| 摘要 |
A process for the preparation of therapeutically useful pristinamycin IIB sulphone derivatives, of the general formula (I): (I) and their acid addition salts, in which R denotes an optionally substituted nitrogen-cotaining 4 to 7-membered heterocyclic 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): (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. |
