[3h]-fluvastatin highly labeled with tritium

FIELD: organic chemistry, labeled compounds, pharmacy.

SUBSTANCE: invention relates to a novel [3H]-fluvastatin of the formula: highly labeled with tritium with molar radioactivity 40-45 Ci/mmole. This compound can be used in analytical chemistry, biochemistry and applied medicine.

EFFECT: valuable properties of compound.

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.

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 London Butterworths, 1974, p.48).

Known [R*,S*-(E)]-(±)-7-[3-(4-forefeel)-1-(1-methylethyl)-1H-indol-2-yl] - for 3,5-dihydroxy-6-geptanona acid of the formula:

This connection, which received the name "fluvastatin", is a strong inhibitor of the reductase (E.Leitersdorfet at., Eur.J.Clin.Pharmacol. 1993. Vol.45. 513 [1].

Known tritium-labeled analogue of fluvastatin, containing the label in anthopology relative to the fluorine atom in tortenelem the Deputy (Database REGISTRY on STN, No. 776261-24-6 from 08.11.2004) [2].

However, the molar radioactivity of this known connection low.

The technical result achieved by the present invention, is expanding the range labeled analogs of the physiologically active compounds, increasing the molar radioactivity of the target product.

Achieved the specified technical result obtaining vysokobarnogo tritium [3N]-fluvastatin formula:

with molar radioactivity 40-45 CI/mmol.

The following is an example implementation of the invention.

Example I.

A solution of 4 mg of fluvastatin in 0.1 ml of methanol was added to 100 mg of Lindlar catalyst 6% Pd/BaSO4The methanol was removed by evaporation on a rotary evaporator and liofilizirovanny. The catalyst is coated with a substance transferred to the reaction vial. The analysis showed that the catalyst was adsorbirovannoi 3.5 mg of fluvastatin. Then the ampoule was evacuated to a pressure of 0.1 PA, filled with gaseous tritium to pressure 333 hPa and kept at a temperature of 180°With 6 minutes the Excess gaseous tritium was removed by vacuum. Obtained [3N]-fluvastatin were extracted from the catalyst with methanol (5×2 ml) and was separated by filtration. Labile tritium was removed, repeatedly dissolving the substance in methanol (5×2 ml) and pariva last.

Purification of [3H]-fluvastatin was performed by HPLC on a column: Kromasil 100S 18, 7 μm, 8·150, eluent - 75% Meon+0.1% Asón, 2 ml/min retention time - 7.83 min Output labeled drug - 15-20%, molar radioactivity - 40-45 CI/mmol, radiochemical purity 98-99%.

Obtained [3H]-fluvastatin kept in ethanol solution, which the water-methanol fraction was diluted with water 2 times, put on the cartridge Sep-Pack C18, washed with water and blotted out the desired product ethanol.

The thus obtained new visokomernoe tritium physiologically active compound with a high molar radioactivity.

Viscometry tritium [3H]-fluvastatin formula:

with molar radioactivity 40-45 CI/mmol.



 

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