1,1'-(hinzelin-2,4-diyl)bis(pyridine)diperchlorate with depolymerase activity

 

(57) Abstract:

Use of invention: as a cotton defoliant. The inventive product - 1.1 - (hinzelin-2,4-diyl)bis(pyridine)diperchlorate f - ly indicated in the text of the description, C18H14Cl2N4O8exit 97% . Reagent 1: 1.1 - (hinzelin-2,4-diyl)bis(pyridine)diperchlorate. Reagent 2: 42% HClO4. Reaction conditions: water environment. 5 table.

The invention relates to derivatives of 2,4-bis-(pyridine)hintline, which can find application in agriculture for cotton defoliation.

Inorganic defoliants, such as chlorates of sodium and magnesium, chlorate-chloride of calcium, calcium cyanamide and other trubolt the use of high doses of 5-50 kg/ha, which is associated with environmental pollution and high transport costs.

The activity of Droppa strongly depends on the air temperature, which is a factor limiting its use. It is found that high delirously effect drop shows when daily temperatures 22-24aboutAt 20-18aboutIts activity is reduced by 20-30% , and at temperatures below 18aboutWith this defoliant almost unusable insulina, in particular 1,1'-(2,4-chinazolinei)bis(pyridine)dichloride: 1,1'- (7-chlorination-2,4-diyl)bis(pyridine)dichloride: 1-(2,6 - dechlorination-4-yl)pyridinethione and 1-(2-chlorination-4-yl)pyridinethione, as cotton defoliants [2] .

Connection effective dose of 0.1-2 kg/ha of nutrient content

However, their disadvantage is the low stability due to hygroscopicity and volatility at elevated temperatures.

The aim of the invention is to increase the stability of defoliants on the basis of derivatives of 4-pyridinediamine.

The purpose of the invention is achieved by a new derivative of 4-pyridinediamine, namely: 1,1'-(hinzelin-2,4-diyl)bis(pyridine)diperchlorate formula:

The proposed connection depolymerase activity is not inferior to the famous, but far exceeds their consumer qualities-stability to water, temperature, stability during storage.

Comparison of the stability of the proposed connection I have had with 1,1'-(2,4-chinazolinei)bis(pyridine)dichloride (compound II).

P R I m e R 1. The determination of the stability of substances during storage in air.

0.5 g of diperchlorate and dichloride 1,1'-(2,4-chinazolinei)bis(pyridi who have the appearance of the samples and their IR spectra.

The results of the tests are presented in table. 1.

P R I m m e R 2. Determination of the hydrolytic stability of the substances. 0.5 g of the dichloride and diperchlorate 1,1-(2,4-hinata - Linder)bis(pyridine) are placed in 10 ml of water, boil for 30 min, the precipitate is filtered off and determine the quality of the connection by comparing the IR spectra before and after heating in water. Range of diperchlorate not changed, but in the spectrum dichloride bar appears, corresponding to the group C= O (C=O1680 cm-1).

P R I m e R 3. Determination of thermal stability of substances.

Determination of thermal stability of the compounds was carried out on derivatograph in the temperature range from 20 to 250aboutC.

The results of the tests are presented in table. 2.

From the test results of the proposed and known compounds can be seen that the known connection dichloride 1,1-(hinzelin-2,3-diyl)bis(pyridinium) is subjected to hydrolysis in the presence of water (appearance in the infrared spectrum bands characteristic of C= O group) and decomposition at elevated temperatures, which makes it difficult to manufacture and practical application.

The method of obtaining the proposed connection lies in the interaction of 1,1'-(hinzelin-2,4-diyl)bis(pyridine the thief 2 g (0,0056 mol) of 1,1'-(hinzelin-2,4-diyl)bis(pyridine)dichloride in 20 ml of water with stirring, add 1.3 ml (0,0056 mol) 42% perchloric acid, the precipitation is filtered off, washed, air-dried and gain of 1.93 g (97% of theory. ) 1,1'-(hinzelin-2,4-diyl)bis(pyridine) diperchlorate. Calculated, % : C 44,62: H 2, 89: N 11,57. C18H14Cl2N4O8. Found, % : C 44,84: H 2,63: N 11,42. The IR spectrum contains the characteristic bands: 1100 cm-1(ClO4-), 1620 cm-1(C= N).

P R I m e R 5. Comparative tests of the proposed compound I and the known compound (II - 1,1'-(hinzelin-2,4-diyl)bis(pyridine)dichloride carried out on the plants of cotton Gossypium hirsufum, grade 108-f) in a climatic chamber. Illumination in the chamber 8 thousand Lux. the duration of the photoperiod 16 h, temperature day 28aboutWith night 22aboutC. the age of the plants of cotton at the time of processing 3 weeks.

Aqueous suspension of the test substances applied to the surface of the leaves by spraying. Compounds of experience in the concentration of 0.1 and 0.3% . The experience carried out in triplicate (one repetition 4 plants). The results of the actions of the test compounds is evaluated by counting the number of fallen leaves after 7 and 10 days after treatment.

The results are shown in table. 3.

According to the data obtained new defoliant not inferior to nick varieties 6425, grown by the conventional technology at the site Yangiyul basic laboratory (Tashkent region ), in the period of the opening in the middle on one of the boxes on the hive. Processing of data was performed with 0.1 and 0.3% aqueous suspensions using a handheld sprayer. The rate of fluid flow 1000 l/ha, repeated 4 times. The plot size 1 m2. Reference defoliant - a 0.6% aqueous solution of chlorate magnesium.

The data obtained indicate that compound I at a concentration of 0.3% causes the same defoliation of plants, such as magnesium chlorate in a concentration of 0.6% , much activity is superior to the reference drug.

The results are shown in table. 4.

P R I m e R 7. Field test connection I conducted on cotton varieties With-4880. The spot test, the conditions for growing plants and methods the experiment described in example 6.

The connection I have at concentrations of 0.1 and 0.3% . Standard magnesium chlorate in a concentration of 0.6% .

The results of the tests are presented in table. 5.

Based on the presented results, the effective concentration of compound I at this grade cotton is the concentration of 0.1% . Defoliaria the potency of the compound in the ed which are widely used by defoliant-chlorate magnesium is also manifested in the fact, the proposed connection I caused the fall nepotroshenyh or malopocetnych leaves that fell, not lingering on the box, and accordingly did not litter the fiber when cleaning. In plants treated with chlorate magnesium, leaves falling off dry, this way of action is inevitably a strong contamination of the fiber.

Thus, the obtained results show that the proposed in the invention of new defoliants are not inferior to the previously known defoliants and far surpass them in their operational properties-stability to water, stability during storage and nasleduemoe. (56) Nuridjanyan K. A. and other Chemistry and application of desiccants and defoliants. Survey information. Series: Chemical plant protection, Ed. Niitekhim, M. , 1989.

U.S. patent N 4502880, class C 07 D 401/14, 1985.

1,1'-(hinzelin-2,4-diyl)bis(pyridine)diperchlorate formula:

< / BR>
with depolymerase activity.

 

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EFFECT: valuable medicinal properties of compound and composition.

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15 cl, 57 ex

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to new compounds of the general formula (I) in racemic form, enantiomer form or in any combinations of these forms possessing affinity to somatostatin receptors. In the general formula (I): R1 means phenyl; R2 means hydrogen atom (H) or -(CH2)p-Z3 or one of the following radicals: and Z3 means (C3-C8)-cycloalkyl, possibly substituted carbocyclic or heterocyclic aryl wherein carbocyclic aryl is chosen from phenyl, naphthyl and fluorenyl being it can be substituted, and heterocyclic aryl is chosen from indolyl, thienyl, thiazolyl, carbazolyl, or radicals of the formulae and and it can be substituted with one or some substitutes, or also radical of the formula: R4 means -(CH2)p-Z4 or wherein Z4 means amino-group, (C1-C12)-alkyl, (C3-C8)-cycloalkyl substituted with -CH2-NH-C(O)O-(C1-C6)-alkyl, radical (C1-C6)-alkylamino-, N,N-di-(C1-C12)-alkylamino-, amino-(C3-C6)-cycloalkyl, amino-(C1-C6)-alkyl-(C3-C6)-cycloalkyl-(C1-C6)-alkyl, (C1-C12)-alkoxy-, (C1-C12)-alkenyl, -NH-C(O)O-(C1-C6)-alkyl, possibly substituted carbocyclic or heterocyclic aryl; p = 0 or a whole number from 1 to 6 if it presents; q = a whole number from 1 to 5 if it presents; X means oxygen (O) or sulfur (S) atom n = 0 or 1. Also, invention relates to methods for preparing compounds of the general formula (I), intermediate compounds and a pharmaceutical composition. Proposed compounds can be used in treatment of pathological states or diseases, for example, acromegaly, hypophysis adenomas, Cushing's syndrome and others.

EFFECT: improved preparing method, valuable medicinal properties of compounds and composition.

11 cl, 2 tbl

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