Process for the synthesis of pyrido-imidazo- rifamycins

Details Process for the synthesis of pyrido-imidazo- rifamycins Process for the synthesis of pyrido-imidazo- rifamycins

C - Chemistry, Metallurgy

07

D

260/235.82

C07D 498/22 (2006.01) A61K 31/435 (2006.01) C07D 491/22 (2006.01) C07D 498/00 (2006.01) C07D 498/10 (2006.01) C07H 15/26 (2006.01)

Patent

CA 1218650

ABSTRACT OF THE DISCLOSURE A new process for the synthesis of pyrido-imidazo- rifamycins of formula Image I wherein R is hydrogen or acetyl, R1 and R2 independently repre- sent 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, mer- capto, (C1-4)-alkylthio, phenylthio, carbamoyl, mono- or di-(C1- 4)-alkyl-carbamoyl, or R1 and R2 taken together with two consecu- tive 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 Image II with a 2-aminopyridine of formula Image III wherein R1 and R2 have the same meanings as before, in presence of a suitable oxidizing agent.

491511

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