α-hederin uniformly marked with tritium

FIELD: medicine; pharmacology.

SUBSTANCE: new described α-hederin of formula: uniformly marked with tritium is actually analog of α-hederin - biologically active saponin.

EFFECT: new effective biological properties.

1 cl, 1 ex

 

The invention relates to the field of organic chemistry and can find application in analytical chemistry and biological research.

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

It is known that replacement of hydrogen atoms in organic compounds on their isotopes does not change any properties of the original compound (E.A. Evans - Tritium and its compounds London Butterworths, 1974, p.48) [1].

Famous α-hedelin formula

This connection is one of the most intensively studied of saponin (Merck No. 4655, 1999) (Tschesche et al. Z.Naturforsch. 20b, 708, 1965) [2].

However, tritium-labeled analogue not described.

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 renominating tritium α-khadarina formula

The following is an example implementation of the invention.

Example 1.

A solution of 11 mg α-khadarina in 0.8 ml of methanol was added to 110 mg of Lindlar catalyst (Fluka), methanol was removed by evaporation on a rotary evaporator, and then for a more uniform distribution of matter on the catalyst was again added 0.4 ml of methanol. The methanol was removed by evaporation to Roto the nom evaporator and the residue liofilizirovanny. An aliquot of the dry mixture (66 mg) was transferred to the reaction vial. 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 235°10 minutes the Excess gaseous tritium was removed by vacuum. The substance of the catalyst was extracted with methanol (5×2 ml) and was separated by filtration. Labile tritium was removed several times, dissolving the substance in methanol (5×2 ml) and pariva last. The radioactivity of the selected product is about 350 MCI, in the sought compound contains 3 % of the tritium label, the chemical yield of 35%. After two HPLC (Kromasil 8×150 mm, gradient of 75% methanol with 0.1% acetic acid to pure methanol for 30 min) allocated 6.75 MCI of labeled product with a radiochemical purity of 98% (analytical chromatography on a column Kromasil C187 μm, 4.6×150 mm, 60% Meon - ammonium phosphate buffer, pH 2.8, a flow rate of 1.0 ml/min, retention time - 7.48 min), the output is 29%, the molar radioactivity - 2.9 CI/mmol.

Thus, the resulting new ravnomernoto tritium connection.

Ravnomernijeg tritium α-hedelin formula:



 

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