Abstract: The invention provides a new process for the preparation of solifenacin or a pharmaceutically acceptable acid addition salt thereof, comprising reacting (R)-quinuclidin-3-yl phenethylcarbamate with benzaldehyde in the presence of an acid to obtain a diasteroisomeric mixture (S,R)—((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate of formula (IV) which can be resolved and the solifenacin or a pharmaceutically acceptable acid addition salt thereof recovered. The invention also provides the new key intermediate (R)-quinuclidin-3-yl phenethylcarbamate involved in the process. Further the invention provides a method for the transformation of (R)—((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate into a diasteroisomeric mixture (S,R)—((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate.

Abstract: The invention relates to a method for the synthesis of exocyclic derivatives of cycloalkyl-hydrazines and exocyclic derivatives of heterocycloalkyl-hydrazines The invention is characterised in that the method comprises a step consisting in demixing a solution containing said synthesised derivative, by reacting a heterocyclic amine with monochloramine, in an organic phase and an aqueous phase with the addition of anhydrous sodium hydroxide. According to the invention, the starting amine which has not reacted is collected and reused directly without any additional treatment. The inventive method can also be used to obtain the corresponding exocyclic heterocycloalkyl-hydrazine or cycloalkyl-hydrazinederivative derivative at a low cost compared to that of other known methods.

Abstract: The invention relates to a method of preparing urethane-protected N-carboxyanhydrides of alpha amino acids. The inventive method enables the synthesis of urethane-protected N-carboxyanhydrides of alpha amino acids in the presence of a catalytic quantity of triethylene diamine without the addition of a tertiary amine-type base.

Abstract: The invention concerns a method for preparing poly(-hydroxy acids), the polymerization reaction being performed in controlled manner in the presence of a catalytic system including a base, said base being a 5- or 6-membered aromatic heterocycle comprising at least one endocyclic nitrogen atom, provided that when the base is used alone in the catalytic system, it does not represent pyridine, 2-methylpyridine, 2,6-dimethylpyridine or 2-methoxypyridine. The invention also concerns poly(-hydroxy acids) of formula (IV). Finally, the invention concerns the use of a poly(-hydroxy acid), obtainable by the inventive method, for vectoring active principles or for making biomaterials.

Abstract: The invention relates to a method for the continuous synthesis of monoalkyl-hydrazines with a functionalized alkyl group. The inventive method is characterized in that it comprises a step consisting in demixing a solution containing the synthesized monoalkyl-hydrazine, by reacting an anhydrous amine with monochloramine, in an organic phase and an aqueous phase with the addition of anhydrous sodium hydroxide. The invention can be used to obtain perfect selectivity in relation to monoalkyl-hydrazine without the presence of the di- and tri-substituted forms thereof. According to the invention, the staffing amine which has not reacted is collected and reused directly without any additional treatment.

Abstract: The invention relates to a compound of formula (I) wherein X represents an activating radical such as a chlorine atom or imidazoyl, Y represents a saturated aliphatic C6-C20 radical, and Z represents an aliphatic C2-C10 radical. The invention also relates to a method for synthesising the compound of formula (I), according to which the compound of formula (II) is formed by the reaction between an alcohol and an acid anhydride, and by the activation of the carbonyl function. Furthermore, the invention relates to the use of the compound of formula (I) for increasing the hydrophobic character of polymers comprising amine and/or hydroxyl functions by means of grafting, and to a support based on natural textile fibres onto which the compound of formula (I) is grafted.

Abstract: The invention relates to a method of preparing urethane-protected N-carboxyanhydrides of alpha amino acids. The inventive method enables the synthesis of urethane-protected N-carboxyanhydrides of alpha amino acids in the presence of a catalytic quantity of triethylene diamine without the addition of a tertiary amine-type base.

Abstract: According to the process of the invention, the hexahydropyridazine-3-carboxylic acid derivatives are prepared by reacting a compound of formula (II) with a compound of formula (III) in the presence of a base with a pK of greater than or equal to 8.5, in a ketone organic solvent, to obtain an intermediate compound that is not isolated and that is treated with a basic aqueous medium. By means of this process, the derivatives are obtained more quickly and more economically.

Abstract: The invention relates to a process for the preparation of an ?-benzyl ester of an amino diacid, characterized in that the amino diacid is reacted with a benzyl alcohol derivative of formula (I) in which the R1 substituent or substituents, which are identical or different, represent a hydrogen atom, a C1 to C4 alkyl group, a C1 to C4 alkoxy group or a halogen atom and n is equal to 1, 2 or 3, in the presence of at least one mol per mole of the amino diacid of an alkanesulphonic acid, optionally in the presence of a solvent. The intermediate alkanesulphonates of the ?-benzyl esters of amino diacids and the ?-benzyl esters of amino diacids are obtained with a good yield and an excellent purity by virtue of this process.

Abstract: The invention relates to a process for the synthesis of monochloramine by reaction of an ammonium chloride solution with a sodium hypochlorite solution. The sodium hypochlorite solution is basified beforehand with an inorganic base and the ratio of the concentration of ammonium chloride in the reaction medium to the concentration of sodium hypochlorite in the reaction medium is between 1 and 1.5. This ratio is preferably equal to 1.1.

Abstract: The present invention relates to a process for the selective decomposition of hydrazine in a hydrazine/substituted hydrazine/water mixture. A catalyst chosen from the group consisting of nickel supported on silica/alumina, the nickel-nickel oxide mixture supported on silica/alumina and rhodium supported on carbon is introduced into this mixture and then the mixture is heated at a temperature of between 60° C. and 120° C.

Abstract: A method for the production of aliphatic fluoroformates, wherein carbonyl fluoride is made to react with aliphatic alcohol in the presence of sodium fluoride in ether at a temperature of ?20° to 50° C. The method is carried out using carbonyl fluoride obtained by reacting phosgene with surplus powdered sodium fluoride, whereby the grains thereof have a specific surface of 0.1 m2/g or more and/or an average diameter of 20 ?m or less, at a temperature ranging from 25° to 120° C. The method enables unstable fluoroformates such as tertiobutyl to be obtained with excellent yields.

Abstract: A process for the preparation of fluoroformates of the formula wherein R1 is a saturated or unsaturated, substituted or unsubstituted and primary or secondary aliphatic, a saturated or unsaturated, substituted or unsubstituted secondary cycloaliphatic or a substituted or unsubstituted aromatic or heteroaromatic, and n is equal to 1, 2 or 3, comprising reacting a corresponding chloroformate of formula I with an alkali metal fluoride in ethylene carbonate at a temperature wherein the ethylene carbonate is liquid whereby it is possible to very rapidly obtain the fluoroformates with excellent yields and high purity.

Abstract: The invention relates to an improved process for the preparation of N-carboxyanhydrides by reaction of the corresponding amino acid or one of its salts with phosgene, diphosgene and/or triphosgene in a solvent medium, characterized in that at least a portion of the reaction is carried out under a pressure of less than 1000 mbar. The N-carboxyanhydrides are thus obtained with better yields and an improved purity.

Abstract: The invention relates to a process for the preparation of N-carboxyanhydrides by reaction of the corresponding amino acid with phosgene, diphosgene and/or triphosgene in a solvent medium, characterized in that the reaction is a least partially carried out in the presence of an unsaturated organic compound which has one or more ethylenic double bonds, one of the carbon of at least one ethylenic double bond of which is completely substituted by substituents other than halogen atoms. The N-carboxyanhydrides are thus obtained with better yields and an improved purity.

Abstract: A process for producing N-formylleucine includes reacting leucine with formamide, precipitating the N-formylleucine, once the reaction is complete, at a temperature of approximately 0° to 40° C., by mixing the reaction medium with water and an acid, so that the final pH of the mixture is approximately 2 to 3, wherein the amount of water used in between approximately 1.5 and 5 parts per part by weight of starting formamide.

Abstract: The invention relates to a process for preparing carboxamide oximes of the formula (I): in which R.sup.1 represents an aryl or heteroaromatic group, and R.sup.2 and R.sup.3 represent a hydrogen atom or groups as defined in the description, characterized by the three following steps:1) An amide of the formula (II) R.sup.1 CONHR.sup.4, with R.sup.1 having the previous meaning and R.sup.4 being a C.sub.1 to C.sub.8 alkyl group, is reacted with a chlorinating agent in order to obtain the corresponding chloroimine,2) The resulting chloroimine is then caused to react with an aminopyrazole in order to obtain a novel disubstituted amidine,3) The resulting amidine is caused to react with hydroxylamine or one of its salts.Carboxamide oximes are prepared more rapidly, and in a good yield, in this way. They are useful as synthesis intermediates, in particular for preparing photographic developing agents.

Abstract: The invention concerns a process for preparation of a polymorphic form of terphenadine having a high melting point and enhanced purity, according to which water and a raw terphenadine solution are mixed in dimethylformamide and the pure terphenadine thus precipitated is collected.The invention also concerns the product obtained.

Abstract: 2,3,5-(4H)-Trimethyl pyranone having the formula: ##STR1## which is prepared by acetylation of a ketone derived from 2-formyl-3-pentanone and preparation of 2,3,5-(1H)-trimethyl 4-pyridinone having the formula: ##STR2## by ammonolysis of the 2,3,5-(4H)-trimethyl 4-pyranone.

Abstract: The present invention is directed to a composition and method relating to the preparation of aspartyl peptides having the general formula: ##STR1## where the radical-NHR represents an amino acid or peptide group. In the method, a .beta.-monoester of aspartic acid having the general formula: ##STR2## where R.sub.1 represents a hydrocarbon-containing radical, is reacted with a .beta.-dicarbonyl compound, preferably ethylacetoacetate to protect the aspartyl amino group and form an enamine. The enamine is then coupld to an amino acid or peptide, following which any protecting groups are removed to yield .alpha.-aspartyl peptides without any .beta.-isomer. In its composition aspects, the present invention is directed to novel enamines resulting from reaction of the .beta.-monoester of aspartic acid with a .beta.-dicarbonyl compound.