D-1-phenyl-2-metilaminopropanola-1,5,6,7-trioxifene-7-0--d-glucuronide possessing antioxidant and vasodilator activity

 

(57) Abstract:

Usage: as an antioxidant and vasodilator drug. The inventive product D-1-phenyl-2-methylaminopropane-1-5,6,7-trioxifene-7-o - b-D-glucuronide. Yield 78%. BF C31H32NO7so pl. 134 to 140C. Reagent 1: pseudoephedrine base. Reagent 2: baicalin(trioxypurine). Reaction conditions: heating at 85C. table 2.

The invention relates to new chemical compound, specifically to D-1-phenyl-2-metilaminopropanola-1,5,6,7-trick - sillavan-7-0--D-glucuronidase possessing antioxidant and vasodilator activity (bicarinata pseudoephedrine) having the following structural formula

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Arsenal domestic medicines antioxidant and vasodilator actions is small, so the search among the different classes of chemical compounds new biologically active substances with a similar action and creation on their basis of new highly effective preparations is of considerable interest and is the actual problem.

The purpose of the invention is the creation of new biologically active compounds (bicarinata pseudoephedrine), which has antioxidant D-1-phenyl-2-aminopropanol-1 acid 5,6,7-trioxi - flavone-7-0--D-glucuronide and receive at this water-soluble salts. Yield 78%.

P R I m m e R. Synthesis of D-1-phenyl-2-metilaminopropanola-1-5,6,7-trioxifene-7-0- -D-glucuronidase.

1 grams of pseudoephedrine base is dissolved in 10 ml of ethanol. In the resulting solution of pseudoephedrine base in the flask with reflux condenser added 2.7 g of baicalin and the resulting solution was heated on a water bath for 1 h at 85aboutC.

The resulting solution was cooled to room temperature, filtered, cooled filtrate add ethyl acetate at a ratio of 1:2 and evaporated the resulting solution to room temperature.

The precipitation of a yellow-orange color filtered off, washed with ethyl acetate, dried.

The yield of the desired product in 78%.

Physico-chemical properties of the obtained compound (pseudoephedrine of bicarinata) is a yellow-orange crystalline powder, soluble in water, alcohols (methanol, ethanol and insoluble in ethers; so pl. 134-140aboutC.

The elemental composition, %: C 5,98; H 5,97; N 2,88.

Mol. weight 611,45.

IR-spectrum:

3420,3319 cm-1(OH - and NH-groups);

1601, 1492 cm-1(skeletal vibrations of benzene ring);

1438, 1377 cm-1(asymmetric and fluctuations monoamino benzene ring).

When pharmacological study found that the synthesized compound D-1-phenyl-2-metilaminopropanola-1-5,6,7-trioxifene-7-0- -D-GLUCURONIDE POSSESSING ANTIOXIDANT AND VASODILATOR ACTIVITY.

D-1-phenyl-2-metilaminopropanola-1-5,6,7-trioxifene-7-0 - b-D-glucuronide formula

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possessing antioxidant and vasodilator activity.

 

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