Patent · US Expired

Rifamycin XII derivatives, their preparation and anti-bacterial compositions thereof

US4305941A · kind A · utility

4Cited by
5References
8Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJan 5, 1981
Grant dateDec 15, 1981
Priority date
Expiry dateJan 5, 2001

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D498/22
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.