New process for the synthesis of imidazo rifamycins

Details New process for the synthesis of imidazo rifamycins New process for the synthesis of imidazo rifamycins

C - Chemistry, Metallurgy

07

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260/235.82

C07D 498/18 (2006.01) A61K 31/435 (2006.01) C07D 498/10 (2006.01) C07D 498/22 (2006.01) C07H 15/24 (2006.01) C07H 19/00 (2006.01)

Patent

CA 1215976

ABSTRACT A process for the synthesis of imidazo rifamycins of for- mula Image wherein R is hydrogen or acetyl, R1 and R2 independently re- present hydrogen, (C1-4)-alkyl, benzyloxy, mono- or di-(C1-3)- -alkylamino-(C1-4)-alkyl, (C1-3)-alkoxy-(C1-4)-alkyl, hydroxy- -(C1-4)-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 1 or 2 methyl or ethyl groups. The process comprises reacting the rifamycin S of formula Image II with a 2-aminopyridine of formula Image III wherein R1 and R2 have the above seen meanings.

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