1,5-bis[(tert-butylamino)methyl]-n,n'-di-tert-butylbispidin-9-one and method for production thereof

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbispidin-9-one and a method for production thereof. 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbispidin-9-one is obtained by condensation of acetone with 1,3,5-tri-(tert-butyl)-1,3,5-triazacyclohexane while heating in an alcohol in the presence of acetic acid. The reaction is carried out while heating in ethanol or another alcohol. The obtained product is extracted after condensation of the reaction mass in a vacuum with hot toluene and recrystallised from ethyl alcohol.

EFFECT: obtaining a novel compound which can be used as a starting substance when producing bispidine and 1,3-diazaadamantane derivatives.

2 cl, 3 ex

 

The invention relates to the field of organic chemistry and particularly to a previously unknown 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-ONU or 1,5-bis[(tert-butylamino)methyl]was 3.7-di-tert-butyl-3,7-diazabicyclo[3.3.1]nonan-9-ONU and the method of its production.

The invention is a derivative of Besedin-9-it having two tert-butylaminoethyl Deputy at the nodal positions (C-1 and C-5). Derivatives Besedina and its analogs possess analgesic [G.S.Smith, M.D.Thomson, K.D.Berlin, E.M.Holt, B.J.Scherlag, E.Patterson, R.Lazzara. Eur. J. Med. Chem., 1990, 25,1], neurotrophic [.Siener, A.Cambareri, U.Kuhl, et al. J. Med. Chem., 2000, 43, 3746-3751], cardiovascular activity and can be used as a cardiovascular drug [G.L.Garrison, K.D.Berlin, B.J.Scherlag, et al. J. Med. Chem., 1996, 39, 2559].

The closest technical solution is the way to obtain 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-it-1,5-dimethyl-3,7-di-tert-butyl-3,7-diazabicyclo-[3.3.1]nonan-9-she [Cauteren, Ahiliya, Uttrachi, Amelea, Residronate, Waalewijn, Nesterov, Mendeleyev Somep., 1991, 1(3), 87-88] condensation of diethylketone, formaldehyde and tert-butylamine in the presence of acetic acid in ethanol under heating.

However, this method is not suitable for obtaining patent 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-it.

The technical result is an atom of the invention is a new compound 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-he, which can be used as the starting substance to obtain derivatives Besedina and 1,3-deazaadenosine.

The technical result of the invention is a method for 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-it, which can be used as the starting substance to obtain derivatives Besedina and 1,3-deazaadenosine with diverse biological activity.

The technical result is achieved by the fact that 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-it is produced by condensation of acetone with 1,3,5-tri-(tert-butyl)-1,3,5-triazacyclohexane when heated in alcohol in the presence of acetic acid, the reaction is carried out at heating in ethanol or another alcohol, the resulting product is extracted after the condensation reaction mass under vacuum hot toluene and recrystallized from ethanol.

Example 1

1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-he.

A solution of 2.90 g (50 mmol) propanone, 25.53 g (100 mmol) of 1,3,5-tri-(tert-butyl)-1,3,5-triazacyclohexane and 13.21 g (120 mmol) of acetic acid in 100 ml of ethanol is heated at the boil for 6 hours, the Reaction mass is evaporated. Add K2CO3to rn, stirred and extracted with boiling toluene (3×20 ml). The solvent is distilled off, the residue is recrystallized from ethanol. The output of 8.50 g (67%), white crystals, TPL 128-130°C. IR spectrum, ν, cm-1: 3323 (NH), 1706 (C=O). An NMR spectrum1N, δ, ppm: 0.978 d (N, SN3and 2NH), 2.421 (4H, 2NCH2), 2.90 (4H, 2NCH2C, J 10.28), 2.67 (4H, 2NCH2C, J 10.28). An NMR spectrum13S, δ, ppm: 218.79 (C-9), 55.62 (-2, 4, 6, 8), 53.61 (C-2CN), 50.61 (C-CNH), 50.05 (C-CH2N), 46.04 (C-1, 5), 29.21 (SN3), 26.78 (SN3). Mass spectrum, m/z (IRel., %): [M+H]+423.40. Found, %: C 71.16; N, 11.85; N, 12.98. With25H50N4O. Calculated, %: C 71.04; H 11.92; N, 13.25. Mthe calc.422.39.

Example 2

A solution of 2.90 g (50 mmol) propanone, 25.53 g (100 mmol) of 1,3,5-tri-(tert-butyl)-1,3,5-triazacyclohexane and 13.21 g (120 mmol) of acetic acid in 100 ml of isopropyl alcohol is heated at the boil for 4 hours, the Reaction mass is evaporated. Add K2CO3to rn, stirred and extracted with boiling toluene (3×20 ml). The solvent is distilled off, the residue is recrystallized from ethanol. The output of 6.50 g (53%), white crystals.

Example 3

The solution 14.63 g (200 mmol) of tert-butylamine, 9 g (300 mmol) of paraformaldehyde and 13.21 g (220 mmol) of acetic acid and 2.90 g (50 mmol) of acetone in 100 ml of ethanol is heated for 12 h at boiling. The reaction mass is evaporated. Add K2CO3to rn, stirred and extracted with boiling toluene (3×20 ml). The solvent is distilled off, the residue is recrystallized from ethanol. The output of 6.00 g (49%)

The identity of the compounds was confirmed by a combination of IR, NMR1H-NMR13With and mass spectra.

Thus, the proposed method allows to obtain from acetone and 1,3,5-tri-tert-butelek-sagitarian previously unknown 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-he that can be used as an intermediate product in the development of drugs for various purposes.

1. 1,5-Bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-it

as a starting substance to obtain derivatives Besedina and 1,3-deazaadenosine.

2. The way to obtain 1,5-bis[(tert-butylamino)methyl]-N,N'-di-tert-butylbiphenyl-9-it is the condensation of acetone with 1,3,5-tri-(tert-butyl)-1,3,5-triazacyclohexane when heated in alcohol in the presence of acetic acid, the reaction is carried out at heating in ethanol or another alcohol, the resulting product is extracted after the condensation reaction mass under vacuum hot toluene and recrystallized from ethanol.



 

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FIELD: chemistry.

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5 cl, 14 ex

FIELD: organic chemistry, medicine.

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132 cl, 1 tbl, 37 ex

FIELD: medicine, pharmaceutics.

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21 cl, 2 ex

FIELD: chemistry.

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Liquid hardening // 2447114

FIELD: chemistry.

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19 cl, 8 tbl, 5 ex

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28 cl, 117 ex, 3 tbl, 3 dwg

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8 cl, 2 ex

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10 cl, 1 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

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21 cl, 112 ex

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12 cl, 27 ex, 1 tbl

FIELD: chemistry.

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69 cl, 55 ex

FIELD: chemistry.

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4 cl, 1 tbl, 6 ex

FIELD: organic chemistry, medicine.

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132 cl, 1 tbl, 37 ex

FIELD: organic chemistry, chemical technology.

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11 cl, 2 tbl

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to a novel chemical compound, namely, to biologically active compound of the formula (I): possessing anti-arrhythmic activity and representing 5'-bromolappaconitine hydrobromide. Toxicity of this compound is by 4.8-fold less toxic as compared with analog used in medicinal practice and representing lappaconitine hydrobromide. Proposed compound possesses the expressed anti-arrhythmic activity in models with calcium chloride and adrenaline arrhythmia and provides the complete blocking both types of arrhythmia after administration of the dose that is 10-fold less of the therapeutic dose of lappaconitine hydrobromide.

EFFECT: improved and valuable medicinal properties of compound.

2 cl, 2 tbl, 4 ex

FIELD: organic chemistry, medicine, oncology.

SUBSTANCE: invention relates to condensed heterocyclic succinamide compounds of the formula (I): , their pharmaceutically acceptable salts, solvates or isomers wherein G represents mono- or polycyclic aryl or heterocyclic group substituted possibly at one or more positions; L represents a bond, -(CR7R7')n (wherein n = 1; R7 and R7' represents independently hydrogen atom (H), alkyl or substituted alkyl) or -CH2-NH-; Z1 represents oxygen atom (O); Z2 represents O; A1 and A2 represent -CR7 or in common with R7 from group W is a heterocyclic ring wherein oxygen represents a heteroatom; Y represents -O-, -SO-, -N(V2)-, -CH2-N(V2)-, -CO-N-(alkyl)-, -CH2-S-, -CH2-SO2-; V2 represents hydrogen atom, alkyl, arylalkyl, -CO-alkyl, -CO-O-aryl, -CO-O-arylalkyl; W represents -CR7R7'-CR7R7'-, -CR7R7'-C=O, -NR9-, -CR7R7'-, -N=CR8-, -N=N, -NR9-NR9'-, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo- or substituted heterocyclo-group, aryl or substituted aryl wherein if W doesn't mean -NR9-CR7R7'-, -N=CR8-, -N=N, -NR9-NR9'- or heterocyclo- or substituted heterocyclo-group then Y must mean -O-, -CH2-S-, -SO-, -CH2-SO2-, -N-(V2)- or -CH2-N-(V2)-; Q1 and Q2 represent hydrogen atom (H). Also, invention describes a method for synthesis of intermediate compounds in synthesis of compounds of the formula (I), using the latter for preparing agents modeling function of the nuclear hormone receptors. Compounds of the formula (I) can be used in treatment of prostate cancer.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds.

8 cl, 11 tbl, 463 ex

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to novel 3-phenyl-3,7-diazabicyclo[3,3,1]nonane compounds of the formula (I): wherein R1 means (C1-C6)-alkyl, (C4-C7)-cycloalkyl; R2 means (lower)-alkyl; R3 means (lower)-alkyl, or R2 and R3 form in common (C3-C6)-alkylene chain; R4 means phenyl monosubstituted at ortho- or para-position with nitro-, cyano-group or (lower)-alkanoyl, or disubstituted at ortho- and para-position with nitro-group, and their physiologically acceptable acid-additive salts. Compounds of the formula (I) possess anti-arrhythmic activity and therefore they can be used in pharmaceutical composition used in treatment and/or prophylaxis of cardiac rhythm disorders. Also, invention describes a method for synthesis of these compounds.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

8 cl, 6 tbl, 2 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of 1,4-diazabicycloalkane of the formula (IV): or its pharmaceutically acceptable addition salt wherein Ar represents carbocyclic aromatic (aryl) group or heterocyclic aromatic (heteroaryl) group that represents 5-6-membered ring comprising one nitrogen, sulfur or oxygen atom as a heteroatom and wherein aromatic group can be substituted with one substitute chosen from group consisting of (C1-C6)-alkoxy, halogen atom, -CF3, phenyl and benzyl. Also, invention relates to a pharmaceutical composition possessing inhibitory effect on nicotine acetylcholine receptors and containing the effective amount of compound of the formula (IV) or its pharmaceutically acceptable addition salt in combination with at least one pharmaceutically acceptable carrier or diluting agent. Invention provides derivatives of 1,4-diazabicycloalkane possessing inhibitory activity with respect to nicotine acetylcholine receptors.

EFFECT: valuable medicinal and pharmacological properties of compounds.

10 cl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention concerns malonamide derivatives of the formulae (IA) or (IB) , and pharmaceutically acceptable acid additive salts of them, where R1, R1',(R2)1,2,3, R3, R4, R14, L, and are such as described in this invention. Also the invention concerns a medicine with inhibition effect on γ-secretase, which can be applied in treatment of Alzheimer's disease.

EFFECT: obtaining new malonamide derivatives with beneficial biological properties.

17 cl, 188 ex

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