SEEN TO PROMOTE NEW DERIVATIONS OF 3-FORMYLRIFAMYCIN SV

摘要

1336399 3-Formylrifamycin SV derivatives GRUPPO LEPETIT SpA 26 April 1972 [24 June 1971] 19458/72 Heading C2A The invention comprises 3-formylrifamycin SV compounds of general Formula I wherein R 1 and R 2 are independently selected from (a) hydrogen, (b) alkyl, (c) alkenyl, (d) alkynyl, (e) aryl, (f) aralkyl, (g) heterocyclic and (h) cycloalkyl, and are further characterized in that only one of R 1 and R 2 can be hydrogen or C 1-4 alkyl, and if hydrogen or lower alkyl is present, the other of R 1 and R 2 must be unsubstituted alkyl or hydroxyalkyl of at least 5 carbon atoms or a substituted alkyl other than dimethylaminoethyl or a member of groups (c), through (h), wherein aryl is other than phenyl and p-carboxyphenyl, and aralkyl is other than benzyl and where R 3 is -H or CH 3 CO- and the 16, 17, 18, 19, 28, 29 hexahydro and 27-demethoxy-27-hydroxy derivatives thereof. A process for the preparation of compounds of Formula I comprises reacting a 3-formylrifamycin of general Formula II or the corresponding hexahydro derivative with a hydrazine of the general formula H 2 N-NR 1 R 2 wherein R 1 and R 2 are as defined above. A therapeutic composition comprises as active ingredient a compound of Formula I in conjunction with a pharmaceutically acceptable carrier.