Abstract: A method for the formation of intramolecular amide bonds by the action of cyanogen, under mild reaction conditions, in the preparation of cyclic amides, including lactams, in biologically active compounds. A compound containing at least one carboxylic acid group and at least one primary or secondary amino group is reacted with cyanogen to form an intramolecular amide bond. The method has utility in the synthesis of B-lactam antibiotics, such as penicillins, cephalosporins, and their derivatives, in enzyme modification, in cyclization of peptides, and in covalent cross-linking of proteins.

Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.

Abstract: The invention relates to the preparation of an ester or an amide from an anhydride with an alcohol or an amine, wherein the anhydride is first prepared by reacting an acid and an alkyl chloroformate in a 100% aqueous medium, that is, 100% water.

Abstract: A process for the preparation of 2-chloro-6-haloquinoxaline compounds from the corresponding 4-halo-2-nitroaniline utilizing four reaction steps with generally compatible solvents and reagents with volatile by-products to minimize the isolation and purification of intermediates has been developed.

Abstract: The present disclosure is concerned with a process of reacting a solid aromatic amine with liquid acetic anhydride to yield a solid amide. The amine is in a flowable particulate form and it is subject to sufficient agitation during the reaction to prevent agglomeration. The amide is recovered as a flowable particulate by evaporation of the acetic acid by product and any excess acetic anhydride.

Abstract: The invention relates to a novel process for preparing chloroacetanilides of the formula ##STR1## wherein: R.sub.1 and R.sub.2 represent independently from each other a hydrogen atom or a C.sub.1-8 alkyl or C.sub.1-8 alkoxy group; andR.sub.3 stands for a straight chained or branched C.sub.1-8 alkoxy group.Said process is characterized by chloroacetylating a 2,6-dialkylaniline of the formula ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, at a temperature of 10.degree. to 120.degree. C., optionally in a solvent medium in the presence of an acid binding agent, then reacting a thus-obtained intermediate with chloromethyl chloroformiate or, alternatively, reacting a compound of the formula (II) first with chloromethyl chloroformiate and subjecting then to chloroacetylation, thereafter reacting a thus-obtained intermediate with an alcohol of the formulaR.sub.3 --OH (III),wherein R.sub.

Abstract: The present invention relates to itaconamide compounds of the formula ##STR1## wherein R is hydrogen, alkyl, aryl, alkaryl, or aralkyl and to a method of preparing the subject compounds which comprises preparing a mixed anhydride of 2-methylenesuccinamic acid and reacting the mixed anhydride with a compound of the formula RNH.sub.2, wherein R is as previously defined, to provide the corresponding itaconamide compound.

Abstract: A new process for the preparation of the 1-(4-chloro-benzoyl)-5-methoxy-2-methyl-3-indolyl-acetohydroxamic acid, which comprises reacting the reaction product of 1-(4-chloro-benzoyl)-5-methoxy-2-methyl-3-indolyl-acetic acid and an alkyl-halocarbonate, with hydroxylamine.

Abstract: Alkyl amides have been synthesized from cyclic anhydrides, carboxyl acids and their esters by contacting them with an amine carbamic acid salt.

Abstract: N,N,N',N'-tetraacetylethylenediamine (TAED) is made by an improved multicyclic process, which comprises, in each cycle, the steps of reacting N,N'-diacetylethylenediamine (DAED) with acetic anhydride and thereby forming a reaction mixture of N,N,N',N'-tetraacetylethylenediamine and acetic acid and anhydride, and distilling off acetic acid and working up the distillation residue to give substantially pure N,N,N',N'-tetraacetylethylenediamine, and in which the molar ratio of DAED:acetic anhydride in each cycle is at least 1:6.

Abstract: Carboxylic amides can be produced simply and in good yield by reacting primary alcohols with at least one compound selected from ammonia, primary amines, and secondary amines, in the presence of a molecular oxygen-containing gas and a palladium or platinum catalyst under oxidative conditions.

Abstract: A process for the manufacture of a substantially isomerically pure acylanilide of the structure ##STR1## where R is hydrogen, lower alkyl, hydroxy-lower alkyl or lower alkoxy-lower alkyl;R.sub.1 is lower alkyl, phenyl, lower alkylphenyl, lower alkoxy, lower alkoxyphenyl, chlorophenyl, nitrophenyl, dichlorophenyl, chloro-lower alkyl, cyano-lower alkyl, lower alkyl amino, sulfamoylphenyl, carbamoylphenyl or lower alkoxy-lower alkyl; andX is --CO-- or --SO.sub.2 --;comprising the step of treating an alcohol solution of a diamino compound of the structure ##STR2## with an acylating agent, to give an alcohol solution of the acylanilide, wherein substantially equivalent amounts of the acylating agent and the diamino compound are used and wherein the treatment is carried out by the slow, drop-wise addition of the acylating agent at a temperature in the range of about 0.degree. to 5.degree. C.

Abstract: The present invention relates to a process for producing a 2-amino 4-acylaminophenyl ether by acylation of a 2,4-diaminophenyl ether with a good selectivity.

Abstract: 1,2,3,4-Tetrahydro-1,5-benzodiazocines having the following formula ##STR1## in which R.sup.1 is a hydrogen, alkyl radical having at most 6 carbon atoms, methoxyethyl, or benzyl radical,R.sup.2 is a halo, hydroxyl, acetoxy or benzoxy radical,R.sup.3 is a phenyl, 2-methylphenyl, 2-chlorophenyl, 2-bromophenyl, 2-fluorophenyl, 2-nitrophenyl, 2-(trifluoromethyl)phenyl, 3-(trifluoromethyl)phenyl, 2,3-dichlorophenyl, 2,4-dichlorophenyl, 2,6-dichlorophenyl, 3,4-dichlorophenyl, 3,4-dimethoxyphenyl, or 3,4,5-trimethoxyphenyl radical,R.sup.4 is a hydrogen, chloro, fluoro, bromo, trifluoromethyl, methyl, methoxy, or methylthio radical, andR.sup.5 is a hydrogen or methoxy radical, or R.sup.4 and R.sup.5 together are an ethylendioxy radical, or an acid addition salt of the said benzodiazocine, and processes of making the same are described.