌劑係選自亞托敏、百克敏、三氟敏、三氟嘧菌酯、啶氧菌酯、氟嘧菌酯、甲氧基乙醯胺類菌酯、吡菌苯威、丁香菌酯、烯肟菌酯、氟菌蟎酯、唑菌酯、唑胺菌酯、氯啶菌酯、醚菌胺、芬胺司唑賓、苯氧菌胺、肟醚菌胺或克收欣。 In one embodiment, there is provided a method of combating or controlling fungi, the method comprising applying to a plant or its habitat, plant seeds or soil a fungicidally effective amount of a fungicide comprising buclide and strobilurin. Compositions of molten mixtures, wherein the strobilurin fungicide is selected from the group consisting of ytropamine, bectilamine, trifluramine, azflustrobin, picoxystrobin, fluoxastrobin, methoxyethyl Aminostrobin, pyribencarb, syringstrobin, erythoxystrobin, fludiostrobin, pyraclostrobin, pyraclostrobin, cloxastrobin, krasstrobin, fenamistazobine, benzene Oxystrobin, orysastrobin, or cloxin.

在一實施例中,提供一種對抗或控制真菌之方法,該方法包含對植物或其棲地、植物種子或土壤施用殺真菌有效量之包含白克列及亞托敏之共熔混合物的組成物。 In one embodiment, there is provided a method of combating or controlling fungi, the method comprising applying to a plant or its habitat, plant seeds or soil a fungicidally effective amount of a composition comprising a eutectic mixture of bakleyl and yatormine.

在一實施例中,提供一種對抗或控制真菌之方法,該方法包含對植物或其棲地、植物種子或土壤施用殺真菌有效量之包含白克列及氟嘧菌酯之共熔混合物的組成物。 In one embodiment, there is provided a method of combating or controlling fungi, the method comprising applying to a plant or its habitat, a plant seed or soil a fungicidally effective amount of a composition comprising a eutectic mixture of bakleyl and fluoxastrobin things.

以下係本發明之較佳實施例,其係例示性且非限制性的:一種共熔混合物,其包含白克列及嗜球果傘素殺真菌劑。 The following is a preferred embodiment of the present invention, which is illustrative and non-limiting: A eutectic mixture comprising bacilli and strobilurin fungicides.

一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物。 An agricultural chemical composition comprising a eutectic mixture of bacrine and strobilurin fungicides.

一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物,其中該組成物包含以重量計10至90%之間的白克列及90至10%之間的嗜球果傘素殺真菌劑。 An agrochemical composition comprising a eutectic mixture of buccalidine and a strobilurin fungicide, wherein the composition comprises between 10 and 90% by weight of buccalidine and between 90 and 10% strobilurin fungicides.

一種共熔混合物,其包含白克列及亞托敏。 A eutectic mixture comprising bakleyl and yatormin.

一種農業化學組成物,其包含白克列及亞托敏之共熔混合物。 An agricultural chemical composition, which comprises a eutectic mixture of becryl and yatomin.

一種農業化學組成物,其包含白克列及亞托敏之共熔混合物,其中該組成物包含以重量計10至90%之間的白克列及90至10%之間的亞托敏。 An agrochemical composition comprising a eutectic mixture of becrylide and yatormin, wherein the composition comprises 10 to 90% of becryl and 90 to 10% of yatormin by weight.

一種白克列及亞托敏之共熔混合物,其中該共熔混合物的特徵在於DSC具有100±3℃的起始溫度及103.5±3℃的吸熱峰。 A eutectic mixture of becryl and yatormin, wherein the eutectic mixture is characterized by a DSC onset temperature of 100±3°C and an endothermic peak of 103.5±3°C.

一種包含白克列及亞托敏之共熔混合物之組成物,其中該共熔混合物的特徵在於DSC具有100±3℃的起始溫度及103.5±3℃的吸熱峰。 A composition comprising a eutectic mixture of bacletide and yatormin, wherein the eutectic mixture is characterized by a DSC onset temperature of 100±3°C and an endothermic peak of 103.5±3°C.

一種共熔混合物,其包含白克列及氟嘧菌酯。 A eutectic mixture comprising bakleyl and fluoxastrobin.

一種農業化學組成物,其包含白克列及氟嘧菌酯之共熔混合物。 An agricultural chemical composition, which comprises a eutectic mixture of bakleyl and fluoxastrobin.

一種農業化學組成物,其包含白克列及氟嘧菌酯之共熔混合物,其中該組成物包含以重量計10至90%之間的白克列及90至10%之間的氟嘧菌酯。 An agricultural chemical composition comprising a eutectic mixture of bucaria and fluoxastrobin, wherein the composition comprises between 10 and 90% by weight of bucaria and between 90 and 10% of fluoxastrobin ester.

一種白克列及氟嘧菌酯之共熔混合物,其中該共熔混合物的特徵在於DSC具有92±3℃的起始溫度及97±3℃的吸熱峰。 A eutectic mixture of bakleyl and fluoxastrobin, wherein the eutectic mixture is characterized in that DSC has an onset temperature of 92±3°C and an endothermic peak of 97±3°C.

一種包含白克列及氟嘧菌酯之共熔混合物之組成物,其中該共熔混合物的特徵在於DSC具有92±3℃的起始溫度及具有97±3℃的吸熱峰。 A composition comprising a eutectic mixture of bakleyl and fluoxastrobin, wherein the eutectic mixture is characterized by a DSC onset temperature of 92±3°C and an endothermic peak of 97±3°C.

一種白克列及氟嘧菌酯之共熔混合物,其中該共熔混合物的特徵在於DSC具有100±3℃的起始溫度及具有107±3℃的吸熱峰。 A eutectic mixture of bakleyl and fluoxastrobin, wherein the eutectic mixture is characterized by a DSC onset temperature of 100±3°C and an endothermic peak of 107±3°C.

一種包含白克列及氟嘧菌酯之共熔混合物之組成物,其中該共熔混合物的特徵在於DSC具有100±3℃的起始溫度及107±3℃的吸熱峰。 A composition comprising a eutectic mixture of bakleyl and fluoxastrobin, wherein the eutectic mixture is characterized by a DSC onset temperature of 100±3°C and an endothermic peak of 107±3°C.

一種用於配製農業化學組成物之程序,該農業化學組成物包含白克列及嗜球果傘素殺真菌劑之共熔混合物。 A process for formulating an agrochemical composition comprising a eutectic mixture of bacrine and strobilurin fungicides.

一種用於製備白克列及嗜球果傘素殺真菌劑之共熔混合物之程序,其包含將白克列與嗜球果傘素殺真菌劑以預定比率一起加工。 A process for the preparation of a eutectic mixture of a strobilurin fungicide and a buccalide comprising co-processing the buccalidine and a strobilurin fungicide in a predetermined ratio.

一種控制植物病原性真菌之方法,該方法包含對植物或其棲地、植物種子或土壤施用殺真菌有效量之包含白克列及嗜球果傘素殺真菌劑之共熔混合物的組成物。 A method of controlling phytopathogenic fungi comprising applying to a plant or its habitat, plant seeds or soil a fungicidally effective amount of a composition comprising a eutectic mixture of buccalide and strobilurin fungicides.

一種共熔混合物,其包含白克列及嗜球果傘素殺真菌劑。 A eutectic mixture comprising buclide and strobilurin fungicides.

一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物。 An agricultural chemical composition comprising a eutectic mixture of bacrine and strobilurin fungicides.

一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物;以及至少一種農業化學上可接受的賦形劑,其中該共熔混合物的形成抑制白克列及嗜球果傘素殺真菌劑的結晶程序。 An agrochemical composition comprising a eutectic mixture of buccalidine and a strobilurin fungicide; and at least one agrochemically acceptable excipient, wherein formation of the eutectic mixture inhibits buccalidine and strobilurin fungicides; Crystallization procedure for the strobilurin fungicide.

一種包含以重量計10至90%之間的白克列及90至10%之間的嗜球果傘素殺真菌劑之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight, between 10 and 90% buccalidine and between 90 and 10% strobilurin fungicides, wherein at least a portion of the fungicide mixture is a eutectic mixture form.

一種包含以重量計50至80%之間的白克列及50至20%之間的嗜球果傘素殺真菌劑之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight, between 50 and 80% buccalidine and between 50 and 20% strobilurin fungicides, wherein at least a portion of the fungicide mixture is a eutectic mixture form.

一種包含以活性成分之重量計50至80%之間的白克列及50至20%之間的嗜球果傘素殺真菌劑之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of the active ingredient, between 50 and 80% bacrine and between 50 and 20% strobilurin fungicides, wherein at least a portion of the fungicide mixture is co- form of molten mixture.

一種白克列及亞托敏之共熔混合物。 A eutectic mixture of becryl and yatormin.

一種農業化學組成物,其包含白克列及亞托敏之共熔混合物。 An agricultural chemical composition, which comprises a eutectic mixture of becryl and yatomin.

一種包含以重量計10至90%之間的白克列及90至10%之間的亞托敏之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising between 10 and 90% by weight of becryl and between 90 and 10% of atropamine, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture.

一種包含以重量計50至80%之間的白克列及50至20%之間的亞托敏之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising between 50 and 80% by weight of becryl and between 50 and 20% of atropamine, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture.

一種包含以活性成分之重量計50至80%之間的白克列及50至20%之間的亞托敏之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of active ingredient, between 50 and 80% of bacilli and between 50 and 20% of atropamine, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture.

一種共熔混合物,其包含以活性成分之重量計約60%的白克列及約40%的亞托敏。 A eutectic mixture comprising, by weight of active ingredient, about 60% becryl and about 40% atropamine.

一種包含以活性成分之重量計約60%的白克列及約40%的亞托敏之組成物,其中該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of active ingredient, about 60% becryl and about 40% atropamine, wherein the fungicide mixture is in the form of a eutectic mixture.

一種共熔混合物,其包含以活性成分之重量計約37.5%的白克列及約25%的亞托敏。 A eutectic mixture comprising, by weight of active ingredients, about 37.5% becryl and about 25% atropamine.

一種包含以活性成分之重量計約37.5%的白克列及約25%的亞托敏之組成物,其中該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of active ingredient, about 37.5% bacilli and about 25% atropamine, wherein the fungicide mixture is in the form of a eutectic mixture.

一種組成物,其包含白克列及亞托敏,其莫耳比為1:9至9:1,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising bacilli and yatormin in a molar ratio of 1:9 to 9:1, wherein at least a part of the fungicide mixture is in the form of a eutectic mixture.

一種組成物,其包含白克列及亞托敏,其莫耳比為1:5至5:1,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition, which comprises bacilli and yatormine, the molar ratio of which is 1:5 to 5:1, wherein at least a part of the fungicide mixture is in the form of eutectic mixture.

一種組成物,其包含白克列及亞托敏,其莫耳比為1:3至3:1,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising bacilli and yatormin in a molar ratio of 1:3 to 3:1, wherein at least a part of the fungicide mixture is in the form of a eutectic mixture.

一種組成物,其包含白克列及亞托敏,其莫耳比為1.5:1,其中該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising bacilli and yatormin at a molar ratio of 1.5:1, wherein the fungicide mixture is in the form of a eutectic mixture.

一種共熔混合物,其包含白克列及亞托敏,其莫耳比為1.5:1。 A eutectic mixture, which contains bakleyl and yatormin, with a molar ratio of 1.5:1.

一種包含白克列及亞托敏之共熔混合物之組成物的特徵在於DSC具有100±3℃的起始溫度及103±3℃的吸熱峰。 A composition comprising a eutectic mixture of bakleyl and tropamine is characterized in that DSC has an onset temperature of 100±3°C and an endothermic peak of 103±3°C.

一種包含白克列及亞托敏之共熔混合物的特徵在於DSC具有100±3℃的起始溫度及103±3℃的吸熱峰。 A eutectic mixture comprising bakleyl and tropamine is characterized by a DSC onset temperature of 100±3°C and an endothermic peak of 103±3°C.

一種包含白克列及亞托敏之共熔混合物之組成物的特徵在於DSC具有100±3℃的起始溫度及102℃與106℃之間的吸熱峰。 A composition comprising a eutectic mixture of bakleyl and yatormin is characterized by a DSC onset temperature of 100±3°C and an endothermic peak between 102°C and 106°C.

一種包含白克列及亞托敏之共熔混合物的特徵在於DSC具有100±3℃的起始溫度及102℃與106℃之間的吸熱峰。 A eutectic mixture comprising bakleyl and tropamine is characterized by a DSC onset temperature of 100±3°C and an endothermic peak between 102°C and 106°C.

一種包含白克列及亞托敏之共熔混合物之組成物的特徵在於DSC具有100.07℃的起始溫度及103.5℃的吸熱峰。 A composition comprising a eutectic mixture of bacletide and tropamine is characterized by a DSC onset temperature of 100.07°C and an endothermic peak of 103.5°C.

一種包含白克列及亞托敏之共熔混合物的特徵在於DSC具有100.07℃的起始溫度及103.5℃的吸熱峰。 A eutectic mixture comprising bakleyl and tropamine is characterized by a DSC onset temperature of 100.07°C and an endothermic peak of 103.5°C.

一種包含白克列及亞托敏之共熔混合物,其特徵在於具有如第3圖所繪示之DSC熱分析圖。 A eutectic mixture comprising bakleyl and yatormin is characterized by having a DSC thermogram as shown in FIG. 3 .

一種包含白克列及亞托敏之組成物,其特徵在於具有如第3圖所繪示之DSC熱分析圖。 A composition comprising bacryl and yatormin is characterized by having a DSC thermogram as shown in FIG. 3 .

一種包含白克列及亞托敏之共熔混合物,其特徵在於具有如第4圖所繪示之相圖。 A eutectic mixture comprising bakleyl and yatormin is characterized by having a phase diagram as shown in FIG. 4 .

一種包含白克列及亞托敏之組成物,其特徵在於具有如第4圖所繪示之相圖。 A composition comprising bekleyl and yatormin is characterized by having a phase diagram as shown in FIG. 4 .

一種白克列及氟嘧菌酯之共熔混合物。 A eutectic mixture of bacilli and fluoxastrobin.

一種農業化學組成物,其包含白克列及氟嘧菌酯之共熔混合物。 An agricultural chemical composition, which comprises a eutectic mixture of bakleyl and fluoxastrobin.

一種包含以重量計10至90%之間的白克列及90至10%之間的氟嘧菌酯之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising between 10 and 90% by weight of becryl and between 90 and 10% of fluoxastrobin, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture.

一種包含以重量計50至80%之間的白克列及20至50%之間的氟嘧菌酯之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising between 50 and 80% by weight of becryl and between 20 and 50% of fluoxastrobin, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture.

一種包含以重量計20至50%之間的白克列及50至80%之間的氟嘧菌酯之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising between 20 and 50% by weight of becryl and between 50 and 80% of fluoxastrobin, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture.

一種包含以活性成分之重量計50至80%之間的白克列及50至20%之間的氟嘧菌酯之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of active ingredient, between 50 and 80% of buccolidine and between 50 and 20% of fluoxastrobin, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture .

一種包含以活性成分之重量計20至50%之間的白克列及50至80%之間的氟嘧菌酯之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of active ingredient, between 20 and 50% of baccolidine and between 50 and 80% of fluoxastrobin, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture .

一種共熔混合物,其包含以活性成分之重量計約25%的白克列及約75%的氟嘧菌酯。 A eutectic mixture comprising, by weight of the active ingredient, about 25% bekret and about 75% fluoxastrobin.

一種包含以活性成分之重量計約25%的白克列及約75%的氟嘧菌酯之組成物,其中該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of active ingredient, about 25% baccolidine and about 75% fluoxastrobin, wherein the fungicide mixture is in the form of a eutectic mixture.

一種共熔混合物,其包含以活性成分之重量計約50%的白克列及約50%的氟嘧菌酯。 A eutectic mixture comprising, by weight of the active ingredient, about 50% bacilli and about 50% fluoxastrobin.

一種包含以活性成分之重量計約50%的白克列及約50%的氟嘧菌酯之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of the active ingredient, about 50% buccolidine and about 50% fluoxastrobin, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture.

一種共熔混合物,其包含以活性成分之重量計約60%的白克列及約40%的氟嘧菌酯。 A eutectic mixture comprising, by weight of the active ingredient, about 60% bekret and about 40% fluoxastrobin.

一種包含以活性成分之重量計約60%的白克列及約40%的氟嘧菌酯之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of active ingredient, about 60% baccolidine and about 40% fluoxastrobin, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture.

一種共熔混合物,其包含以活性成分之重量計約75%的白克列及約25%的氟嘧菌酯。 A eutectic mixture comprising, by weight of active ingredient, about 75% bucret and about 25% fluoxastrobin.

一種包含以活性成分之重量計約75%的白克列及約25%的氟嘧菌酯之組成物,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising, by weight of active ingredient, about 75% baccolidine and about 25% fluoxastrobin, wherein at least a portion of the fungicide mixture is in the form of a eutectic mixture.

一種組成物,其包含白克列及氟嘧菌酯,其莫耳比為1:9至9:1,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising buclide and fluoxastrobin in a molar ratio of 1:9 to 9:1, wherein at least a part of the fungicide mixture is in the form of a eutectic mixture.

一種組成物,其包含白克列及氟嘧菌酯,其莫耳比為1:5至5:1,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising buclide and fluoxastrobin in a molar ratio of 1:5 to 5:1, wherein at least a part of the fungicide mixture is in the form of a eutectic mixture.

一種組成物,其包含白克列及氟嘧菌酯,其莫耳比為1:3至3:1,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising buclide and fluoxastrobin in a molar ratio of 1:3 to 3:1, wherein at least a part of the fungicide mixture is in the form of a eutectic mixture.

一種組成物,其包含白克列及氟嘧菌酯,其莫耳比為1.5:1,其中至少一部分的該殺真菌劑混合物係呈共熔混合物的形式。 A composition comprising buclide and fluoxastrobin in a molar ratio of 1.5:1, wherein at least a part of the fungicide mixture is in the form of a eutectic mixture.

一種共熔混合物,其包含白克列及氟嘧菌酯,其莫耳比為1:3。 A eutectic mixture comprising buclide and fluoxastrobin in a molar ratio of 1:3.

一種包含白克列及氟嘧菌酯之共熔混合物之組成物的特徵在於DSC具有92±3℃的起始溫度及97±3℃的吸熱峰。 A composition comprising a eutectic mixture of bakleyl and fluoxastrobin is characterized in that DSC has an onset temperature of 92±3°C and an endothermic peak of 97±3°C.

一種包含白克列及氟嘧菌酯之共熔混合物的特徵在於DSC具有92±3℃的起始溫度及97±3℃的吸熱峰。 A eutectic mixture comprising bakleyl and fluoxastrobin is characterized by a DSC onset temperature of 92±3°C and an endothermic peak of 97±3°C.

一種包含白克列及氟嘧菌酯之共熔混合物之組成物的特徵在於DSC具有92±3℃的起始溫度及94℃與100℃之間的吸熱峰。 A composition comprising a eutectic mixture of bakleyl and fluoxastrobin is characterized by a DSC onset temperature of 92±3°C and an endothermic peak between 94°C and 100°C.

一種包含白克列及氟嘧菌酯之共熔混合物之組成物的特徵在於DSC具有92±3℃的起始溫度及97與99℃之間的吸熱峰。 A composition comprising a eutectic mixture of bakleyl and fluoxastrobin is characterized by a DSC onset temperature of 92±3°C and an endothermic peak between 97 and 99°C.

一種包含白克列及氟嘧菌酯之共熔混合物之組成物的特徵在於DSC具有100±3℃的起始溫度及104℃與110℃之間的吸熱峰。 A composition comprising a eutectic mixture of bakleyl and fluoxastrobin is characterized by a DSC onset temperature of 100±3°C and an endothermic peak between 104°C and 110°C.

一種包含白克列及氟嘧菌酯之共熔混合物之組成物的特徵在於DSC具有100±3℃的起始溫度及107℃至108℃的吸熱峰。 A composition comprising a eutectic mixture of bakleyl and fluoxastrobin is characterized in that DSC has an onset temperature of 100±3°C and an endothermic peak of 107°C to 108°C.

一種包含白克列及氟嘧菌酯之共熔混合物,其特徵在於具有如第10圖及第11圖所繪示之DSC熱分析圖。 A eutectic mixture comprising bakleyl and fluoxastrobin is characterized by having a DSC thermogram as shown in FIG. 10 and FIG. 11 .

一種包含白克列及氟嘧菌酯之組成物,其特徵在於具有如第10圖及第11圖所繪示之DSC熱分析圖。 A composition comprising bakleyl and fluoxastrobin is characterized by having a DSC thermogram as shown in Fig. 10 and Fig. 11 .

一種共熔混合物,其包含白克列、嗜球果傘素殺真菌劑及第三殺真菌劑。 A eutectic mixture comprising bacrine, a strobilurin fungicide and a third fungicide.

一種共熔混合物,其包含白克列、嗜球果傘素殺真菌劑、至少一種第三殺真菌劑,及至少一種第四殺真菌劑。 A eutectic mixture comprising bacrine, a strobilurin fungicide, at least one third fungicide, and at least one fourth fungicide.

一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物,及第三殺真菌劑。 An agricultural chemical composition comprising a eutectic mixture of bacrine and strobilurin fungicides, and a third fungicide.

一種農業化學組成物,其包含白克列及嗜球果傘素殺真菌劑之共熔混合物、至少一種第三殺真菌劑,及至少一種第四殺真菌劑。 An agricultural chemical composition comprising a eutectic mixture of bacrine and strobilurin fungicides, at least one third fungicide, and at least one fourth fungicide.

現在將參照下列特定實例來描述本發明。應注意的是,下文所附之實例說明而非限制本發明,且所屬技術領域中具有通常知識者將能夠設計許多替代實施例,而不脫離本發明之範疇。 The invention will now be described with reference to the following specific examples. It should be noted that the following examples illustrate rather than limit the invention, and that those skilled in the art will be able to design many alternative embodiments without departing from the scope of the invention.

實例1:根據本發明之白克列及亞托敏之共熔混合物製備如下: Example 1: The eutectic mixture of Bacryl and Atropamine according to the present invention was prepared as follows:

在瑪瑙研缽中以如表1所示之不同比率研磨白克列及亞托敏,並將混合物徹底研磨。藉由DSC分析所得混合物。 Grind bekrell and yatormin at different ratios as shown in Table 1 in an agate mortar and grind the mixture thoroughly. The resulting mixture was analyzed by DSC.

Figure 108124806-A0305-02-0028-1
Figure 108124806-A0305-02-0028-1
Figure 108124806-A0305-02-0029-2
Figure 108124806-A0305-02-0029-2

檢測共熔混合物之方法:Method for detecting eutectic mixture:

藉由記錄DSC來檢測共熔混合物。 Eutectic mixtures were detected by recording DSC.

白克列的吸熱峰記錄在144至148℃之間(起始溫度為144.71,△H=83.65J/g)[第1圖]。亞托敏的吸熱峰記錄在112至118℃之間(起始溫度為114.34.2℃,△H=86.19J/g)[第2圖]。對各種比率的白克列:亞托敏之混合物進行DSC。結果顯示白克列:亞托敏之比率為60:40,所形成的共熔混合物在103.5℃顯示單一的吸熱峰(共熔點)(第3圖)。在所有其他比率中,觀察到兩個不同的吸熱,一者係來自共熔混合物之熔化,而另一者係來自過量組分之熔化,其繪示於相圖(第4圖)中。 The endothermic peak of Bekleyl was recorded between 144 and 148°C (onset temperature of 144.71, △H=83.65J/g) [Figure 1]. The endothermic peak of ytropamine was recorded between 112 and 118°C (onset temperature of 114.34.2°C, △H=86.19J/g) [Figure 2]. DSC was performed on mixtures of various ratios of bectilide:yatormin. The results showed that the ratio of Becglide:Atropamine was 60:40, and the eutectic mixture formed showed a single endothermic peak (eutectic point) at 103.5°C (Fig. 3). In all other ratios, two different endotherms were observed, one from the melting of the eutectic mixture and the other from the melting of the excess components, which are depicted in the phase diagram (Fig. 4).

實例2:一種包含根據本發明之白克列(無水物修飾I)及亞托敏之共熔混合物之組成物,其已製備如下: Example 2 : A composition comprising a eutectic mixture of Bacrine (anhydrous modified I) and atropamine according to the present invention, which has been prepared as follows:

Figure 108124806-A0305-02-0029-3
Figure 108124806-A0305-02-0029-3

將白克列及亞托敏秤重、在瑪瑙研缽中研磨,並將混合物徹底研磨。然後將混合物與所列成分一起在空氣噴射研磨機(Air jet mill)中研磨,以獲得所需的粒度。在此粉末狀混合物中添加水以製備麵團。將麵團置於造粒機中來製備顆粒。使用乾燥器乾燥顆粒,然後過篩。藉由DSC分析顆粒。在下列情況下觀察DSC吸熱峰:104.5℃。(第5圖)。 Weigh the bekrell and yatomin, grind in an agate mortar, and grind the mixture thoroughly. The mixture was then ground in an Air jet mill with the listed ingredients to obtain the desired particle size. Add water to this powdered mixture to prepare the dough. Pellets were prepared by placing the dough in a granulator. Dry the granules using a drier, then sieve. Particles were analyzed by DSC. The DSC endothermic peak was observed at: 104.5°C. (Figure 5).

實例3:一種包含根據本發明之白克列(無水物修飾II)及亞托敏之共熔混合物之組成物,其已製備如下: Example 3 : A composition comprising a eutectic mixture of Bacrine (anhydrous modification II) and atropamine according to the present invention, which has been prepared as follows:

Figure 108124806-A0305-02-0030-4
Figure 108124806-A0305-02-0030-4

將白克列及亞托敏秤重,然後與所列成分一起在空氣噴射研磨機(Air jet mill)中研磨,以獲得所需的粒度,並按照實例2之程序製備組成物。藉由DSC分析顆粒。在下列情況下觀察DSC吸熱峰:105.89℃。(第6圖)。 The Bacryl and Yatropin were weighed, and then ground together with the listed ingredients in an air jet mill to obtain the desired particle size, and the composition was prepared according to the procedure in Example 2. Particles were analyzed by DSC. The DSC endothermic peak was observed at the following conditions: 105.89°C. (Figure 6).

表4中給出根據本發明之各種本發明組成物的細節,其包含白克列及亞托敏之共熔混合物。按照實例2之程序製備組成物。 Details of various inventive compositions according to the present invention are given in Table 4, which comprise eutectic mixtures of bakleyl and atropamine. The composition was prepared according to the procedure of Example 2.

使用不同比率之白克列及亞托敏來製備不同配方。各種組分之重量比的細節列於下表4中:

Figure 108124806-A0305-02-0030-5
Different formulations were prepared using different ratios of bacilli and yatormin. Details of the weight ratios of the various components are listed in Table 4 below:
Figure 108124806-A0305-02-0030-5

根據本發明之配方的穩定性 Stability of formulations according to the invention

根據BIS規格測試根據本發明所製備的白克列-亞托敏組成物之儲存穩定性。將樣品保持在室溫(27±2℃)下,以落實配方的實時穩定性。本發明人已觀察到,根據本發明所製備之組成物係穩定的,且並未觀察到該組成物的形態 變化。實例2的DSC,在儲存9個月之後,在105.3℃顯示對應於該共熔混合物的吸熱峰(第8圖),證明該組成物的穩定性。 The storage stability of the bakleyl-yatropin composition prepared according to the present invention was tested according to the BIS specification. Samples were kept at room temperature (27±2°C) to ensure real-time stability of the formulation. The inventors have observed that the composition prepared according to the present invention is stable and the morphology of the composition has not been observed Variety. The DSC of Example 2, after storage for 9 months, showed an endothermic peak corresponding to the eutectic mixture at 105.3°C (Fig. 8), demonstrating the stability of the composition.

實例4:根據本發明之白克列及氟嘧菌酯之共熔混合物製備如下(乾式研磨方法): Example 4: The eutectic mixture of bacilli and fluoxastrobin according to the present invention was prepared as follows (dry grinding method):

在瑪瑙研缽中以如表5所示之不同比率研磨白克列及氟嘧菌酯,並將混合物徹底研磨。藉由DSC分析所得混合物。 Grind bacilli and fluoxastrobin in different ratios as shown in Table 5 in an agate mortar and grind the mixture thoroughly. The resulting mixture was analyzed by DSC.

Figure 108124806-A0305-02-0031-6
Figure 108124806-A0305-02-0031-6

檢測共熔混合物之方法:Method for detecting eutectic mixture:

藉由記錄DSC來檢測共熔混合物。 Eutectic mixtures were detected by recording DSC.

白克列的吸熱峰記錄在144至148℃之間(起始溫度為144.71,△H=83.65J/g)[第1圖]。氟嘧菌酯的吸熱峰記錄在104至114℃之間(起始溫度為105.82℃,△H=72.04J/g)[第9圖]。對各種比率的白克列:氟嘧菌酯之混合物進行DSC。結果顯示白克列:氟嘧菌酯之比率為30:70,所形成的共熔混合物在97.7℃顯示單一的吸熱峰(共熔點)(第10圖)。 The endothermic peak of Bekleyl was recorded between 144 and 148°C (onset temperature of 144.71, △H=83.65J/g) [Figure 1]. The endothermic peak of fluoxastrobin was recorded between 104 and 114°C (onset temperature of 105.82°C, △H=72.04J/g) [Figure 9]. DSC was performed on mixtures of various ratios of bacilli:fluoxastrobin. The results showed that the ratio of Bakleyl: fluoxastrobin was 30:70, and the eutectic mixture formed showed a single endothermic peak (eutectic point) at 97.7°C (Fig. 10).

實例5:根據本發明之白克列及氟嘧菌酯之共熔混合物製備如下(溶劑蒸發法): Example 5: According to the eutectic mixture of bakleyl and fluoxastrobin of the present invention is prepared as follows (solvent evaporation method):

將白克列(1.005g,1.02莫耳)及氟嘧菌酯(4.029g,3.0莫耳)在丙酮(20ml)中攪拌直至在50至55℃下溶解,並將溶液在此溫度下保持15min。將溶劑部分蒸發,並使濃縮溶液放置一邊18小時以促進結晶。將結晶固體在真空下乾燥以獲得4.9g的共熔混合物(白克列:氟嘧菌酯:25:75)。藉由DSC分析晶體。在下列情況下觀察DSC吸熱峰:107.5℃。(第11圖)。 Stir beclay (1.005g, 1.02 mol) and fluoxastrobin (4.029g, 3.0 mol) in acetone (20ml) until dissolved at 50 to 55°C, and keep the solution at this temperature for 15min . The solvent was partially evaporated and the concentrated solution was set aside for 18 hours to promote crystallization. The crystalline solid was dried under vacuum to obtain 4.9 g of eutectic mixture (Bekrell:fluoxastrobin:25:75). Crystals were analyzed by DSC. The DSC endothermic peak was observed at: 107.5°C. (Fig. 11).

實例6:一種包含根據本發明之白克列(無水物修飾II)及氟嘧菌酯之共熔混合物之組成物,其已製備如下: Example 6 : A composition comprising a eutectic mixture of Bacrine (anhydrous modification II) and fluoxastrobin according to the present invention, which has been prepared as follows:

Figure 108124806-A0305-02-0032-7
Figure 108124806-A0305-02-0032-7

取出白克列及氟嘧菌酯,並按照實例2之程序製備組成物。 Take out the buccalide and fluoxastrobin, and prepare the composition according to the procedure in Example 2.

表7中給出根據本發明之各種本發明組成物的細節,其包含白克列及氟嘧菌酯之共熔混合物。按照實例2之程序製備組成物。 Details of various compositions of the invention according to the invention are given in Table 7, which comprise eutectic mixtures of bakret and fluoxastrobin. The composition was prepared according to the procedure of Example 2.

使用不同比率之白克列及氟嘧菌酯來製備不同配方。各種組分之重量比的細節列於下表7中:

Figure 108124806-A0305-02-0032-9
Figure 108124806-A0305-02-0033-10
Different formulations were prepared using different ratios of bacilli and fluoxastrobin. Details of the weight ratios of the various components are listed in Table 7 below:
Figure 108124806-A0305-02-0032-9
Figure 108124806-A0305-02-0033-10

田間試驗研究: Field trial research:

方案:使用根據本發明所製備的白克列及亞托敏之共熔混合物的組成物作為殺真菌劑來進行田間試驗。該等組成物可選地與其他槽混合助劑混合,並以500至600kg/ha的施用率施用至番茄(早疫病)、辣椒(白粉病)、洋蔥(枯萎病)、及葡萄(白粉病)。百克敏12.8%+白克列25.2% WG-Visma之商業習知配方的劑量係600ml/h。亞托敏250 SC-Amistar之商業習知配方的劑量係562.5ml/h。處理後10天及14天的觀察結果已總結於下表,證明該組成物的生物效能。 Solution: use the composition of the eutectic mixture of bakleyl and yatormine prepared according to the present invention as a fungicide to carry out a field test. These compositions are optionally mixed with other tank mixing aids and applied to tomatoes (early blight), peppers (powdery mildew), onions (fusarium wilt), and grapes (powdery mildew) at an application rate of 500 to 600 kg/ha. ). The dosage of the commercially known formulation of Becmin 12.8%+Beccleline 25.2% WG-Visma is 600ml/h. The dosage of Atropin 250 SC-Amistar is 562.5ml/h in a commercially known formulation. The observations at 10 days and 14 days after treatment are summarized in the table below, demonstrating the biological efficacy of the composition.

田間試驗:番茄(早疫病)、辣椒(白粉病)、洋蔥(枯萎病)、及葡萄(白粉病)的真菌控制研究。 Field Trials: Fungal Control Studies in Tomatoes (Early Blight), Peppers (Powdery Mildew), Onions (Fusarium Wilt), and Grapes (Powdery Mildew).

測試包含白克列及亞托敏之共熔混合物(實例2)、以及百克敏+白克列WG(VISMA)之市場樣本及亞托敏(AMISTAR)之市場樣本的配方之各種劑量對於番茄、辣椒、洋蔥、及葡萄的真菌控制。真菌包括對於番茄之番茄夏疫病菌、對於辣椒之韃靼內絲白粉菌(Leveillula taurica)、對於洋蔥之囊狀匍柄黴(Stemphylium vesicarium)、及對於葡萄之韃靼內絲白粉菌(Leveillula taurica)。 Tests of formulations containing eutectic mixtures of bacrylide and yatoramine (Example 2), and market samples of becclemine + bacrylide WG (VISMA) and yatoramine (AMISTAR) at various doses for tomato, pepper , onion, and grape fungus control. Fungi include Phytophthora solani on tomato, Leveillula taurica on pepper, Stemphylium vesicarium on onion, and Leveillula taurica on grape.

Figure 108124806-A0305-02-0033-11
Figure 108124806-A0305-02-0033-11

從上述結果已觀察到,包含根據實例2所製備之布克列及亞托敏之共熔混合物的配方,在400kg/ha的較低施用率下顯示出良好的真菌控制。已 注意到,在任何給定的施用率下,相較於VISMA(百克敏12.8%+白克列25.2% WG,商業樣本)及AMISTAR(亞托敏250 SC,商業樣本),包含白克列及亞托敏之共熔混合物的配方顯示較高的生物效能及較高的一致性。更具體而言,已觀察到包含白克列及亞托敏之共熔混合物的配方,在500.0kg/ha之較低施用率下,比施用率為600kg/ha之VISMA及施用率為562.5kg/ha之AMISTAR,展現出更好的生物效能。因此,結論為相較於其他習知的白克列及/或嗜球果傘素系配方,包含白克列及亞托敏之共熔混合物的配方,在較低劑量下可有效地用作為具有較佳生物效能之殺真菌劑。 From the above results it has been observed that the formulation comprising the eutectic mixture of Buccolid and Itropamine prepared according to Example 2 showed good fungal control at a lower application rate of 400 kg/ha. already Note that, at any given application rate, compared to VISMA (12.8% bacclemine + 25.2% WG, commercial sample) and AMISTAR (yatropamine 250 SC, commercial sample), the combination of Bacryl and The formulation of the eutectic mixture of yatormin showed high bioefficacy and high consistency. More specifically, it has been observed that formulations comprising eutectic mixtures of buclide and yatormin, at a lower application rate of 500.0 kg/ha, were more effective than VISMA at an application rate of 600 kg/ha and at an application rate of 562.5 kg/ha. ha's AMISTAR showed better biological efficacy. Therefore, it was concluded that formulations comprising eutectic mixtures of bacrine and yatormin could be effectively used at lower doses as Fungicide with better biological efficacy.

Claims (12)

一種50-80%白克列(boscalid)及50-20%嗜球果傘素(strobilurin)殺真菌劑之共熔混合物,該嗜球果傘素殺真菌劑選自包含下列之群組:亞托敏(azoxystrobin)、啶氧菌酯(picoxystrobin)、三氟敏(trifloxystrobin)及氟嘧菌酯(fluoxastrobin),其中該共熔混合物在103.5±3℃、97±3℃或107±3℃具有一吸熱峰。 A eutectic mixture of 50-80% boscalid and 50-20% strobilurin fungicide selected from the group comprising: Azoxystrobin, picoxystrobin, trifloxystrobin and fluoxastrobin, wherein the eutectic mixture has An endothermic peak. 一種農業化學組成物,其包含50-80%白克列及50-20%嗜球果傘素殺真菌劑之一共熔混合物,該嗜球果傘素殺真菌劑選自包含下列之群組:亞托敏(azoxystrobin)、啶氧菌酯(picoxystrobin)、三氟敏(trifloxystrobin)及氟嘧菌酯(fluoxastrobin),其中該共熔混合物在103.5±3℃、97±3℃或107±3℃具有一吸熱峰。 An agricultural chemical composition comprising a eutectic mixture of 50-80% buccalidine and 50-20% strobilurin fungicide selected from the group comprising: Azoxystrobin, picoxystrobin, trifloxystrobin and fluoxastrobin, wherein the eutectic mixture is at 103.5±3°C, 97±3°C or 107±3°C Has an endothermic peak. 一種製備50-80%白克列及50-20%嗜球果傘素殺真菌劑之共熔混合物的程序,該程序包含使白克列及嗜球果傘素殺真菌劑經受溶液結晶、乾式研磨、溶劑滴式研磨技術,或噴霧乾燥技術,其中該共熔混合物在103.5±3℃、97±3℃或107±3℃具有一吸熱峰。 A process for the preparation of a eutectic mixture of 50-80% buccalidine and 50-20% strobilurin fungicide, the process comprising subjecting the buccalide and strobilurin fungicide to solution crystallization, dry Milling, solvent drop milling technique, or spray drying technique, wherein the eutectic mixture has an endothermic peak at 103.5±3°C, 97±3°C or 107±3°C. 如申請專利範圍第3項之程序,其中該程序包含:a.在一或多種溶劑中製備一白克列及嗜球果傘素殺真菌劑之濃縮溶液;b.可選地將該溶劑蒸發,該溶劑選自脂族醇、酮、酯、醚、極性質子性溶劑、極性非質子性溶劑、鹵化溶劑、脂族烴或芳族烴;及c.用一反溶劑研製或沉澱以獲得一共熔混合物,其中該反溶劑選自脂族或芳族烴溶劑。 A procedure as claimed in claim 3, wherein the procedure comprises: a. preparing a concentrated solution of buccalidine and strobilurin fungicides in one or more solvents; b. optionally evaporating the solvent , the solvent is selected from aliphatic alcohols, ketones, esters, ethers, polar protic solvents, polar aprotic solvents, halogenated solvents, aliphatic hydrocarbons or aromatic hydrocarbons; and c. Trituration or precipitation with an antisolvent to obtain A eutectic mixture wherein the anti-solvent is selected from aliphatic or aromatic hydrocarbon solvents. 如申請專利範圍第3項之程序,其中該程序包含:a.將白克列與嗜球果傘素殺真菌劑摻和; b.可選地將溶劑摻和至該摻和物中,該溶劑選自脂族醇、酮、酯、醚、極性質子性溶劑、極性非質子性溶劑、鹵化溶劑、脂族烴或芳族烴;及c.研磨或壓碎或碾磨該摻和物以獲得該共熔混合物。 Such as applying for the procedure of item 3 of the patent scope, wherein the procedure includes: a. blending bakleyl with strobilurin fungicide; b. Optionally blending into the blend a solvent selected from aliphatic alcohols, ketones, esters, ethers, polar protic solvents, polar aprotic solvents, halogenated solvents, aliphatic hydrocarbons or aromatic and c. grinding or crushing or milling the blend to obtain the eutectic mixture. 一種50-80%白克列及50-20%亞托敏之共熔混合物,其在103.5±3℃具有一吸熱峰。 A eutectic mixture of 50-80% becryl and 50-20% tropamine, which has an endothermic peak at 103.5±3°C. 一種農業化學組成物,其包含白克列及亞托敏之共熔混合物,其中該組成物包含以重量計50-80%之間的白克列及50-20%之間的亞托敏,以及其中該共熔混合物在103.5±3℃具有一吸熱峰。 An agrochemical composition comprising a eutectic mixture of becrylide and yatormin, wherein the composition comprises 50-80% by weight of becrylide and 50-20% of yatormin, and Wherein the eutectic mixture has an endothermic peak at 103.5±3°C. 一種50-80%白克列及50-20%氟嘧菌酯之共熔混合物,其在97±3℃具有一吸熱峰。 A eutectic mixture of 50-80% beclay and 50-20% fluoxastrobin, which has an endothermic peak at 97±3°C. 一種農業化學組成物,其包含白克列及氟嘧菌酯之共熔混合物,其中該組成物包含以重量計50-80%之間的一白克列及50-20%之間的氟嘧菌酯,以及其中該共熔混合物在97±3℃具有一吸熱峰。 An agricultural chemical composition comprising a eutectic mixture of buccalidine and fluoxastrobin, wherein the composition comprises between 50-80% by weight of a buccalidine and between 50-20% of fluoropyrim Strostrobin, and wherein the eutectic mixture has an endothermic peak at 97±3°C. 一種用於配製包含50-80%白克列及50-20%嗜球果傘素殺真菌劑之共熔混合物的農業化學組成物之程序,該程序包含在添加或不添加農業化學上可接受的賦形劑的情況下製備白克列及嗜球果傘素殺真菌劑之共熔混合物,及將該混合物進一步加工成適合的形式,其中該共熔混合物在103.5±3℃、97±3℃或107±3℃具有一吸熱峰。 A process for formulating an agrochemical composition comprising a eutectic mixture of 50-80% buccalidine and 50-20% strobilurin fungicide comprising the addition or absence of agrochemically acceptable Preparation of eutectic mixture of bacrine and strobilurin fungicides with excipients, and further processing of the mixture into a suitable form, wherein the eutectic mixture is at 103.5±3°C, 97±3 °C or 107±3°C has an endothermic peak. 如申請專利範圍第10項之程序,其中該農業化學組成物係配製成一粒狀組成物。 Such as the procedure of item 10 of the scope of the patent application, wherein the agricultural chemical composition is formulated into a granular composition. 一種對抗或控制真菌之方法,該方法包含使真菌或其基因座與殺真菌有效量之組成物接觸,該組成物包含50-80%白克列及50-20%嗜球果傘素殺真菌劑之共熔混合物,該嗜球果傘素殺真菌劑選自包含下列之群組:亞托敏、啶氧 菌酯、三氟敏及氟嘧菌酯,其中該共熔混合物在103.5±3℃、97±3℃或107±3℃具有一吸熱峰。 A method of combating or controlling fungi, the method comprising contacting the fungi or their genetic loci with a fungicidally effective amount of a composition comprising 50-80% buccalidine and 50-20% strobilurin fungicidal A eutectic mixture of a strobilurin fungicide selected from the group comprising: atropamine, pyridoxine Strostrobin, triflurin and fluoxastrobin, wherein the eutectic mixture has an endothermic peak at 103.5±3°C, 97±3°C or 107±3°C.
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