| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: invention relates to anthracycline derivatives of general structural formula given below ^ where R1, R2 and R3 are H or OH; R4 denotes H, OH, C1-C5alkyl, or O-(C1-C5)alkyl; R5 is O or NH; and R6 is selected from a group comprising H, OH and a sugar residue which is The invention also relates to a method of producing said derivatives by reacting 13-ketoanthracycline or acid salt thereof with benzenidesulphonylhydrazide in an alcohol solvent at temperature of approximately 35-50C for approximately 10-24 hours. The invention also pertains to a method of producing 13-deoxyanthracyclines, involving preparation of an alcoholic solution of the said 13-benzenidesulphonylhydrazine anthracycline; addition of a reducing agent and acid to the said solution; heating said solution without stirring, agitation or dephlegmation in order to reduce said 13-benzenidesulphonylhydrazine anthracycline; neutralisation of said solution with an aqueous solution of a base to obtain said 13-deoxyanthracycline derivative and precipitation; and, additionally, filtration of said precipitate, extraction of said 13-deoxyanthracycline from said precipitate, as well as extraction of said 13-deoxyanthracycline from the filtrate. The invention also relates to a method of producing 5-imino-13-deoxyanthracyclines involving synthesis of 13-deoxyanthracyclines as described above; dissolution of said 13-deoxyanthracyclines in an alcohol and conversion of said 13-deoxyanthracyclines to the corresponding 5-imino-13-deoxyanthracyclines under the effect of ammonia at temperature lower than approximately 20C. The invention also relates to a method of producing 13-deoxyanthracyclines involving preparation of an alcoholic solution of 13-benzenidesulphonylhydrazine anthracycline having structural formula given below; addition of a reducing agent and a pyridinium acid salt to the said solution and heating said solution to reduce said 13-benzenidesulphonylhydrazine anthracycline. The invention also relates to a method of producing 5-imino-13-deoxyanthracyclines involving preparation of said 13-deoxyanthracycline and its conversion to the corresponding 5-imino-13-deoxyanthracycline under the effect of ammonia at temperature lower than approximately 20C. ^ EFFECT: new compounds have useful biological properties. ^ 21 cl, 4 tbl, 4 ex |
