Tritium high-labeled [3h]-(e)-n-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methyl-6-noneneamide

FIELD: organic chemistry, analytical chemistry, bioorganic chemistry, biochemistry, applied medicine, labeled compounds.

SUBSTANCE: invention proposes labeled analogue of physiologically active compound, namely, tritium high-labeled [3H]-(E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methyl-6-noneneamide of the formula:

.

Invention provides expanding the assortment of labeled analogues of physiologically active compounds.

EFFECT: valuable properties of compounds.

1 ex

 

The invention relates to the field of organic chemistry and can find application in analytical chemistry, Bioorganic chemistry, biochemistry and applied medicine.

In the study of physiologically active compounds necessary for their labeled counterparts.

Known (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methyl-6-nonenamide formula:

This connection, which received the name of "capsaicin", is the strongest stimulus of nerve endings. For short term exposure causes selective degradation of peripheral nerve endings. Prolonged exposure leads to loss of sensitivity to various mechanical and chemical stimuli. It is also used for the clinical assessment of chronic post-herpetic neuralgia (G.Jancso et al. // Nature 1977. Vol.270. P 741).

However, tritium-labeled analogue not described.

It is known that substitution of atoms of compounds for their labeled counterparts does not change any properties of the original compound (E.A. Evans - Tritium and its compounds Butterworths, 1974, p.48).

The technical result achieved by the present invention, is expanding the range labeled analogs of the physiologically active compounds.

Achieved the specified technical result obtaining vysokobarnogo tritium [3H]-(E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-IU the Il-6-nonenamide formula:

The following is an example implementation of the invention.

Example.

In the first chamber of the reaction chamber ampoule was placed 30 mg of palladium oxide and 30 mg of 5% PdO/BaSO4in another 100 ál anti-lock brakes. dioxane, 10 μl of triethylamine and 5 mg of capsaicin. The second camera was frozen with liquid nitrogen, the vial was evacuated to a pressure of 0.1 PA and filled with gaseous tritium to pressure 333 hPa. Then, the first chamber was heated to 70°C. When the oxide of palladium was recovered tritium water was peremarazhival the second chamber. The reaction vial was evacuated to a pressure of 0.1 PA, and continuing to heat the first ampoule up to 70°With, filled with argon. Then the contents of the second chamber is transferred into the first chamber, which was sealed. Thus, the reaction mixture consisted of the recovered catalyst, 100% tritium water, triethylamine and a solution of capsaicin in dioxane. The contents of the ampoules were heated for 30 min at 145°under stirring. Then, the ampoule was opened, the reaction mixture was diluted with 0.5 ml ethyl acetate, the catalyst was separated by filtration and washed successively with ethyl acetate (3×0.5 ml) and methanol (3×0.5 ml). Tritium water, dioxane and triethylamine drove on the rotor. Labile tritium was removed, repeatedly dissolving the substance in methanol (5×2 ml) and pariva last (radioactiv the ity of the reaction mixture is 500 MCI).

Purification of labeled preparation was carried out by HPLC on a Kromasil 100 C187 µm (8×150 mm), v - 2 ml/min, the system Meon-water-acetic acid-TFA (65:35:0.1:0.01). Retention time was determined by the standard (radioactivity and radiochemical purity, respectively, was equal to 30 MCI, and 30%). A second purification was performed on a Kromasil 100 C87 µm (8×150 mm), v - 2 ml/min, the system Meon-water-acetic acid-TFA (60:40:0.1:0.01), retention time was determined by the standard (radioactivity and radiochemical purity, respectively, was equal to 23 MCI and 98%). The output labeled product after chromatography was 25-30%, molar radioactivity 7 CI/mmol.

Thus, the resulting new visokomernoe tritium physiologically active compound.

Viscometry tritium [3N]-(E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methyl-6-nonenamide formula



 

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