SU1037441A1 - 2/alpha-phenyl-alpha-(n-ethyl)-phenyl-acetyl/indandion-1,3 showing raticide activity - Google Patents

Abstract

2-Id-phenyl-o - (p-ethyl) -phenylacetyl / indandion-1, 3 of the formula O II i nbcH-c-GH "o C s S showing ratios activity (L

Description

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4 4 GBb 1/3 of the solution and maintain the reaction mass for 2 hours at a temperature of P5-120C. The resulting dark thick mass is cooled, 100 ml of 50% NaOH solution is added and the mixture is left to stand in the fridge. Kick during the day. Contaminated Na-salt is left, washed with benzene, dissolved in a small amount of hot ethyl alcohol, and acidified with diluted (1: 5) hydrochloric acid. The reddish brown oil is separated. The product is technical, contains 80% of the basic substance. The yield is 12.7 g (58%) .. g) Isolation of 2 - / (- phenyl-o - (petyl) -phenylacetyl / indanedione-1,3 in pure form. After , as from the reaction mass, when preparing the Na-salt (see preparation of the Na-salt in example c), 1/3 part of benzene is distilled off, water is added to the flask until complete dissolution of the Na-salt and heated to boiling. the organic layer is separated from the aqueous layer, the organic layer is washed with water and combined with the aqueous layer. The aqueous solution is acidified with diluted (1: 1) hydrochloric acid. Formation of toxicity studies 2- / s | C-Fensch for white rats and the muddy solution left for 10-12 hours in a cold place until the red-brown oil comes out and the solution is clear. The oil is separated, dissolved in ether, dried or MgSO4 , the ether is distilled off in vacuo, the residue — the red-brown oil is 2- / -phenyl- (at-ethyl) -phenylacetyl / idanedione, 1. The product is recrystallized from ice-acetic acid. mp. 180- 181 pp. Yield 2.5 g (11.4%). Identification was carried out according to elemental analysis and IR spectra. Elemental analysis: C Calculated,%: Found,%: G-spectra: 1500-1590 cm Benzene ring: carbonyl group 1695 cm, diketone form: 1705-1770 cm. The resulting substance was examined for ratid activity. A study of the toxicity and rodenticidal activity of the above compound on white rats and white mice was carried out, the results of the research are presented in .table. 1. That blitz-ethyl) -fesh-acetyl / 1 Shdandione-1,3

probe

Rats in the stomach through

probe 1.9

Rats in the stomach through

probe2,9

ABOUT

50

50

The test preparation was prepared in the form of an oil solution. The corresponding dose of the drug at the rate of 0.9, 1.9; 2.9; 3.4 and 3.9 µg / kg for rats and 1.8; 3.8; 5.8; 6.8 and 7.8 needles / kg for mice in sunflower oil were injected subcutaneously and into the stomach through a probe: in 0.5 ml mice and 1.0 ml rats.

The following materials indicate that LDUo of white rats is subcutaneous and when administered to the stomach through a probe was 2.4 mg / kg, and for white mice mg / kg.

Three - Fourfold feeding of a bait containing 0.00250, 005% and white rats and mice resulted in their 100% death within 3-6 days. The bait was eaten willingly, in the amount of 8–9 g / goal by the masses and 20–25 g / goal to the rats (in the control 6 g / goal and 20 g / goal, respectively. 1 The occurrence of a protective-reflex reaction in rodents was not observed.

Thus, the 2- / o-phenyl-o - (p-ethyl) -phenylacetyl / indanedione-1, 3 preparation has high rodenticide properties and can be successfully used in rodent control practices.

Results compared to phentolacin and difenacin are presented in

Table 2. I.

table 2

LD mg / kg

Title

(for gray

rats)

Difenacin8-9

Fentolacin4-5

2- / o; -phenyl-o (p-ethyl) -phenylacetyl / indandione1, 31.5-2

71037441 8

 It follows from Table 2 that toxicity is greater than that of difenation a and 2.5 times higher for rats 2- / o-phenyl-l :- (p-ethyl) -phenyl- than that of fentolacin while maintaining isacetyl / indanedione-1 , 3 to 4 times more, bi-selective action.

Claims (1)

2 - / </ -phenyl-o (- (p-ethyl) -phenylacetyl / indandion-1,3 formulas exhibiting ratidicidal activity. one