Pristinamycin II.sub.B derivatives of formula I in which R represents: ##STR1## either a 4- to 7-membered nitrogen-containing heterocyclic radical, optionally containing 1 or more other hetero atoms chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form, and unsubstituted or substituted by alkyl, or alkyl of 2 to 4 carbon atoms, substituted by 1 or 2 radicals chosen from phenyl, cycloalkylamino or N-alkyl-N-cycloalkylamino having 3 to 6 ring carbon atoms, alkylamino, dialkylamino or dialkylcarbamoyloxy (the alkyl parts of these last 2 radicals being optionally joined to form, with the nitrogen atom to which they are attached, a 4- to 7-membered saturated or unsaturated heterocycle optionally containing another hetero atom chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form, and unsubstituted or substituted by alkyl) or a said alkyl substituted by one or more 4- or 7-membered nitrogen-containing heterocycles optionally containing 1 or 2 other hetero atoms chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form and unsubstituted or substituted by an alkyl radical, the said heterocycles being attached to the alkyl via a carbon atom, at least one of the substituents carried by the alkyl being a nitrogen-containing substituent capable of forming salts, or a [(S)-1-methyl-2-pyrrolidinyl]methyl radical, the aforesaid alkyl radicals being straight-chain or branched and containing, unless otherwise stated, 1 to 10 carbon atoms each, including isomeric forms thereof and mixtures thereof, and the salts thereof, are made by oxidizing a pristinamycin II.sub.B derivative of formula II ##STR2## with potassium peroxymonosulphate.
公式I中,R代表:##STR1##
其中,一个4-至7元素的含氮杂环基团,可选地含有1个或多个其他杂原子,包括从氮、氧和
硫中选择的在亚
磺酸或砜形式下的原子,并且未取代或由烷基或2至4个碳原子的烷基取代,取代基为苯基、环状烷基
氨基或N-烷基-N-环状烷基
氨基,具有3至6个环碳原子,烷基
氨基,二烷基
氨基或二烷基碳酰氧基(这两个基团的烷基部分可以选择与它们所附着的氮原子结合,形成4至7元饱和或不饱和的杂环,该杂环可选地包含另一个从氮、氧和
硫中选择的杂原子,在亚
磺酸或砜形式下,未取代或取代为烷基),或者一个该烷基取代物,该取代物取代为一个或多个4-或7元素的含氮杂环,可选地含有1或2个其他从氮、氧和
硫中选择的杂原子,在亚
磺酸或砜形式下,未取代或取代为烷基基团,该杂环通过碳原子连接到烷基上,烷基所携带的取代基中至少有一个是能够形成盐的含氮取代基,或者一个[(S)-1-甲基-2-
吡咯烷基]甲基基团,上述烷基基团是直链或支链的,并且每个含1至10个碳原子,包括其同分异构体和混合物,以及它们的盐,是通过将公式II的priSTinamycin II.sub.B衍
生物氧化而制得:##STR2##,其中,KHSO5是过
硫酸钾。