Rhone-Poulenc Sante

Rhone-Poulenc Agrochimie

Rhone-Poulenc Rorer S.a.

Jean-Pierre Corbet

Jean-Marc Paris

Daniel Farge

Claude Cotrel

Jean-Claude Barriere

Michel Mulhauser

Jean-Louis Clavel

Bernard Botannet

Michel Arnaud

Xavier Radisson

Salts derived from 26-(dialkylaminoalkylsulphonyl)pristinamycin IIB

The invention relates to an N-sulfomethylglycinate of formula:

N-sulfomethylglycinate, use in the preparation of herbicides of the

Process for the preparation of N-sulfomethylglycinate

The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl,

3-phenyl-2-propeneamine derivatives, their preparation and composition

Preparation of intermediates for herbicides of formula ##STR1## by the reaction of organic phosphites with benzoxazines of formula

Preparation of herbicides containing a phosphonate group from

The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.7 =H or alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl or benzoyl, optionally substituted by one or two halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 groups, (ii) or Y and A together form a 1-hydroxycycloalkyl radical, the ring of which contains 5 or 6 C, optionally joined to a benzene ring, it being understood that the alkyl radicals and alkyl parts contain 1 to 4 C as a straight or branched chain, and that the invention relates to all the possible geometric and optical isomers as well as their mixtures. These compounds are useful as antidepressants.

3-phenyl-2-propeneamine derivatives, their preparation and compositions

The invention provides new synergistine derivatives of the formula: ##STR1## in which Y=H or N(CH.sub.3).sub.2 and (a) R.sub.1 and R.sub.2 =H and R=pyrrolidin-3-ylthio or piperidin-3-ylthio or piperidin-4-ylthio (optionally substituted by alkyl), or altenatively R=alkylthio substituted by 1 or 2 SO.sub.3 H radicals or alkylamino or dialkylamino radicals (optionally substituted) or by 1 or 2 piperazino rings (optionally substituted) or morpholino, thiomorpholino, piperidino, pyrrolidin-1-yl, piperidin-2-yl, piperidin-3-yl or piperidin-4-yl or pyrrolidin-2-yl or pyrrolidin-3-yl rings (these last 5 rings being optionally substituted by alkyl), or

Synergistine derivatives having anti-bacterial activity and their use

The invention provides new synergistine derivatives of the formula: ##STR1## in which Y=H or N(CH.sub.3).sub.2 and R represents: (a) H or OH,

Synergistine derivatives and their preparation

The invention provides novel synergistine derivatives of the formula: ##STR1## in which Y=H or N(CH.sub.3).sub.2 : and R.sub.1 =H and R.sub.2 =OH or alkyl optionally substituted by COOH, alkoxycarbonyl or OH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R.sub.2 =cycloalkyl (of 3 to 7 carbons) or a heterocycle chosen from azetidine, pyrrolidine, piperidine or azepine (optionally substituted on the nitrogen by alkyl), or R.sub.1 =formyl or alkylcarbonyl and R.sub.2 =alkyl substituted by COOH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R.sub.2 is a heterocycle as defined above, or R.sub.1 and R.sub.2, which are identical or different, represent alkyl optionally substituted by COOH, alkoxycarbonyl, OH, alkylamino, or dialkylamino of which the alkyl radicals can form a heterocycle, or R.sub.1 and R.sub.2 form an azetidine, pyrrolidine, piperidine, morpholine or piperazine ring (optionally substituted by alkyl), all the alkyls having 1 to 5 carbon atoms. These compounds are useful as antibacterial agents.

Synergistine derivatives, their preparation and pharmaceutical

1,2,3,4-Tetrahydro-4-quinolinone of formula: ##STR1## are prepared from a 3-anilinopropionic acid of formula: ##STR2## which is treated successively with phosgene, phosgene in the presence of dimethylformamide, a Lewis acid or a strong acid, and a base. In the formula (I) and (II), R denotes a hydrogen atom, a halogen atom or an alkyl (1 to 4 carbon atoms) or alkoxy (1 to 4 carbon atoms) radical, and R.sub.1 denotes a hydrogen atom or an alkyl radical (1 to 4 carbon atoms). The compounds of formula I are useful as intermediates in the production of known drugs.

Process for the preparation of 4-quinolinones

The invention provides new pristinamycin II.sub.B derivatives of the formula: ##STR1## in which R represents alkylthio substituted by (i) alkylamino or dialkylamino of which the alkyl parts can form a pyrrolidin-1-yl, piperidino, azetidin-1-yl, azepin-1-yl, morpholino, thiomorpholino or piperazin-1-yl ring (optionally substituted by alkyl), or (ii) pyrrolidin-2-yl or pyrrolidin-3-yl, piperidin-2-yl, piperidin-3-yl or piperidin-4-yl, azetidin-2-yl or azetidin-3-yl or azepin-2-yl, azepin-3-yl or azepin-4-yl;

Pristinamycin derivatives, their preparation and their use

1,2,3,4-Tetrahydro-4-quinolinones of the formula ##STR1## are prepared from a 3-anilinopropionic acid of general for formula ##STR2## which is treated successively with phosgene, with a base or by heating, and then with a Lewis acid or a strong acid. In the formulae (I) and (II), R denotes a hydrogen atom, a halogen atom, an alkyl radical (1 to 4 carbon atoms) or an alkoxy radical (1 to 4 carbon atoms), and R.sub.1 denotes a hydrogen atom or any alkyl radical (1 to 4 carbon atoms). The compounds of formula I are useful as intermediates in the production of known drugs.

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Ecully, France

Jean-Pierre Corbet