Spirodiclofen original drug feasibility analysis report

Spirodiclofen original drug feasibility analysis report

I. Background

Generations of mite damage occurs, the ability to propagate, in the appropriate temperature and humidity conditions, the number of mites multiply rapidly in a short time to grow and easy to acaricide resistance, fruit trees and other crops to cause harm. Keto esters quarter mite Bayer CropScience as a time-consuming than a decade developed a new mechanism of action of acaricides, the mites mechanism completely different from the various existing acaricides, mite damage can effectively improve the control effect.

Quarter of the new season are ketone keto esters mite acaricide class. Keto esters quarter mite mite body by inhibiting fat synthesis, destruction of energy metabolism mites, and ultimately kill the mites, it is a new, efficient handling of non-foliar miticide within the suction, and other existing Acaricide no cross resistance problem, a variety of different crops are good mite control efficacy and effectiveness of the excellent support, both to kill the eggs and kill the larva, is particularly suitable for production control of existing acaricides resistance to the harmful mites.

1.1 The name, type and molecular structure

Common name: Spirodiclofen

Name: mite crisis Envidor

Alias: mite more than Viagra

Active ingredients: Season keto esters Spirodiclofen mite

Product Type: Quarter keto class acaricide tetronic acid

CAS # :148477-71-8

Chemical name: 3 - (2,4 - dichlorophenyl) -2-- oxo -1-- oxa spiro [4,5] - decane -3-- en 4 - base 2,2 - dimethyl butyl

Molecular formula: C21H24Cl2O4

Molecular weight: 411.32

Structure:

1.2 The physical and chemical properties, toxicity and mode of action

Physical and chemical properties: Appearance white powder, no special smell, melting point: 94.8 ℃, 20 ℃ vapor pressure of 3 × 10-7Pa, 20 ℃ density 1.29g/cm3. Solubility (material / 1000ml solvent, 20 ℃): n-hexane, 20, dichloromethane> 250, isopropanol 47, xylene> 250, water 0.05.

Toxicity: Acute oral LD50> 2500mg/kg, acute dermal LD50> 4000mg/kg; sunfish LC50> 0.0455mg / L, rainbow trout LC50> 0.0351mg / L, daphnia LC50> 100mg / L. Bees LD50> 100μ g / bee only on North American quail LD50> 2000mg/kg.

Mode of action: a new mechanism, a contact action, with no suction. Mainly inhibit mite fat synthesis, blocking the energy metabolism of mites, mites are valid in all developmental stages, including eggs.

1.3 Features

1. The new structure, the unique mechanism of action: the active ingredient is a mite dangerous mite season ketone esters, mechanism of action is to inhibit the synthesis of fat in the body of harmful mites. It no cross-resistance between the current acaricides for acaricide used to control resistance to existing harmful mites.

2. Acaricidal broad spectrum, strong adaptability: risk of spider mites, yellow spiders, rust Pi lice, yellow tea mite, carmine spider mite and two spotted spider mite and so have a good control effect can be used for citrus, grapes and other fruit trees and eggplant, pepper, tomato and other Solanaceae crops mite damage control. In addition, the risk of Psylla mites, elm leafhopper class oyster Diaspididae and good to rid of pests such effect.

3. And kill immature eggs: Eggs exceptionally good results, while if the mites on the child have good contact action. Mite crisis although it can not kill the female mite faster, but the female mite have a good sterilization effect. Touch drug female mite eggs after the 96% can not be hatched, died late embryonic stage.

4. Persistence length: mite-risk persistence length, the production by 5,000 fold dilution to control the citrus red mite damage of 40 to 50 days. Wei Shi mite resistance after the crop leaves by rainfall, moderate rain event 2 hours after spraying does not affect the efficacy of normal play.

5. Low toxicity and residue, good security. Different temperature conditions in the very safe to crops, livestock and crops on the safety, low toxicity. For pollution-free production.

6. No cross resistance: with most of the pesticides (strong alkaline copper formulations of pesticides and other than me) is mixed with the active. Mix with the existing acaricides, mite can increase risk of quick result, and it helps victims of mite resistance management.

1.4 Application Methods

1. Uniform spray: the role of the product by contacting control mite eggs, young and female mite if the mites, with no suction, so when the pharmaceutical watered spray, spray evenly as possible to ensure the liquid spraying both sides of leaves and fruit to the surface, to maximize its efficacy.

2. Application of time: Control of citrus red mite, mite damage recommended pre-application in order to give full play to the characteristics of long persistence mite dangerous.

⑴ spring regimen 1:

When the red spider, yellow spider harm to control index (number of eggs per leaf or per leaf reached 10 nymphs 3-4 head), the use of mite crisis of 4000-5000 times (100 ml bottle of watered 800-1000 Jin) uniform spray to control red spider, yellow spider about 50 days. Since then, the case of spider, yellow spider insect population to rise again to a quick result with miticide (such as pyridaben, propargite, Avermectin, etc.) can be.

⑵ spring regimen 2:

Such as red spider, yellow spiders to control targets occurs earlier, the first use 1-2 times a quick result acaricides (eg, pyridaben, propargite, Avermectin, etc.), about the beginning of May, the use of mite crisis 400-5000 times (100 ml bottle of watered 800-1000 Jin) sprayed once to control red spider, yellow spider about 50 days.

⑶ Fall medication:

9,10 spider, yellow spider insect population control targets was achieved, the use of mite re-spraying crisis of 4000-5000 times a mite damage or under conditions mixed with other drugs, to control the citrus harvest, until the winter clearance Park.

3. Application number: crisis in the citrus mites during the growing season is best applied only once, and the other different acaricidal acaricide rotating mechanism, can effectively prevent and control resistance to mites, while reducing the risk arising mite mite resistance risk.

1.5 Notes

1. If the citrus red mite damage in the late stage, the number of adult mites damage is already quite large, due to risk killing mite eggs and young mites features, advice and quick result is good, a short residual effect of acaricides, such as Avi streptozotocin and other mixed use, both to quickly kill adult mites, mite insect population can control the number of long recovery.

2. Taking into account resistance management, it is recommended in a growing season (spring and autumn), mite-risk no more than twice the frequency of use.

3. Mites major role in crisis mode for the contact and stomach, without the suction, so spraying even want to spray the whole plant, especially the back.

4. Recommended to avoid the fruit trees blossom medication.

1.6 Prospects

As China's citrus production levels and increasing demand for food safety, orange farmers control pest mites on citrus requirements are increased accordingly. According to plant protection experts predict, some toxicity, poor security, high residual insecticide acaricide in the near future will be efficient, safety and environmental protection of new varieties gradually replaced. Mite crisis in China in 2004 to obtain temporary registration in Citrus (Registration No: LS20042173), then in the south of the citrus areas in 8 provinces spent 18 points in the demonstration test, the results proved it Panonychus citri excellent control effect. Crisis started in 2005, domestic sales mites, some citrus growers try to use the mite crisis, it was generally reflect its control effect is good, the persistence of long. Quarter of the market prospects of keto esters mites can be expected, species of mite acaricide replacement risk in the process of miticide may develop into an important citrus varieties.

II. Feasibility Analysis Process:

The product has completed a small pilot process, the product of the total five-step synthesis reaction, the yield of each step is greater than 85%, product content over 95%, synthetic raw material costs less than 30 yuan / ton.

The product is one of Bayer's fifth major product, the global sales of about 1 billion U.S. dollars. The product is not in China because of various reasons the patent. Bayer in China in 2006 began to promote this product in 2006 sales of about 5,000 yuan. Spirodiclofen 24% (mite crisis) price is 60 yuan / ton. 2007 sales in China reached 100 million yuan or so.