JP5733810B2 - Mosquito coil for infectious disease control mosquito control - Google Patents

Description

The present invention relates to a mosquito coil for controlling infection-borne mosquitoes.

There are many types of mosquitoes in the world that not only bite and suck blood, but also cause serious damage through infection. For example, the following relationships are known for several infectious diseases and the types of mosquitoes that carry them.
Malaria: Anopheles dirus, A. minimus, A. gambiae, A. sinensis
・ Dengue fever: Aedes aegypti, Aedes aegypti,
・ Yellow fever: Aedes aegypti
• Filariasis: Attached squid, squid, chikaeka,
・ Japanese encephalitis: Culex mosquito,
・ West Nile fever: 30-40 kinds such as squid and yabuka,
Chikungunya: Aedes aegypti, Aedes aegypti.
The best way to protect yourself from these infections is to avoid being stabbed by mosquitoes today, where there is no appropriate vaccine, and the use of mosquito coils is the best choice, especially in open houses. Although mosquito nets impregnated with pyrethroids are also used, there are many problems in usability, such as being usable only while sleeping and being hot in mosquito nets.
In this situation, supplying mosquito coils with excellent effects on Aedes aegypti, Aedes albopictus, etc. and low manufacturing costs is extremely important in protecting tropical inhabitants from Southeast Asia, Africa, etc. from infectious diseases. It is an effective countermeasure.

Until now, allethrins of pyrethroid insecticidal ingredients have been used worldwide as active ingredients of mosquito coils, but recently, the effects of allethrins on the main species of Aedes mosquitoes have been partly in Southeast Asia. There is a report that it has fallen, and there is interest in dealing with it.
In recent years, the development of new insecticidal components has also been promoted. For example, according to the literature [Biosci. Biotechnol. Biochem., 68 (1) 170, 2004] (Non-patent Document 1), a novel pyrethroid insecticidal component, metfluthrin [4- Mosquito coils containing methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2-dimethyl-3- (1-propenyl) cyclopropanecarboxylate] It has been reported that at a concentration of 1/40 to 1/20, a knockdown effect almost equivalent to that of d-alleslin mosquito coil was shown. However, metofluthrin has a difficulty in that it cannot be supplied at low cost when it is attempted to obtain a mosquito coil incense that is complicated in synthesis and high in production cost and has several times higher insecticidal efficacy than d-areslin mosquito coil.

The present inventors first focused on 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2,3,3-tetramethylcyclopropanecarboxylate as an active ingredient of a mosquito coil. As an efficacy enhancer, N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide [hereinafter referred to as efficacy enhancer A] is effective. By blending 0.1 times or more, preferably 2.0 to 5.0 times the amount of the ingredients, it is effective for Aedes aegypti, Aedes mosquito, etc. It has been disclosed (Patent Document 1).
Furthermore, the present inventors used (S) -2-methyl-4-oxo-3- (2-propynyl) -2-cyclopentenyl (1R) -trans-chrysantemate as an active ingredient, and the active ingredient It was found that mosquito coil incense containing 1.0 to 5.0 times the potency enhancer A with respect to the amount was also extremely effective for Aedes aegypti, Aedes squid, etc., and obtained a patent (Patent Document 2). .

The present inventors tried to apply the knowledge obtained in Patent Document 1 and Patent Document 2 to the above-mentioned novel pyrethroid insecticidal component Metofluthrin, and added a potentiator A 1.0 to the practical concentration of Metofluthrin. A mosquito coil with a blending amount of ˜5.0 times was prepared and examined for insecticidal efficacy against Aedes aegypti and Aedes albopictus, but satisfactory insecticidal efficacy was not obtained unexpectedly.
In such a situation, even if the chemical structure of the active ingredient due to pyrethroid is similar, it is impossible to analogize the insecticidal effect obtained by the addition of the efficacy enhancer A. The findings based on the above 2 show that it is not always valid for metfluthrin.
In addition, even if the potency enhancer A is generally applied to other pyrethroids having a chemical structure similar to those of the active ingredients of Patent Documents 1 and 2, the same effect can be obtained qualitatively or quantitatively. What is not obtained is as described later in comparative experimental examples corresponding to the respective examples.
Japanese Patent No. 3926836 Japanese Patent No. 4127721 Biosci. Biotechnol. Biochem., 68 (1) 170, 2004

The present invention is a mosquito coil containing metofluthrin, which is effective for infectious disease mosquitoes such as Aedes aegypti and Aedes aegypti, can be manufactured at low cost, and has excellent safety for human livestock, and for controlling infectious disease mosquitoes The challenge is to provide mosquito coils.

In order to solve the above problems, the present invention employs the following configuration.
(1) Methofluthrin [4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2-dimethyl-3- (1-propenyl) -cyclopropanecarboxylate] as an active ingredient is 0.0075-0. 0.02 to 0 % by mass of N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide as a potency enhancer. Mosquito for controlling infection-borne mosquitoes, characterized in that it is contained in an amount of 5% by mass and the content of the potentiating agent is 8 times or more and 40 times or less that of the active ingredient Tori Incense.
(2) The mosquito coil for controlling infection-borne mosquitoes according to (1), wherein the content of metfurthrin is 0.01 to 0.02% by mass.

The mosquito coil for controlling infection vector mosquitoes according to the present invention is based on the synergistic effect of metfurthrin and the above-mentioned potency enhancer A, exhibits excellent effects on infection vector mosquitoes such as Aedes aegypti and Aedes aegypti, and can be manufactured at low cost. Since it is excellent in safety against livestock, its practicality is extremely high.

The active ingredient used in the mosquito coil for controlling infection vector mosquitoes of the present invention is metfurthrin [4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2-dimethyl-3- (1-propenyl). ) -Cyclopropanecarboxylate].
This compound is already known by reacting the cyclopropanecarboxylic acid or a reactive derivative thereof with 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl alcohol or a reactive derivative thereof. Can be prepared.
Examples of the reactive derivative of carboxylic acid include acid halides, acid anhydrides, carboxylic acid lower alkyl esters, alkali metal salts, and salts with organic tertiary bases. On the other hand, examples of the reactive derivative of alcohol include chloride, bromide, and p-toluenesulfonic acid ester. The reaction is carried out in a suitable solvent, if necessary, in the presence of an organic or inorganic base or acid as a deoxidizing agent or catalyst as necessary.

Metofluthrin is liquid at room temperature and is generally easily dissolved in organic solvents. However, it is mixed with mosquito strips such as wood powder and mosquito-repellent mosquito repellents according to the present invention. Make up an incense stick.
The active ingredient content in the mosquito coil is set to 0.0075 to 0.02 % by mass, preferably 0.01 to 0.02 % by mass in consideration of the insecticidal efficacy against various infectious disease vector mosquitoes and the economy. The

The mosquito coil for controlling infection-borne mosquitoes of the present invention has N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide ( the enhancer a), containing 0.08 to 0.5 wt%, and compared to the amount of content the active ingredient of the enhancer state, and are more than eight times, and 40 times or less Oh, wherein the Rukoto.

Conventionally, in various preparations, piperonyl butoxide, N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide (efficacy enhancer A), N Synergists for pyrethroids such as-(2-ethylhexyl) -1-isopropyl-4-methylbicyclo [2,2,2] -oct-5-ene-2,3-dicarboximide and octachlorodipropyl ether; Mixing has often been done.
That is, when the above-mentioned synergist for pyrethroid is used for, for example, a liquid or a powder, it does not exhibit biological activity by itself, but is known to enhance the efficacy of pyrethroid when mixed with pyrethroid. There are many reports on the mechanism of synergists. For example, the body itself undergoes metabolic degradation to inhibit the oxidative detoxification metabolism of pyrethroids, or promote the penetration of pyrethroids into the skin, acting on the nervous system. It is known to increase the insecticidal efficacy of pyrethroids by making it easy to reach the point. However, the mechanism of action of such a synergist depends naturally on the type of insect, and the synergistic effect of the synergist is generally only about 10 to 20%.

On the other hand, as disclosed in Patent Document 1 and Patent Document 2, the present inventors have used 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2 as an active ingredient of a mosquito coil. , 3,3-tetramethylcyclopropanecarboxylate and (S) -2-methyl-4-oxo-3- (2-propynyl) -2-cyclopentenyl (1R) -trans-chrysanthemate It has been found that the efficacy enhancer A is compounded several times to 5.0 times the amount of the active ingredient, thereby exhibiting an excellent effect on Aedes aegypti, Aedes squid, and the like. This fact cannot be explained only by the mechanism of the synergist conventionally used in pyrethroid preparations, that is, the insect physiological mechanism described above. As another cause, a certain substance contributes to an increase in the volatilization rate of the active ingredient and the active ingredient. It was thought that the physical action also contributed, such as raising the concentration in the air and promoting the diffusion of the volatilized active ingredient.

Next, the present inventors tried to apply the knowledge obtained in Patent Document 1 and Patent Document 2 to the above-described novel pyrethroid insecticidal component Metofluthrin, and to add efficacy enhancer A to the practical concentration of Metofluthrin. Mosquito coils with 1.0 to 5.0 times the amount were prepared and examined for insecticidal efficacy against Aedes aegypti and Aedes aegypti, but satisfactory insecticidal efficacy could not be obtained contrary to expectations.

Therefore, the present inventors consider that when the active ingredient is metfluthrin, not only the quantitative ratio to metfluthrin but also the absolute amount thereof is important for the necessary amount of the efficacy enhancer A. Various intensive tests were carried out at 5% by mass and 8 times to 40 times the amount of metfurthrin.
As a result, it has been clarified that the combination of metofluthrin and the efficacy enhancer A shows a remarkable efficacy enhancing effect in a blending range different from Patent Literature 1 and Patent Literature 2, and the present invention has been completed. There are Exo type and Endo type based on the three-dimensional structure of the potency enhancer A, but the Exo type ratio is 30% or more, and the Endo type ratio is 70% or less in terms of the potency enhancing effect. Is preferred.

As an embodiment of the present invention, in addition to the efficacy enhancer A, a lower alkylamine salt of alkylbenzene sulfonic acid may be further blended as an adjunct to the efficacy enhancing agent. Here, the alkyl group of the alkylbenzene sulfonic acid is preferably about C _{8 to} C ₁₄ , while the lower alkyl group of the alkyl amine salt is preferably about C _{2 to} C ₄ , for example, dodecyl benzene sulfonic acid isopropylamine salt or dodecyl benzene sulfonic acid. A typical example is an ethylamine salt.
The ratio of the alkylbenzenesulfonic acid lower alkylamine salt to the efficacy enhancer A is suitably in the range of 0.2 to 1.0 times.

As mosquito coils, there are flame retardants and binders. The former includes plant powders such as wood powder, pesticide extracted chrysanthemum powder, citrus skin powder, coconut shell powder, charcoal powder, bare ash, etc. Carbon powder. Examples of the latter binder include tab powder, starch, methyl cellulose, carboxymethyl cellulose and the like.

The mosquito coil for controlling infectious disease-mediated mosquitoes of the present invention may contain a dye, an antiseptic, a stabilizer and the like, if necessary. Examples of the pigment include organic dyes such as malachite green, and typical examples of the preservative include acids such as sorbic acid, dehydroacetic acid, p-hydroxybenzoic acid, and salts thereof. Examples of the stabilizer include 2,6-di-tertiarybutyl-4-methylphenol (BHT) and 2,2′-methylenebis (4-ethyl-6-tertiarybutylphenol), but are not limited thereto. Not.

Furthermore, other insecticides and insect repellent components such as pyrethrin, allethrin, praretrin, framethrin, transfluthrin, empentrin, 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl, unless the purpose of the present invention is disturbed. Multipurpose composition with excellent efficacy by mixing conventional pyrethroid insecticides such as 2,2,3,3-tetramethylcyclopropanecarboxylate, fungicides, antibacterial agents, repellents, fragrances, deodorants, etc. You can also get things.

In preparing the mosquito coil for controlling infection vector mosquitoes of the present invention, any special technique is not required and a known production method can be adopted. For example, premix powder (containing active ingredients and potency enhancer in part of the flame retardant) and the remaining mosquito coil base material are mixed with water and then kneaded, followed by an extruder After molding with a punching machine, it can be dried to produce a mosquito coil. Further, after molding using only the mosquito coil incense base material, a liquid agent containing an active ingredient or the like may be sprayed or applied thereto.

The mosquito coil for controlling infection vector mosquitoes of the present invention is particularly effective for infection vector mosquitoes such as Aedes aegypti, Aedes aegypti, Anopheles, Aedes albopictus, Culex, but of course other mosquitoes and flies, It is also effective against various pests such as cockroaches and sanitary pests such as indoor dust mites, and its practicality is extremely high.

Next, the specific significance of the mosquito coil for controlling infection vector mosquitoes of the present invention will be clarified based on each example, and the technical position of the present invention will be clarified by comparative experimental examples.

Methofluthrin (0.015 parts) and potency enhancer A (0.2 parts) are uniformly mixed with 99.785 parts of a mosquito coiled incense base such as pesticide extracted chrysanthemum powder, wood powder, starch, etc., followed by pigment and preservative The mosquito coil for controlling infection vector mosquitoes of the present invention was obtained by a known method.

Metofluthrin (0.02 parts), potency enhancer A (0.16 parts), 0.08 parts dodecylbenzenesulfonic acid isopropylamine salt, and 0.1 parts 2,6-di-tert-butyl-4-methylphenol Is uniformly mixed with 99.64 parts of mosquito coils such as coconut shell powder, wood powder, tab powder and starch, and then water containing an antiseptic is added thereto. A mosquito coil was obtained.

[Practical efficacy test compared with d-alleslin in a room of 25 m ³ ]
Aedes aegypti were collected from various places where dengue fever developed in Thailand and were subjected to field efficacy tests after successive breeding. After releasing 100 female adults of the test Aedes aegypti in a room of 25 m ^{3 which} was closed, a test mosquito coil (prepared according to Example 1) was placed in the center of the room. 2 hours exposed, counted Aedes aegypti females dropped Osshaten with time was shown in Table 1 was determined the KT ₅₀ values.

・Ｐ地区： Uttaradit 地区
・Ｑ地区： Songkla 地区

・ P district: Uttaradit district ・ Q district: Songkla district

As a result of the test, 0.0075 to 0.02 % by mass of metfurthrin was contained, and the potency enhancer A was added to 0.08 to 0.5 % by mass and more than 8 times the amount of the active ingredient. The mosquito coil of the present invention has a knockdown effect of about 1.5 times or more enhanced by the KT ₅₀ value index as compared to methoflutrin alone incense at the same concentration (this point is, for example, 0.02% by mass of metfurthrin) In this case, it is also clear from the fact that the KT ₅₀ value is 113 / 77≈1.5 when the efficacy enhancer A is not blended and when the 8 times to 40 times amount is not blended. ). In particular, for the P-zone collected colonies and BS colonies where the sensitivity to pyrethroid insecticidal components is reduced and no effect is observed with d-arethrin 0.5% incense, only the mosquito coil of the present invention has a KT ₅₀ value. Showed a practical knockdown effect of 100 minutes or less, and was found to be extremely effective in controlling Aedes aegypti against infection vector mosquitoes.
Moreover, the incense in which the compounding amount of the efficacy enhancer A with respect to methfluthrin is 2 to 4 times is less effective than the single incense of the same concentration of metofluthrin alone, and the active ingredient is 4-methoxymethyl-2,3,5, Patent Document 1 of 6-tetrafluorobenzyl 2,2,3,3-tetramethylcyclopropanecarboxylate and (S) -2-methyl-4-oxo-3- (2-propynyl) -2- A tendency completely different from the case of Patent Document 2 of cyclopentenyl (1R) -trans-chrysanthemate was shown.

[Contrast field efficacy testing with other pyrethroids in the 25m ³ of the room]
As an active ingredient, metfurflurin and transfluthrin [2,3,5,6-tetrafluorobenzyl 2,2-dimethyl-3- (2,2-dichlorovinyl) -cyclopropanecarboxy, in which both alcohol moieties are benzyl derivatives Rate], permethrin [3-phenoxybenzyl 2,2-dimethyl-3- (2,2-dichlorovinyl) -cyclopropanecarboxylate], and phenothrin [3-phenoxybenzyl 2,2-dimethyl-3- (2- Methyl-1-propenyl) -cyclopropanecarboxylate] was prepared, and an experiment similar to that of Example 3 was performed using Culex mosquito instead of Aedes aegypti. That is, after releasing 100 female female testicular mosquitoes in a closed 25 m ³ room, an ignited test mosquito coil was placed in the center of the room. Table 2 shows the KT ₅₀ values obtained by counting the female mosquitoes that had been exposed for 2 hours and fell and turned over with the passage of time.

The results of the test, if the active ingredient is metofluthrin, similar to the Aedes aegypti Example 3, for the Culex, evident in both the KT ₅₀ values and lethality by 8 times blended enhancer A to the active ingredient A potent potency enhancing effect was observed. On the other hand, in the case of transfluthrin, permethrin, and phenothrin, even if the compounding amount of efficacy enhancer A was doubled or multiplied by 8, no efficacy enhancing effect was observed. Although the experiment was conducted on a Culex mosquito, if the results of Example 3 were also taken into account, it was confirmed that the effect of the potency enhancer A was common to other infectious disease-borne mosquitoes such as Aedes aegypti and Aedes aegypti. And the effect by the compounding of the efficacy enhancer A can never be inferred from the commonality of the chemical structural formula, and the technical value focusing on the combination of methfluthrin and the efficacy enhancer A, and further usefulness is supported. It will be.

INDUSTRIAL APPLICABILITY The present invention can be used in the field of manufacturing and selling mosquito coils, particularly mosquito coils for controlling infection-borne mosquitoes.

Claims (2)

0.0075-0.02 mass of metfurthrin [4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2-dimethyl-3- (1-propenyl) -cyclopropanecarboxylate] as an active ingredient % N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide as an efficacy enhancer, 0.08 to 0.5 mass A mosquito coil for controlling infectious disease mosquitoes, characterized in that it is 8% or more and 40 times or less the content of the active ingredient, compared with the content of the active ingredient.   The mosquito coil for controlling infection-borne mosquitoes according to claim 1, wherein the content of metfurthrin is 0.01 to 0.02% by mass.