JPS59219206A - Novel composition showing synergistic activity as agricultural insecticide, repellent and tickicide - Google Patents

Abstract

(57) [Abstract] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

DETAILED DESCRIPTION OF THE INVENTION Avermectin compounds are produced by Streptomyces avermitilis (Streptomyces averm mount 1).
1s) is a series of natural substances isolated from the culture fluid of a single strain of bacteria. The compound group consists of 8 compounds, ie, 4 major components and 4 trace components. This compound is disclosed in US Pat. No. 4,510.590. Certain derivatives of the compounds have also been disclosed, e.g. 22.23.
-dihydro derivatives are described in U.S. Pat. No. 4,199,569. 13-deoxy derivatives of avermectin compounds are US%r! - Disclosed in Nos. 4,171,514 and 4,173,571.

Furthermore, 41+-phosphate ester derivatives of avermectin compounds having a 13-0-disaccharide group are also included in the combination of the present invention.

The compound is disclosed in co-pending U.S. Patent Application No. 461.846.
Disclosed in the issue.

Combinations that exhibit synergy are also l-The1981F
arm Chemicals Handbook,
C266 page, and Merck-Index l-Tbe
Merck Indcxj.

Contains insect metabolic inhibitors such as piperonyl butoxide, which is listed in the 9th Edition, 7270.

The present invention describes certain combinations of avermectin compounds and insect metabolic inhibitors that act synergistically as insecticides, repellents, and acaricides. It is an object of the present invention to describe such cooperative combinations. It is also an object to describe the individual components of the cooperative combination and the relative proportions of the individual components in the combination. A further object of the present invention is to describe the insecticidal, control and acaricidal effects of the combination on agricultural pests. Other objects will become apparent from reading the following description of the present application.

The present invention consists of a combination of avermectin compounds and insect and mite metabolic inhibitors that have a synergistic effect when used to control or eliminate infestations in areas that are infested with domestic pests, but still in agricultural environments. . Tree brother
In the formula, n is ol or 1; 几 is hydrogen, α-L-oleandrosyl-α-L-oleandrosyloxy, and sono4''-IJ ester derivative; is hydrogen; a dashed line indicates a single bond or a double bond, but only when the dashed line indicates a single bond does it exist.

The insect metabolism inhibiting compounds constituting the second component of the synergistic combination of the present invention are piperonyl butoxide,
such as triphenyl phosphate.

When used as agricultural insecticides, avermectin compounds may contain 1 to 50 m of active compound per hectare.
Administer at a dosage rate of When insect metabolic inhibitors are used as agricultural insecticides, they should be administered at dosage rates of 1 to 2,500 g of active compound per hectare. l
Administer at a dosage rate of 0.000 ppm.

A synergistic effect of the combination of avermectin compounds and insect and mite metabolic inhibitors is observed resulting in a reduced dosage of one or both components. Furthermore, administering agricultural insecticides and acaricides in smaller amounts than usual results in a reduction in possible side effects and suppression of the development of resistance. Furthermore, what can be expected from considering the activity spectra of individual components has been expanded.
A spectrum of cooperative actions of agricultural pests and mites that can be successfully combated is observed. Thus, the possibility of combating agricultural pest and mite infestations in which the individual components were ineffective or only partially effective is realized with the synergistically acting combinations of the present invention.

An agricultural pest and mite invasion for which the cooperatively acting combination of the present invention is particularly effective is Leptinotarsadecemlineata (Leptinotarsadecemlineata).
beetles such as 5podoptera exigur, Plutella xylost
ella), Helioth
is virescens)
Homoptera such as Psillapyricola and Aphisg□5Sypj;
cbus urticae), Pa1onychus citri, Pbyllocoptivtao
leivora), Pblypbagotai sonemus 1a
tus) and other mites.

Pest invasions for which the cooperative combinations of the present invention are particularly effective include Diptera (flies); Hymenoptera (honey bees, wasps, ants, especially ants and small ants). ); mosquito;
Cockroaches; termites; wood pests such as gypsy moths, larvae of moths of the family Triticidae: and other household insect pests.

The synergistically acting combination of the present invention controls the above insect pests on economically useful crops such as cotton, citrus, deciduous fruits, soybeans, rice, grains, vegetables, and in ponds. It is useful for

When using the synergistic combinations of the present invention, the individual components may range from 1 part avermectin compound to 2500 parts insect metabolism inhibitor to 1 part avermectinized carcass to 1 part insect metabolism inhibitor. Used in a range of percentages up to.

Compositions exhibiting synergistic action are useful against insect and mite pests of stored grain and agricultural plants and the larval stages of insects growing in plant tissues. Compositions that exhibit synergistic action are also useful for the control of soil nematodes and soil-borne insect pests that are still of agricultural importance. When used to combat agricultural pests that harm crops while the crops are growing or in storage, the composition exhibiting a cooperative action provides protection against agricultural pests of growing plants; It is applied to the soil in which plants are grown and to stored grains using any conventional technique such as spraying, granules, powders, emulsions, etc.

The synergistically acting combination of the present invention has the added advantage that the avermectin compound has a long-term effect at very low doses and the piperonyl butoxide has a very fast-acting effect. Rapid control is achieved with piperonyl butoxide, which quickly reduces pest distribution, and long-term control is achieved with avermectin compounds, which prevent redistribution of insect pests and avoid the economic burden of reuse.

The synergistic combination of the present invention is very conveniently used as part of spray, bait, and powder formulations. Spray formulations may be aqueous or non-aqueous, in which the ingredients to be combined are dissolved or suspended. Emulsifying agents, suspending agents and other formulation aids can be included in the formulation as required. A variety of liquid formulations commonly used by those skilled in the art of pesticide spray formulations can be used. Compressed air, high-pressure airless spraying, nebulizer-type aerosol spraying, etc. can be used.Like aerosols, manual, human-powered or electrically driven spraying is suitable for home use, while gasoline-powered spraying or aerial spraying is more Commonly used for large-scale and commercial spraying, the spraying technique is suitable for insect pests, where direct spraying is desired where they feed or live. .

Other formulations suitable for such direct application are powder formulations that are spread over areas where insect pests feed, infest, or live. Combinations exhibiting synergistic action can be prepared in powder formulations by mixing and suspending substrates such as talc, starch, clay, kaolin, silica, bentonite, diatomaceous earth, etc. using techniques known to those skilled in the art. .

The synergistically acting combinations of the present invention can be formulated into baits that are advantageous in dealing with insects that remain in their nests, or that have nests in difficult locations. Bait formulations are particularly advantageous for avermectin compounds in view of their long-term activity and high efficacy, enhanced and assisted by the presence of piperonyl butoxide.

Bait formulations are prepared from animal or vegetable materials that are fed to insect pests. Sugar solutions used in liquid form or added 7111 to other substances are particularly useful. The addition of a synergistic combination to meat products, such as those prepared as pet food, provides a very useful feed formulation. Combinations exhibiting synergistic action can also be made into suspensions or solutions in vegetable oils such as soybean oil, sesame oil, cottonseed oil, etc., defatted soybean meal, citrus pulp (p
ulp), sugarcane pulp, etc., and can be formed into bait formulations in any size and shape.

Furthermore, in addition to the main ingredient, other ingredients such as bait, stabilizer, suspending agent, emulsifier, etc. can be included.

The active ingredients; 5: f'): Use-2 The amounts in the combinations shown may be varied to suit the particular use to which the preparation is applied5, but in general they exhibit a synergistic action. The combination formulation contains about 0% of the active ingredient in a concentrated liquid formulation for spraying, which is usually diluted with about 500 times the amount of water when spraying on plants.
．． Contains 01 to 5%. An exception to this is a technique known as ultra-low volume spraying, which uses solutions that are many times more concentrated. Powder formulations use about 0.01 to 25% of the active ingredient, and bait formulations use about 0.001 to 5% of the active ingredient. The active ingredients are present within the proportions stated above.

Specific formulations containing avermectin compounds and insect metabolic inhibitors that exhibit synergistic agricultural insecticidal and antiparasitic activity are listed below: Concentrate formulation for spraying: Avermectin B1 0.6% Piperonyl Butoxide 0.5% Propylene Glycol 86.2% The above concentrate is diluted with 400 times the amount of water to make the final spray.

Feed preparation: Avermectin Bl O, 1% biperonyl butobeef, 0.1% Suspend the two active ingredients in 10 times the amount of soybean oil to make a suspension of the active ingredients, then add this oil suspension to defatted soybean crude. Mix with flour to form a mixture containing 0.2% active ingredient and form into cube baits or other desired shapes.

Liquid formulation: wt% wt% avermectin Bla/B1 b (91%) 2.2
2.2 Piperonylbutoxito 10.0
20.0 Beef Shiren 75.8
65.8 total uio, o 1oo,.

Granule preparation 2 Weight% Weight% Avermectin: / B1 a/B1 b (91%) 0
．． 33 Dipiperonyl butoxide 1.5
0 6-00 Montmorillonite 92.1
7 87.67 Diethylene glycol 6.0
0 6.00 total i oo, oo too, o
.

Applicant: Merck End Company Incorporated 39

Claims (1)

[Claims] 1. Structural formula: [In the formula, n is 0 or 1; R1 is hydrogen, α-L-oleandrosyl-α-L-oleandrosyloxy, and its 4″-phosphorus An avermectin compound and an insect metabolic inhibitor, which is an acid ester derivative; 几 is hydrogen; the broken line indicates a single bond and also a double bond, but Jt2 exists only when the broken line indicates a single bond. A combination agent exhibiting a synergistic effect as an agricultural insecticide and control agent, characterized by comprising: 2,7 vermectin compound ?7II Ml (from 2500 parts of an insect metabolic inhibitor, 10
A synergistic combination according to claim 1, wherein each compound is present in a ratio of up to 0 parts to 1 part of the insect metabolic inhibitor. 3. The combination agent exhibiting synergistic action according to claim 1, wherein the insect metabolism inhibitor is piperonyl butoxide or triphenyl phosphate. 4. Inert carrier and structural formula: [In the formula, n is 0'! , or 1; cap is hydrogen, α-L-oleandrosyl-α-ly-oleandrosyloxy, and its 4"1-phosphate derivative; R is hydrogen; broken line indicates a single bond or a double bond, but is present only when the broken line indicates a single bond] An insecticide composition comprising an avermectin compound and piperonyl butoxide. 5. The composition is a liquid spray. The insecticidal composition according to claim 4, which is in the form of a powder, dust powder, or bait. 6. Applying the synergistic combination according to claim 1 to areas infested with pests. Z. A method of treating agricultural pest infestation comprising the use of: Z. A method of treating agricultural pest infestation comprising administering to an agricultural crop or commercial product infested with agricultural pests a combination agent exhibiting a synergistic action as claimed in claim 1. How to deal with it.