PROCESS FOR THE SYNTHESIS OF PYRIDO-IMIDAZO- RIFAMYCINS

PROCESS FOR THE SYNTHESIS OF PYRIDO-IMIDAZO- RIFAMYCINS

A new process for the synthesis of pyrido-imidazo-rifamycins of formula I wherein R is hydrogen or acetyl, R1 and R2 independently represent hydrogen, (C1-4)-alkyl, benzyloxy, mono- or di-(C1-3)-alkylamino-(C1-4)-alkyl, (C1-3)-alkoxy-(C1-4)-alkyl, hydroxymethyl, hydroxy-(C2-4)-alkyl, cyano, halogen,...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: TAMAGNONE, GIAN F, CANNATA, VINCENZO, PIANI, SILVANO, ALPINO, RAUL R, CAMPANA, MANUELA
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
DERIVATIVES THEREOF
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SUGARS
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Beschreibung
Zusammenfassung:A new process for the synthesis of pyrido-imidazo-rifamycins of formula I wherein R is hydrogen or acetyl, R1 and R2 independently represent hydrogen, (C1-4)-alkyl, benzyloxy, mono- or di-(C1-3)-alkylamino-(C1-4)-alkyl, (C1-3)-alkoxy-(C1-4)-alkyl, hydroxymethyl, hydroxy-(C2-4)-alkyl, cyano, halogen, nitro, mercapto, (C1-4)-alkylthio, phenylthio, carbamoyl, mono- or di-(C1- 4)-alkyl-carbamoyl, or R1 and R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups. The process comprises reacting the rifamycin B of formula II with a 2-aminopyridine of formula III wherein R1 and R2 have the same meanings as before, in presence of a suitable oxidizing agent.