The method of obtaining derivatives of 19-norprogesterone


(57) Abstract:

Usage: as progestational funds. Essence: the product is a derivative of 19-norprogesterone f-ly 1, where R1- N, methoxymethyl, tetrahydropyranyl, the radical f-crystals of 2 - acyl C1-C6. The output 14 of 88% , so pl. 76 - S. Reagent 1: 3-alkoxy-östra-1,3,5-triene. Reagent 2: bromodiphenylmethane. Reagent 3: 3-alkoxy-17-propylidene-1,3,5, (10)-triene. Reagent 4: Li in liquid NH3. Reagent 5 : 3-oxo-21-methyl-19-norpregna 4,17/20/-diene. Reagent 6: trialkylaluminium + acid. Reagent 7: 3-alkoxy-17-propylidene-östra-3,5-diene. Reagent 8: POCl + dimethylformamide. Reagent 9: 3-alkoxy-6-formyl-21-methyl-19-norpregna-3,5,17(20). Reagent 10: mixed hydride of an alkali metal. Reagent 11: 6-hydroxymethyl-21-methyl-3-oxo-19-norpregna-4,17(20)-diene. Reagent 12: acid (HCl). The reagent 13: 21-methyl-6-methylene-3-oxo-19-norpregna-4,17(20)-diene; Reagent 13: Pd/C+C2H5OH+CH3COONa. The reagent 14: 3-oxo-6-methylestra-4,6-diene. Reagent 15: OSO + hydroxide N-oxydiethylene. The reagent 16: 17-hydroxy-6,21-dimethyl-3,20-dioxo-19-norpregna-4,6-diene, followed if necessary by methoxyethylamine, dehydrophenylalanine or acylation. F-crystals 1 and 2 are given in the description of the invention.

Izopet theron, General formula I (I) where R1is hydrogen, methoxymethyl, tetrahydropyranyl or acyl C1-6.

Known derivatives of 19-norprogesterone with 6-methyl Deputy as, for example, nomegestrol, which is a powerful progestational derived pure progesterone properties.

Also known derivatives of 19-norprogesterone, chain them in position 17 contains 3 carbon atoms, and, in particular, 3,20-dioxo-17-21-dimethyl-19-norpregna - 4,9-diene. This type of connection shows only minor progesteronelike properties in comparison with its lower homologue.

The purpose of the invention is to develop a method of obtaining new progesterona with a higher pharmacological activity.

The proposed method lies in the fact that the compound 3-alkoxy-östra-1,3,5-triene General formula II (II) where R2= C1-C6exposed to bromide propyltrichlorosilane to get propylidene derivative of General formula III (III) as E isomers or Z, where R2have the above values, which are subjected to hydrogenation according to the method of Birsa with the formation of 3-oxo-21-methyl-19-norpregna 4,17 (20)-diene, which obrabatyvati General formula IV (IV) as E isomers or Z, where R2have the above values, and which is then subjected to formirovanie method Wilmsmeier-Haq to obtain 6-formyltransferase General formula V (V) as E isomers or Z, where R2have the above values, then restore using mixed alkali metal hydride to obtain the corresponding 6-hydroxymethylamino derivative with subsequent treatment with an acid to obtain 3-oxo-6-methylene derivative of General formula VI (VI) as E isomers or Z, followed by isomerization in the presence of isomerization catalyst to obtain 3-oxo-6-östra-4,6-diene derivative of the General formula VII (VII) in the form of isomers E and Z, which are bishydroxyethyl using osmium tetroxide and peroxide N-oxide of triethylamine in an inert atmosphere, to obtain 17-hydroxy-20-ketopropane formula VIII (VIII) which is subjected, if necessary, processing methoxyethylamine using methoxyethylamine, or processing dihydropyrimidinase using dihydropyran in an acidic environment, or acylation with functional carboxylic acid derivative in the presence of an acidic agent.

P R I m e R 1. 6,21-Dimethyl-17-hydroxyl-3,20-dioxo-19-nor the toxi-17-oxo-östra 1,3,5(10)-triens injected into the nitrogen atmosphere in 72 ml of dimethyl sulfoxide and 20 ml of hexane. Then add 14.5 g of bromide p-propyltrichlorosilane and 4.2 g of potassium butyl and 0.67 g of 18-crown-6-ether. The insufficient two phase mixture is heated to 60aboutC for 8 h and Then the temperature of the mixture was adjusted to 15aboutC in an ice bath and add 20 ml of water and 20 ml odnopolyarnogo hydrochloric acid in 150 ml of methanol and left under stirring overnight. Add water and extracted with dichloromethane. Obtain 7.5 g of the crude oil that is passed through silica for chromatography, then wash with methylene chloride. Thus obtained 3 g of the product with purity of 80% , shows liquid chromatography with high yield (GHW), i.e., the net yield of 54% , with a melting point 76aboutC; [] D20(C = 1% methanol) = 59about.

b) 3-keto-21-methyl-19-norpregna-4,17(20)-Dien.

At a temperature of 50aboutC in an atmosphere of argon is added to 3 l of liquid ammonia solution 1,72 g 3-methyl-19-nor-21-methylpregna-1,3,5/10/17/20/-tetraene in 175 ml of anhydrous tetrahydrofuran. At intervals of 30 min was added with stirring 3 times in 90 ml of ethanol and 1,72 g of lithium. After 60 min stirring to remove ammonia in a water bath with a weak vacuum. Added to 1.3 liters of water and peremeshivayte add chetyrehkomnatnuyu hydrochloric acid to pH 2 and stirred for further 2 hours Precipitated steroid, adding water, and then separating it by filtration.

Gain of 3.45 g of 3-keto-21-methyl-19-norpregna-4,17(20) of the crude diene. Absorb isopropyl ether and get pure product in the form of liquid oil, pale yellow; []D20= +59about(C = 1% methanol), which is not crystallized.

C) 3-ethoxy-21-methyl-19-norpregna 3,5,17(20)-triene.

5 g of 3-keto-21-methyl-19-norpregna 4,17(20)-diene obtained in the preceding stage, dissolved in 15 ml of ethanol, to which was added 5 ml of utilitiarian and is 0.102 g of p-toluenesulfonic acid. The mixture is brought to boiling for 3 hours with simultaneous removal of the water formed. After this time add 3.6 ml of triethylamine. So get 2,75 g of crystalline product with a melting point of 104aboutC. the Infrared spectrum shows bands characteristic for a system with double bonds from 3.5 to 1650 and 1620 cm-1and vinyl carbon at 3080 cm-1.

UV spectrummax243 NS = 20840.

Stage B.

3 Ethoxy-6-formyl-21-methyl-19-norpregna-3,5,17(20), Z-isomer (VIII).

To 30 g of 3-ethoxy-21-methyl-19-norpregna-3,5,17(20)-triens, the Z isomer (III), and 300 ml of dimethylformamide, add the reagent Willism the organizational environment is maintained with stirring for 1 h 15 min Add 140 ml of an aqueous solution saturated with sodium acetate in 15 min is formed crystalline yellow precipitate, which is filtered and washed with water. After filtration and washing with water to obtain 20.2 g of yellow crystals of 3-ethoxy-6-formyl-21-methyl-19-norpregnane-3,5,17(20) (Z isomer) (VIII).

Yield 62% . The melting point of the pure product 99aboutC.

The rotational ability []D20= = 21,5about(C = 1% dioxane).

Stage Century.

21-Methyl-6-methylene-3-oxo-19-norpregna-4,17 (20)-diene, Z isomer (IX).

14 g of 3-ethoxy-6-formyl-21-methyl-19-norpregna-1,5,17 (20)-triens, the Z isomer (VIII), and 140 ml of methanol is maintained with stirring for 1 h 20 min with 960 mg of sodium borohydride at 0aboutC. Then slowly add 15 ml denormalize hydrochloric acid and stirred to obtain crystals. Obtain 8.7 g of 21-methyl-6-methylene-3-oxo-19-norpregna-4, 17 (20)-diene, Z isomer (IX).

Yield 71% . The melting point 110-14aboutC.

The rotational ability, []D= 218about(1% dioxane),

UV spectrummax. 261 nm, = 10600.


6,21-Dimethyl-3-oxo-19-norpregna-4,6,17 (20)-triene, isomer Z (X)

3.5 g of 21-methyl-6-methylene-3-oxo-19-norpregna-4,17 (20)-diene, the Reaction medium is filtered, extracted with chloroform and washed with water. The organic phase chromatographic on silicon dioxide. The eluates obtain 3.1 g 6,21-dimethyl-3-oxo-19-norpregna-4,6,17 (20)-triens, isomer Z (X), in the form of several yellowish oil.

Yield 88% .

The rotational ability []D= -31o(1% - dioxane),

UV spectrummax288 nm, = 22000.

Stage D.

6,21-Dimethyl-17-hydroxy-3,20-dio - CSR-19-norpregna-4,6-diene.

2.9 g 6,21-dimethyl-3-oxo-19-norpregna-4,6,17 (20)-triens (X), 29 ml of tertiary butanol, of 0.58 ml of 2.5% aqueous solution of camerahouse osmium in the tertiary butanol and 4,06 g complex triethylamine-N-oxide Gidropress stirred for 24 h at ambient temperature. Then add 3 g of celite and 2 g of sodium sulfite in water and again stirred for 2 h

Extracted with toluene and permalert the organic phase layer Dookie silica for chromatography. The eluate is evaporated to dryness and absorb hot methanol. After crystallization obtain 1.66 g 6,21-dimethyl-17-hydroxy-3,20-dioxo-19-norpregna-4,6-diene.

Yield 52% . The melting point of 204aboutC.

P R I m m e R 2. 1 g 6,21-dimethyl-17-acetoxy-3,20-dioxo-19-norpregna-4,6-diene, 10 ml of chloroform, 0.8 ml of acetic any the concentrated hydrochloric acid and again incubated at reflux for 1 h The medium is extracted with chloroform, washed with water, brought to dryness in vacuum. The remainder absorb for crystallization with methanol.

Obtain 780 mg of crystals 6,21-dimethyl-17-acetoxy-3,20-dioxo-19-nocleg - on-4,6-diene.

Yield 69% . UV spectrum;max288 nm, = 23400.

The melting point 203aboutC.

The rotational ability [] D = -34about(1% in dioxane)

The NMR spectrum in chloroform to 0.68 Hz, 3H

the singlet l8 of 1.05 Hz, 3H


Y = 7 Hz C22 to 1.86 Hz, 3H

the methyl singlet at C6 of 2.08 Hz, 3H

the singlet CH3-CO - 5,95 Hz 1H

the singlet N in C7 6,05 Hz 1H

the singlet H in C6

According to the same method are through the action of the chloride propionyl 6,21-dimethyl-17-propionyloxy-3,20-di - oxo-19-norpregna-4,6-diene (example 3).

Yield 57% .

UV spectrummax288 nm; = 24600.

The melting point of 186-187aboutC.

The rotational ability, []D= -41about(C = 1% dioxane).

Through the actions of hexanolactone:

6,21-dimethyl-3,20-dioxo-17 hexano - yloxy-19-norpregna-4,6-diene (example 4).

Yield 38% .

UV spectrum max289 nm; = 24400.

Melting point 132aboutC.

IR-spectrum: 1735, 1715, 1655, 169-norpregna-4,6-diene (example 5).

Exit 14% .

UV spectrummax288 nm, = 24900.

Melting point 195aboutC.

The rotational ability, [] D = -44about(C = 1% dioxane).

Through the action of benzoyl chloride

6,21-dimethyl-3,20-dioxo-17-benzo - yloxy-19-norpregna-4,6-diene (example 6).

Yield 79% .

UV spectrum max294-295. = 24900.

Melting point 221aboutC.

The rotational ability [] D = -81about(C = 2% dimethylformamide).

Through the actions of monochloroethylene

6,21-dimethyl-3,20-dioxo-17-chlorate - tilox-19-norpregna-4,6-diene (example 7).

Yield 29% .

UV spectrum max. 291 nm. = 26400.

Melting point 237aboutC.

The rotational ability, [] D = -53about(C = 1% dioxane).

P R I m e R 8. 6,21-dimethyl-3,20-dioxo-17 tetrahydropyranyloxy-19-nocleg - on-4,6-diene.

2.5 g of 17-gidrauxilirovannogo derivative is dissolved in 75 ml of chloromethylene and 50 ml of benzene. Add 0.5 ml dihydropyran and 25 mg of p-toluensulfonate acid. After 2 h 20 min stirring again add the same amount dihydropyran. After 3 h the reaction mixture was extracted. The reaction product chromatograph is fishing, which melt at 179-180aboutC.

P R I m e R 9. 6,21-dimethyl-3,20-dioxo-17 methoxyethoxy-19-norpregna-4,6-diene.

2.16 g 3,20-dioxo-6,21-dimethyl-17-hydroxy-19-norpregna-4,6-diene is dissolved in 50 ml of chloromethylene and 10 ml of anhydrous formaldehydefree. The solution is cooled to 0aboutC in an ice bath. Add 2 g of phosphorus pentoxide and the mixture was kept at 0aboutWith stirring for 1 h the mixture is Then filtered and the filtrate washed with chloromethylene. To the filtrate add triethylamine to obtain a pH of 9. The mixture was concentrated in vacuo. The residue is recrystallized in a mixture of methanol/chlormethine and gain of 2.27 g 6,21-dimethyl-3,20-dioxo-17-methoxime - yloxy-19-norpregna-4,6-diene.

Melting point 182-184aboutC.

UV spectrummax291 nm. = 26100.

Compounds of General formula (I) possess valuable properties and, in particular, can be used as a means of promoting digestion, and their great affinity for acceptors progesterone gives high progestational activity.

New connections do not show any toxicity. So, when administered to mice by mouth or intravenously in an amount of 200 mg/kg is connected is.

For progesterone receptor determine the ability of each steroid in comparison with the reference substance (cold progesterone).

Labeled progesterone incubated with cytotam cancer, alone or in the presence of increasing concentrations of cold steroid (including unlabeled progesterone), when the ratio R of the two substances from 1 to 1000.

These compounds were compared with acetate, medroxy-progesterone (AMP) and acetate nomegestrol (TX 066).

In the above table. 1 shows the concentration of labeled progesterone, is associated with the receptor in the presence of cold standard.

The data table. 1 allow us to determine the relative affinity. The relative affinity is the ratio of the concentration at 50% inhibition (C) of this steroid and cold hormone that is taken as a reference (in this case progesterone): O. C. = S/Se.

Thus, the relative affinity is expressed as a percentage considering that for the reference hormone (or steroid) value AR O. C. equal 100% .

Values S represent an estimate of the KI (inhibition constant) of the investigated steroids in relation to the connection reference of the steroid (see tab. 2).

Thus, the dimension in cetat > 17-hydroxy.

However, although the affinity for the progesterone receptor is an important characteristic of the compounds, it is not the only characteristic of the connection and average affinity may nevertheless show high biological activity, if the molecule is not subject to metabolism due to the complex chemical structure of the molecule. Thus, the methyl group in position 6 protects the system of double bonds 4,6 metabolism, and the methyl substituent in position 21 protects from metabolism of ketone in position 20. Thanks to this structure, the compounds according to the invention exhibit high progesterone activity. (56) Patent of great Britain N 924981, CL 2/3 / S, 1963.

French patent N 2877877, class A 61 K 27/00, 1971.

French patent N 2271833, class A 61 K 31/57, 1975.


< / BR>
where R1is hydrogen, methoxymethyl, tetrahydropyranyl or C1-C6-acyl, characterized in that the compound 3-alkoxy-östra-1,3,5-triene General formula

< / BR>
where R2-C1-C6-alkyl,

exposed to bromide propyltrichlorosilane to get propylidene prove exposed to the hydrogenation according to the method of Birsa with the formation of 3-oxo-21-methyl-19-norpregna 4,17(20)-diene, that is processed by the alkylation agent, such as trialkylaluminium, in an acidic medium to obtain a derived östra-3,5-diene General formula

where R2has the specified values,

as E isomers or Z, which is then subjected to formirovanie method Wilmsmeier - Haq to obtain 6-formyltransferase General formula

where R2have the specified values,

as E isomers or Z, then restore using mixed alkali metal hydride to obtain the corresponding 6-hydroxy-methyl derivative with subsequent treatment with an acid to obtain 3-oxo-6-methylene derivative of General formula

< / BR>
as E isomers or Z, followed by isomerization in the presence of isomerization catalyst to obtain 3-oxo-6-methyl-östra-4,6-diene derivative of General formula

< / BR>
as E isomers or Z, followed by processing bishydroxyethyl chetyrehokisi osmium and hydropredict N-oxide, triethylamine in an inert atmosphere with the formation of 17-hydroxy-20-ketopropane General formula

< / BR>
if necessary, it will methoxymethylethoxy by the halide methoxymethyl the CSOs carboxylic acid in the presence of an acidic agent.


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