Pristinamycin process

C - Chemistry – Metallurgy – 07 – D

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260/237.2

C07D 498/18 (2006.01) C07K 5/078 (2006.01)

Patent

CA 1314878

ABSTRACT OF THE DISCLOSURE: A process for the preparation of therapeutically useful pristinamycin IIB sulphone derivatives, of the general formula (I): Image (I) and their acid addition salts, in which R denotes an option- ally substituted nitrogen-cotaining 4 to 7-membered hete- rocyclic ring radical, or an optionally substituted alkyl radical of 2 to 4 carbon atoms, and n is 2, and their isomers and their mixtures comprises oxidising a compound of formula (I) as hereinbefore defined in which n is 1 or a compound of formula (II): Image (II) in which R is as hereinbefore defined, with a periodic acid salt and a catalytic amount of a ruthenium (VIII) compound. This ruthenium compound may optionally be prepared in situ by oxidation of a ruthenium compound of a lower oxidation state. Compounds of general formula (I) in which n is equal to 2 in the form of their B isomers, and certain novel compounds of general formula (I) in which n is equal to 2, produced by the above process are useful therapeutically.

541447

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