Methods of obtaining discrete esters of stanol/sterol, connection

 

The invention provides a method of direct esterification of Stanlow and sterols with fatty acids with the formation of discrete stanulovic/stalowych esters of General formula Iwhere R1- C6-C23carbon chain, R2- C3-C15the carbon chain- possible unsaturation in position With5by interaction of the corresponding 3-hydroxy fatty acid CH3-(CH2)n-CO2N, where n=4-22, in the presence of a weak acid catalyst (NaHSO4in a vacuum, at a temperature of about 100-200oWith, the selection is carried out preferably using the water method. The method provides a synthetic route, which can be used in the industrial production of esters with high product yield. 3 C. and 10 C.p. f-crystals.

Description text in facsimile form (see graphic part).

Claims

1. A method of obtaining a discrete esters of scanalatura General formula

where R1is6-C23carbon chain;

R2is3and C5that includes the interaction of stanol/Sterol General formula

where R2is3-C15carbon chain;

has the above meaning,

and fatty acid formula

CH3-(CH2)nCO2N

where n is an integer from 4 to 22, in the presence of a weak acid catalyst, under vacuum and at a temperature of about 100 - 200C, followed by separation of the target product.

2. The method according to p. 1, in which the reaction is carried out in the absence of solvent in the molten fatty acid acts as a solvent.

3. The method according to p. 1, in which the weak acid catalyst is NaHSO4.

4. The method according to p. 1, in which the corresponding serology/stanulovic ester receive not less than about 98 wt.%.

5. The method according to p. 1, in which R1complex ester stanol/Sterol has a value from C12to C21.

6. The method according to p. 1, in which the selection of the appropriate stanovova/Stereolove of ester carried out using only water way.

7. A method of obtaining a discrete esters of stanol/Sterol General formula

is3-C15carbon chain;

has the meaning specified in paragraph 1,

including the interaction of stanol/Sterol formula

wherehas the above meaning,

with a polyunsaturated fatty acid with chain length from C6to C24carbon atoms in the presence of a weak acid catalyst, under vacuum and at a temperature of about 100 - 200C.

8. The method according to p. 7, in which the reaction is carried out without added solvent in the molten fatty acid acts as a solvent.

9. The method according to p. 7, in which the weak acid catalyst is NaHSO4.

10. The method according to p. 7, in which the output of the corresponding stanovova/Stereolove of ester is not less than 98 wt.%.

11. The method according to p. 7, in which the selection of the appropriate stanovova/Stereolove of ester is carried out using only water way.

12. A compound selected from the group consisting of

or

wherehave the above meanings; R2is3Priorities for items:

25.08.1998 on PP.1-13;

15.12.1998 clarification of the characteristics of PP.1-13.

 

Same patents:

The invention relates to steroids Sterol number of General formula I, where R1and R2independently selected from the group comprising hydrogen and unbranched or branched C1-C6-alkyl; R3selected from the group including hydrogen, methylene, hydroxy, oxo, =NOR26where R26represents hydrogen and hydroxy and C1-C4-alkyl, related to the same carbon atom of the Sterol skeleton, or R3together with R9or R14designate an additional bond between the carbon atoms that are associated with R3and R9or R14; R4selected from the group comprising hydrogen and oxo, or R4together with R13designate an additional bond between the carbon atoms that are associated with R4and R13; R5selected from the group comprising hydrogen and hydroxy, or R5together with R6designate an additional bond between the carbon atoms that are associated with R5and R6; R6represents hydrogen or R6together with R5designate an additional bond between the carbon atoms that are associated with R6and R5or R14; R9represents hydrogen or R9together with R3or R10denote dobavlaet hydrogen or R10together with R9designate an additional bond between the carbon atoms that are associated with R10and R9; R11selected from the group comprising hydroxy, acyloxy, oxo, = NOR28where R28represents hydrogen, halogen, or R11together with R12designate an additional bond between the carbon atoms that are associated with R11and R12; R12represents hydrogen or R12together with R11designate an additional bond between the carbon atoms that are associated with R12and R11; R13represents hydrogen or R13together with R4or R14designate an additional bond between the carbon atoms that are associated with R13and R4or R14; R14represents hydrogen or R14together with R3, R6or R13designates an additional bond between the carbon atoms that are associated with R14and R3or R6or R13; R15is hydrogen; R16selected from the group comprising hydrogen, hydroxy, oxo or16together with R17designate an additional bond between the carbon atoms that are associated with R16and R17; R17represents hydrogen or hydroxy, or R1716; R18and R19represent hydrogen; R25selected from the group including hydrogen, and C1-C4-alkyl; a represents a carbon atom or a nitrogen atom; when a represents a carbon atom, R7selected from the group including hydrogen, hydroxy and fluorine, and8selected from the group including hydrogen, C1-C4-alkyl, methylene, and halogen, or R7together with R8designate an additional bond between the carbon atoms that are associated with R7and R8; R20is1-C4-alkyl; R21selected from the group including1-C4-alkyl, C1-C4-hydroxyalkyl,1-C4-halogenated containing up to three halogen atoms; when a represents a nitrogen atom, R7denotes a lone pair of electrons, and R8selected from the group comprising hydrogen and oxo; R20and R21are1-C4-alkyl with the proviso that the compound of General formula (I) does not have any cumulated double bonds and with the additional condition that the connection is not one of the known compounds cholestenone
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< / BR>
which is a known intermediate compound in the synthesis of progesterone

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The invention relates to medicine, namely to otolaryngology, and can be used for the treatment of patients with neoplasms of male genital organs

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FIELD: medicine, immunology.

SUBSTANCE: invention proposes an agent enhancing the immunogenic properties of tetanus anatoxin (adjuvant). Invention proposes the vegetable triterpenic compound miliacin as an agent enhancing immunogenic properties of tetanus anatoxin. Agent enhances the immune response value in its applying as a vaccine preparation of tetanus anatoxin. The agent miliacin elicits its stimulating effect for both the first and repeated administration of vaccine that allows suggesting its possible applying for prophylactic vaccinations with tetanus anatoxin. Taking into account the high tolerance of miliacin in the broad range of its doses it is suggested its practical applying as an agent promoting to the enhanced formation of vaccinal immunity in prophylactic vaccinations with tetanus anatoxin.

EFFECT: valuable medicinal properties of agent.

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