| abstract |
IT REFERS TO A METHOD OF PREPARING TETRACYCLINES, PREFERENTIALLY FORMULA TIGECYCLINE (1), WHERE R1 AND R2 IS INDEPENDENTLY H, ALKYL (C1-C6) OF STRAIGHT OR BRANCHED CHAIN, ALKYL CYCLE OR TOGETHER WITH THE NCI FORM. AND R IS -NR3R4, WHERE R3 AND R4 ARE INDEPENDENTLY H, ALKYL (C1-C4) STRAIGHT OR BRANCHED; WHICH INCLUDES IN THE REACTION OF A COMPOUND OF FORMULA 2 ALSO KNOWN AS MINOCINE OR A DERIVATIVE, WITH AT LEAST ONE NITRANT AGENT, GIVING AS A RESULT A SUBSTITUTE -NO2, FORMING A COMPOUND OF FORMULA 3, WHERE THE SUBSTITUTE -NO2 IS REDUCED AN AMINO THROUGH A HYDROGENATION, WHERE THE REDUCTION AGENT IS PROVIDED IN THE PRESENCE OF AT LEAST ONE CATALYST CONTAINING PALADIUM, FORMING A 9-AMINOMINOCICLINE, AND FINALLY THE ACILATION OF THIS COMPOUND GENERATING IN THIS FORM TIGECYCLIN. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION INCLUDING SUCH COMPOUNDS |