Method for synthesis of 4a,5b,10,12-tetraazaindeno[2,1-b]fluorene

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to method of obtaining 4a,5b,10,12-tetraazaindeno[2,1-b]fluorene, which consists in the fact that interaction of pyridine with 1,5-dichloro-2,4-dinitrobenzene is carried out at temperature 20C in acetone and molar ratio 1,5-dichloro-2,4-dinitrobenzene:pyridine = 1:4 for 4 hours, reduction of alcohol salt solution 1,1'-(4,6-dinitro-1,3-phenylene)dipyridinium is realised with solution SnCl22H2O in 3% hydrochloric acid and molar ratio salt 1,1'-(4,6-dinitro-1,3-phenylene)dipyridinium : SnCl22H2O = 1:6 at temperature 40C for 0.25 h.

EFFECT: method of binding, which is characterised by reduction of synthesis time and increase of purity and target product output, has been elaborated.

2 ex

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to improved method of obtaining pyridine compounds (AA),(BB) and (CC) of respective formulas:

,

,

.

said compounds possess inhibiting action with respect to HIV-integrase. method consists in carrying out the following stages: P-1) bromination of compound of formula (I-I) with obtaining bromine-compound of formula (II-II)

,

where value R represents -CHO, -CH(OH)2, -CH(OH)(OR4), -CH(OH)-CH2OH or -CH(OR5)(OR6); P1 represents benzyl; P3 represents H or protective group of carboxyl; R4 represents lower alkyl; R5 and R6 independently represent lower alkyl or R5 and R6 can represent alkyl and be connected with formation of 5-, 6- or 7-member ring, P-2) formation of side chain of 2,4-di-fluorophenyl-CH2-NH-C(O)- with application of reagents 2,4-di-fluorophenyl-CH2-NH2 and carbon monoxide, stage of formation of Q ring by means of respective amine, selected from 3-amino-butan-1-ol, 2-amino-propan-1-ol and 2-pyrrolidinyl methylamine, and stage of debenzylation with obtaining compound of formula (AA), (BB) or (CC), where said stage P-2 is carried out after formation of Q ring.

EFFECT: method makes it possible to simplify obtaining target compounds due to carrying out regioselective bromination at the first stage.

6 cl, 3 ex, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to fluorinated catharantine derivatives of general formula I in which broken line represents possibility of double bond presence, when substitution X is absent, or simple bond, when X stands for substitution with another group: H, R1, R2 and R3 independent on each other represent a fluorine atom or methylated group, and n=2.

EFFECT: invention also relates to method of obtaining said derivative and to its application as intermediate compound for synthesis of fluorated dimeric Vinca alkaloids, in particular vinflunine, which in its turn is used as anti-cancer agent.

22 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described new N-cyclic sulphonamido-compounds and their pharmaceutically acceptable salts of formula : of formula 1a of formula 1b of formula 1c where the ring A means phenyl, thienyl which can be substituted by halogen, or pyridinyl; a value of the ring B is presented in the patent claim, and also a pharmaceutical composition containing them, and a method of treating Alzheimer's disease.

EFFECT: compounds are gamma-secretase inhibitors and can be used for treating Alzheimer's disease.

16 cl, 98 ex

FIELD: medicine.

SUBSTANCE: there is recovered a fragment of genomic DNA Pseudomonas fluorescent A2-2, including full-size gene cluster of biosynthesis of safracin (A and B) analysis of which showed the presence of several "OPC" arranged in two operons: sacABCDEFGH and sacIJ. Expression of nucleic acid containing full gene cluster of safracin in a heterosystem enabled producing recombinant forms of natural safracins A and B.

EFFECT: removal or malfunction of separate genes found in operons, and applications of the produced modified forms of nucleic acid in the recombinant DNA technology have resulted in synthesised analogues of safracin to be used as an antimicrobial or antitumour agent, and also in synthesis of ecteinascedine compounds.

20 cl, 9 dwg, 7 ex

The invention relates to inhibitors tyrosinekinase type bis-indolylmaleimide compounds of the formula I

< / BR>
where Z denotes a group of General formula II

< / BR>
where A, B, X, Z, R1-R10have the meanings indicated in the claims, as well as the way they are received and drug based on these compounds

The invention relates to new imidazolidine formulas (I) and (II) in which a is a =N-CR=CR-CR=, =CR-N=CR-CR=, =CR-CR=N=CR or = CR-CR= CR-N= ; B represents-NR-C(R)2-C(R)2-C(R)2C(R)2-NR-C(R)2-C(R)2, -C(R)2-C(R)2-NR-C(R)2or C(R)2-C(R)2-C(R)2-NR, where R is hydrogen, R1is hydrogen, unsubstituted or substituted C1-20-alkyl, C1-20-alkylene-NR3-Q-X-R4where Q represents-CO-or-SO2-, X is a simple bond, -O - or-NR3and R4- aryl, heteroaryl, heterocyclyl or1-20-alkyl or C2-20alkenyl
The invention relates to a method by which you can lower cost and with greater purity to obtain alkaloids from plants

FIELD: medicine.

SUBSTANCE: there is recovered a fragment of genomic DNA Pseudomonas fluorescent A2-2, including full-size gene cluster of biosynthesis of safracin (A and B) analysis of which showed the presence of several "OPC" arranged in two operons: sacABCDEFGH and sacIJ. Expression of nucleic acid containing full gene cluster of safracin in a heterosystem enabled producing recombinant forms of natural safracins A and B.

EFFECT: removal or malfunction of separate genes found in operons, and applications of the produced modified forms of nucleic acid in the recombinant DNA technology have resulted in synthesised analogues of safracin to be used as an antimicrobial or antitumour agent, and also in synthesis of ecteinascedine compounds.

20 cl, 9 dwg, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described new N-cyclic sulphonamido-compounds and their pharmaceutically acceptable salts of formula : of formula 1a of formula 1b of formula 1c where the ring A means phenyl, thienyl which can be substituted by halogen, or pyridinyl; a value of the ring B is presented in the patent claim, and also a pharmaceutical composition containing them, and a method of treating Alzheimer's disease.

EFFECT: compounds are gamma-secretase inhibitors and can be used for treating Alzheimer's disease.

16 cl, 98 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to fluorinated catharantine derivatives of general formula I in which broken line represents possibility of double bond presence, when substitution X is absent, or simple bond, when X stands for substitution with another group: H, R1, R2 and R3 independent on each other represent a fluorine atom or methylated group, and n=2.

EFFECT: invention also relates to method of obtaining said derivative and to its application as intermediate compound for synthesis of fluorated dimeric Vinca alkaloids, in particular vinflunine, which in its turn is used as anti-cancer agent.

22 cl

FIELD: chemistry.

SUBSTANCE: invention relates to improved method of obtaining pyridine compounds (AA),(BB) and (CC) of respective formulas:

,

,

.

said compounds possess inhibiting action with respect to HIV-integrase. method consists in carrying out the following stages: P-1) bromination of compound of formula (I-I) with obtaining bromine-compound of formula (II-II)

,

where value R represents -CHO, -CH(OH)2, -CH(OH)(OR4), -CH(OH)-CH2OH or -CH(OR5)(OR6); P1 represents benzyl; P3 represents H or protective group of carboxyl; R4 represents lower alkyl; R5 and R6 independently represent lower alkyl or R5 and R6 can represent alkyl and be connected with formation of 5-, 6- or 7-member ring, P-2) formation of side chain of 2,4-di-fluorophenyl-CH2-NH-C(O)- with application of reagents 2,4-di-fluorophenyl-CH2-NH2 and carbon monoxide, stage of formation of Q ring by means of respective amine, selected from 3-amino-butan-1-ol, 2-amino-propan-1-ol and 2-pyrrolidinyl methylamine, and stage of debenzylation with obtaining compound of formula (AA), (BB) or (CC), where said stage P-2 is carried out after formation of Q ring.

EFFECT: method makes it possible to simplify obtaining target compounds due to carrying out regioselective bromination at the first stage.

6 cl, 3 ex, 7 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to method of obtaining 4a,5b,10,12-tetraazaindeno[2,1-b]fluorene, which consists in the fact that interaction of pyridine with 1,5-dichloro-2,4-dinitrobenzene is carried out at temperature 20C in acetone and molar ratio 1,5-dichloro-2,4-dinitrobenzene:pyridine = 1:4 for 4 hours, reduction of alcohol salt solution 1,1'-(4,6-dinitro-1,3-phenylene)dipyridinium is realised with solution SnCl22H2O in 3% hydrochloric acid and molar ratio salt 1,1'-(4,6-dinitro-1,3-phenylene)dipyridinium : SnCl22H2O = 1:6 at temperature 40C for 0.25 h.

EFFECT: method of binding, which is characterised by reduction of synthesis time and increase of purity and target product output, has been elaborated.

2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compound of formula I or its pharmaceutically acceptable salts, which are inhibitors of Trk kinases and are useful for treating pain, malignant oncological disease, inflammation, neurodegenerative diseases and Trypanasoma Crusi infections. Invention also describes versions of methods of producing compound of formula I. In Formula I (I) ring A is selected from A-1, A-2, A-3, having structure , where wavy line marked 1 indicates connection point of ring A to ring B, and wavy line marked 2 indicates point of connection ring A to W; X is N or CH; Y is H or F; R1 is H or halogen; ring B is selected from rings B-1 and B-2, having structure , where wavy line marked 3 indicates point of connection to ring A, and wavy line marked 4 indicates point of connection to pyrazolo[1,5-a]pyrimidine ring of formula I; W is O, NH or CH2, wherein, when ring A is A-2, then W is CH2; m is 0, 1 or 2; D is carbon, R2 and R2a independently represent H, F, (1-3C)alkyl or OH (provided that R2 and R2a are not simultaneously OH), and R3 and R3a are independently H or (1-3C)alkyl, or (D) is carbon or nitrogen, R2 and R3 are absent, and R2a and R3a together with atoms to which they are bonded, form 5-6-member heteroaryl ring containing 1-2 heteroatoms ring; Z is *-NR4aC(=O)-, *-ONHC(=O)-, *-NR4bCH2- or *-OC(=O)-, where asterix indicates connection point of Z to containing carbon R3; R4a is H or (1-6C)alkyl; R4b is H, (1-6C)alkyl, ((1-6C)alkyl)C(O)-, HOCH2C(O)-, ((1-6 C)alkyl) sulfonyl, HO2CCH2- or ((1-6C)alkyl)NH(CO)-; and R-5 and R6 independently represent H, halogen, OH or (1-6C)alkyl.

EFFECT: useful for treating pain, malignant oncological disease, inflammation, neurodegenerative diseases and Trypanasoma Crusi infections.

73 cl, 1 tbl, 45 ex

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of general formula

or , or pharmaceutically acceptable salts thereof, R is methyl, ethyl, propyl or benzyl; * - X - * is selected from the group consisting of , and ; Y is (-CH2-)3 or (-CH2-)4. The invention also relates to a method for preparation of compounds of general formula 1 or 2.

EFFECT: new compounds are obtained that have the properties of protein-protein interactions inhibitors.

4 cl, 2 tbl, 3 ex

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