Rifamycin XII derivatives, their preparation and anti-bacterial

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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2602393P, 424250, 424267, 424258, 424273B, A61K 31415, C07D52100

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active

043059414

ABSTRACT:
Novel rifamycin derivatives having the formula: ##STR1## wherein Y is --H or --COCH.sub.3 ; R.sub.1 and R.sub.2 may be linear or branched alkyl having from 1 to 7 carbon atoms and alkenyl having 3 or 4 carbon atoms R.sub.2 may be also chloroalkyl having from 2 to 4 carbon atoms, cycloalkyl having from 3 to 7 carbon atoms in the ring, cycloalkylalkyl having from 3 to 6 carbon atoms in the ring, phenyl, bornyl, arylalkyl hydrocarbon having 7 or 8 carbon atoms which may be substituted with one halogen atom in the aryl group; and R.sub.1 and R.sub.2 along with the N atom to which they are bonded form an unsubstituted cyclic moiety having from 5 to 8 carbon atoms, a cyclic moiety having from 5 to 8 carbon atoms substituted with 1 or 2 methyl radicals, 4-alkylpiperazine, morpholine, 1,2,3,4-tetrahydroisoquinoline. These novel compounds are yellow-orange solids having high antibacterical activity which are obtained by reacting 3-amino-4-deoxo-4-imino rifamycin S with a chloroformiminium chloride.

REFERENCES:
patent: 4086225 (1978-04-01), Marsili et al.
patent: 4164499 (1979-08-01), Rossetti et al.
patent: 4165317 (1979-08-01), Rossetti et al.
patent: 4219478 (1980-08-01), Marsili et al.
patent: 4226765 (1980-10-01), Marsili et al.

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