DERIVATIVES OF 7-, 8-, 9-(SUBSTITUTED)-6-DEMETHYL-6-DEHYDROXY-TETRACYCLINES, METHODS OF THEIR SYNTHESIS, INTERMEDIATE COMPOUNDS AND A PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

Abstract RU 2127255 C1

FIELD: organic chemistry, antibiotics. SUBSTANCE: invention relates to derivatives of 7-, 8-, 9-(substituted)-6-demethyl-6-dehydroxy- tetracyclines of the formula (I) where X - halogen; R and R1 are similar or distinct and mean H, NH2, halogen, NR2R3 and when R and R1 is NR2R3 and R2 is H then R3 - methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methyl- propyl, 1,1-dimethylethyl; when R2 - methyl, ethyl then R3 is methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methyl- propyl, 2-methylpropyl; when R2 is n-propyl then R3 is n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methyl- -propyl; when R2 is 1-methylethyl then R3 is n-butyl, 1-methylpropyl, 2-methylpropyl; when R2 is n-butyl then R3 is n-butyl, 1-methylpropyl, 2-methylpropyl; when R2 is 1-methylpropyl then R3 is 2-methylpropyl; when R and R1 are NR2R3 and R2 - H then R3 is -CO-R4 where R4 - H, NH2, mono-(C1-C6)-alkylamino-groups, diastereoisomers and enantiomers of mono - (C1-C6) - alkylamino - group; or R3 is di-(C1-C6)-alkylamino-group. Compounds are used as a pharmaceutical composition showing antibacterial activity. EFFECT: improved method of synthesis, enhanced effectiveness. 7 cl, 3 dwg, 3 tbl, 49 ex

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RU 2 127 255 C1

Authors

Fajk-Eng Sam

Ving Dzh.Li

Dzhozef Dzh. Khlavka

Rehjmond T.Testa

Dates

1999-03-10Published

1993-08-12Filed