Rifamycin XII derivatives, their preparation and anti-bacterial

Details Rifamycin XII derivatives, their preparation and anti-bacterial Rifamycin XII derivatives, their preparation and anti-bacterial

1981-01-05

1981-12-15

Bond, Robert T.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

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

Patent

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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