C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/235.82
C07D 498/08 (2006.01) C07D 513/18 (2006.01)
Patent
CA 1061783
Abstract of the Disclosure This invention relates to a process for the preparation of a thia- zolorifamycin of the formula I Image I wherein R is hydrogen or CH3-CO- and R1 is hydrogen or CH2OH which comprises subjecting a compound of the formula III: Image III wherein R2 is alkyl, cycloalkyl, phenyl,substituted phenyl, benzyl or sub- stituted benzyl and R is a hydrogen atom or an acetyl group, to either:- (a) mild alkaline hydrolysis to form a compound of formula I in which R1 is a hydrogen atom; or to (b) reduction to form a compound of formula I in which R1 is -CH2OH. The two compounds of formula I where R is hydrogen are new and also form part of this invention. The compounds obtained by the process of this invention are useful as antibacterial agents. In particular, they possess very high antibacterial activity in vitro and in vivo against Gram positive and Gram negative microorganisms such as Staphylococcus aureus Streptococcus haemolyticus, Streptococcus faecalis, Diplococcus pneumoniae, Proteus vulgaris and Mycobacterium tuberculosis.
279466
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