Abstract: The invention relates to a novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protected aromatic amine; and removing the N-protecting group therefrom.

Abstract: A process for the preparation of hydroxy-diphenylamines by condensation of dihydroxybenzene with an excess amount of primary aromatic amine in the presence of a catalytic amount of an acid at elevated temperature is described wherein the excess aromatic amine and, if appropriate, the reaction product is distilled off from the reaction mixture in the presence of a base.

Abstract: Perfluoroalkyl compounds containing ether groups have the formulaR.sub.f R.sub.1 SCH.sub.2 CH.sub.2 O T Zwherein R.sub.f is a perfluoroalkyl, R.sub.1 is alkylene or alkyleneoxy or aminoalkylene, T is alkylene, and Z is hydrogen; hydroxy; NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 each is alkyl or together with nitrogen form a heterocyclic ring; N.sup.+ R.sub.3 R.sub.4 (R.sub.5)X.sub.z.sup.-y, where R.sub.5 is hydrogen, oxide, alkyl, or substituted alkyl, X is an anion, and y is 1 or 2; z is 0 or 1 or is --OCH.sub.2 CH.sub.2 SR.sub.1 R.sub.f ; can be prepared directly by free-radical catalyzed addition of a perfluoroalkylthiol to a vinyl ether or subsequent reaction. These compounds are useful as surfactants and oil spill collecting agents.

Abstract: Disclosed herein are monomeric compounds having the formula: ##STR1## wherein: R and R.sup.1 are independently hydrogen, halide or alkyl;R.sup.2 and R.sup.3 are independently hydrogen, alkyl, cycloalkyl, aryl or aralkyl;q is 0 or 1; andAr is arylene, and a method of preparing same.These monomers can be homopolymerized or copolymerized with one or more other monomers to yield polymers having desirable solubility characteristics. In particular, copolymerizable ethylenically unsaturated monomers can comprise aldehyde-containing vinylaryl ethers, to yield crosslinkable polymers useful in relief image materials or as binders in photographic layers.

Abstract: 2-acetamidocinnamic acid and substituted 2-acetamidocinnamic acids are prepared by reacting glycine with an aromtic aldehyde in the presence of acetic anhydride and a tertiary amine and subsequently treating with water.

Abstract: New compounds of the formula ##STR1## are disclosed wherein R.sub.1 =H, linear or branched alkyl-radical with from 1 to 6 carbon atoms, cycloalkyl radical with from 3 to 6 carbon atoms, alkylphenyl radical where the phenyl group may be in turn substituted with a hydroxy or methoxy group;R.sub.2 =hydroxy, hydromethylR.sub.3 =H, alkyl with 1-4 carbon atoms, formyl, carboalkyl where the alkyl groups have 1-3 carbon atoms, carbomido group simple or mono- or di-substituted on the nitrogen atom with alkyl radicals containing 1-3 carbon atoms.The new compounds are useful in the treatment of bronchial affections. They are endowed with unique properties in that they provide the desired bronchial dilation effect without any concomitant cardiac stimulation.

Abstract: N-substituted .omega.-aminoalkanoyl-.omega.-aminoalkanoic acids and their pharmacologically-acceptable salts (with a base) are useful, e.g., in pharmaceutical-composition form for the treatment or prophylaxis of diseases which are based on inadequate performance of the pancreas, the bile and/or the liver. The compounds are prepared, e.g., by reacting an N-(mono- or di-substituted) .omega.-amino-alkanoic acid with an N-(unsubstituted or monosubstituted) .omega.-aminoalkanoic acid.

Abstract: A process for producing an aliphatic carboxylic acid and an aliphatic carboxylic acid esters ofa phenol which comprises reacting a phenol of the general formula ##STR1## wherein n is an integer of 1 to 6, m is an integer of 0 to 5, the sum of n and m is 6, and R represents hydrogen, alkyl, aryl, alkenyl, carbinol, acyl, acyloxy, formyl, carboxy, halogen, sulfo, nitro, nitroso, amino, amido, or cyano, and two or more R groups may be the same or different, and the substituents R may be bonded to each other to form a penta- or hexa-carboxylic or heterocyclic ring, and an aliphatic carboxylic acid ester or an aliphatic ether with carbon monoxide, and separating and recovering the aliphatic carboxylic acid from the reaction mixture.

Abstract: A process for .alpha.-chlorination of side chains of electronegatively substituted aromatic compounds with dichlorine monoxide.

Abstract: Novel cardiocirculatory analeptics are prepared, which are epinine esters as obtained by reacting epinine (N-methyldopamine) with branched-chain aliphatic carboxylic acids. Exemplary members are 3,4-di-O-butyrylepinine and 3,4-di-O-pivaloylepinine. These medicaments are effective also by the oral route of administration, contrary to the hitherto commonly used dopamine derivatives which are rapidly destroyed by metabolization when administered orally.

Abstract: Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.

Abstract: The present application relates to the optical resolution into optical antipodes of compounds of the formula ##STR1## as well as to salts consisting of an optical isomer of a compound of the above formula and an optical isomer of 2-aminobutanol. The optically active compounds of the above formula are employed as starting materials for the production of semisynthetic antibiotics of the cephalosporin or penicillin type.

Abstract: N-acetyl-para-aminophenyl N'-acetylaminothioalkanoates I are new analgesic compounds with greatly reduced hepatotoxic effects, when taken in overdose, relative to N-acetyl-para-aminophenol. They are prepared by reacting an N-acetylaminothioalkanoic acid IV with a reactive organic chloride V to form a mixed anhydride II and then reacting the latter with N-acetyl-para-aminophenol. The mixed anhydrides II are new and useful intermediates. Alternatively the derivatives I may be prepared by reacting the acid IV with bis-(4-nitrophenyl) sulfite to form a para-nitrophenyl N-acetylaminothioalkanoic acid ester VIII, reducing the latter to a para-aminophenyl N-acetylaminothioalkanoate VII, and acetylating this product. The esters VII and VIII are new and useful intermediates. Both reactions may pass through S-blocked intermediates, which are also new. Pharmaceutical compositions containing the derivatives I are disclosed, and also analgesic methods using them.

Abstract: Selenium compounds, and a method of their preparation, are disclosed which have a structure that renders the compounds useful in immunoassays or in competitive protein binding assays wherein either radio-labeled selenium compounds or nonradioactive selenium compounds are used respectively, with radiologic or fluorometric analysis. One class of these compounds have the generalized structural formula of: ##STR1## wherein: X is hydrogen or oxo;R.sub.1 and R.sub.2, together, are ethylene, trimethylene, or 5,6-phenylene;R.sub.3 is alkylene of 1 to 6 carbons;R.sub.4 is alkyl or isoalkyl of 1 to 6 carbons, phenyl or benzyl; orR.sub.3 and R.sub.4 together are 1,2,3-propanetriyl;And n is 1 or 2. The compounds in the aforementioned structure are N-pyrrolidine derivatives wherein R.sub.1 and R.sub.2 together are ethylene; N-succinimdyl derivatives when R.sub.1 and R.sub.2 together are ethylene and the X groups are oxo groups; N-phthalimidyl derivatives when R.sub.1 and R.sub.

Abstract: Ester age resisters such as 4-anilinophenyl acrylate and 4-anilinophenyl methacrylate, age resistant polymers having ester age resisters physically combined therewith and age resistant polymeric compositions prepared by free radical polymerization techniques involving the use of said esters as monomers.

Abstract: Fluorinated anilines, especially p-fluoroaniline and 2,4-difluoroaniline, are prepared by treating aromatic azides with anhydrous hydrogen fluoride. The aromatic azides, in turn, are prepared from the corresponding anilines by treatment with nitrous acid or salt thereof and an alkali metal azide in the presence of a mineral acid, and in an aqueous-nonaqueous, two-phase environment.

Abstract: A compound of the formula ##STR1## in which R.sub.1 denotes optionally substituted lower akyl which is optionally branched at the linking carbon atom, R.sub.2 represents hydrogen or lower alkanoyl and R.sub.3 is a group of the formula --R.sub.3.sup.a -(R.sub.3.sup.b).sub.n -- (Ia), in which R.sub.3.sup.1 represents the radical of the formula --N(R.sub.4)-- or --O-- and R.sub.4 represents hydrogen or lower alkyl, R.sub.3.sup.b denotes the radical of the formula --CH.sub.2 -- or, if R.sub.3.sup.a represents --N(R.sub.4)--, denotes the radical of the formula --C(.dbd.O)-- and n represents nought or 1, and a group of the formula Ia, in which n represents 1, can be linked to the carbonyl group of the carbamoyl grouping either via the group R.sub.3.sup.a or the group R.sub.3.sup.b, or acid addition salts thereof, which can be used pharmaceutically can be used as beta-receptor blocking agents for the treatment of disorders in the cardiac rhythm and coronary heart diseases.

Abstract: A 2-hydrazono-propionic acid derivative of the formula ##STR1## wherein R.sub.1 and R.sub.2, each independently is hydrogen, halogen, trifluoromethyl, alkyl, hydroxyl, acyloxy or alkoxy or together are methylenedioxy, andX is an aliphatic hydrocarbon radical containing 2-4 carbon atoms and is optionally substituted by an alkyl radical in the .beta.- or .gamma.-position to the nitrogen atom,Or a physiologically compatible salt, ester or amide thereof, which exhibit hypoglycaemically activity.

Abstract: A p-acetamidophenol derivative which is soluble in water giving stable aqueous solutions. This derivative is p-acetamidophenyl diethylaminoacetate, optionally in the form of a non-toxic pharmaceutically acceptable acid addition salt, particularly the hydrochloride. This derivative rapidly releases the para-acetamidophenol in the organism.

Abstract: Process for the homogeneous catalytic hydrogenation of .beta.-substituted-.alpha.-acylamido-acrylic acids which yields, after hydrogenation, an optically active mixture. The process comprises the hydrogenation of .beta.-substituted-.alpha.-acylamido-acrylic acids in the presence of an optically active coordinated metal complex hydrogenation catalyst, in which the metal is selected from the group consisting of rhodium, iridium, ruthenium, osmium, palladium and platinum.This process is a generalized process for any asymmetric hydrogenation of .beta.-substituted-.alpha.-acylamido-acrylic acids in which one .alpha.-amino acid enantiomorph is the desired end-product. It is especially useful for the preparation of .alpha.-amino acids found in nature which possess optical activity and which have a hydrogen attached to the asymmetric center.This invention also relates to new optically active coordinated metal complex hydrogenation catalysts.

Abstract: 7.beta.-[(2-Amino-1,2-dioxoethyl)amino]acyl cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl or a salt forming ion; R.sub.1 is hydrogen, lower alkyl, saturated or unsaturated cycloalkyl, phenyl, phenyl-lower alkyl, substituted phenyl or certain heterocyclic groups; R.sub.2 is hydrogen or methoxy; R.sub.3 is hydrogen, lower alkyl or cycloalkyl; and X is hydrogen, lower alkanoyloxy, carbamoyloxy, lower alkoxy, lower alkylthio ##STR2## or certain heterothio groups, are useful as antibacterial agents.

Abstract: Carboxyalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 is hydrogen, lower alkyl, phenyl, phenyl-lower alkyl, diphenyl-lower alkyl, alkali metal ion or alkaline earth metal ion; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR3## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.

Abstract: Compounds of the formula: ##STR1## wherein R represents a member selected from the group consisting of a straight or branched alkyl group of from one to twenty carbon atoms (C.sub.1 -C.sub.5 being preferred), an ethoxycarbonyl group, a benzyloxycarbonyl group, a phenyl group, an ##STR2## WHEREIN R is as defined above and R.sub.3 is a member selected from the group consisting of a hydrogen atom, a methyl group and a phenyl group, and a 2-, 3-, or 4-pyridyl group, or the HX salts thereof, wherein X represents a pharmaceutically acceptable acid addition salt anion, are extremely valuable in the treatment of conditions responsive to sympathomimetic agents.The compounds of this invention find therapeutic application to warm-blooded animals (e.g., humans) in the management of asthma, nasal congestion and as decongestants, vasoconstrictors, mydriatic agents, and anti-glaucomatous agents in the practice of opthalmology.

Abstract: Novel acyloxy-phenylethanolamines, characterized in that the acyloxy group or groups are pivaloyloxy or phenylacetyloxy and having a more prolonged sympaticomimetic action than acyloxy-phenylethanolamines known previously, are described together with a method for their manufacture by reduction of the corresponding acyloxy-phenylketo-N-benzyl amines using hydrogen in an aqueous medium over a noble metal catalyst.

Abstract: Aromatic 1,3-diketones are produced by reacting aromatic compounds with acetoacetyl fluoride optionally substituted in the .gamma.-position by fluorine, chlorine and/or bromine, in hydrofluoric acid of at least 90% strength at a temperature of from about -40.degree. to +50.degree. C. The products obtained are important starting products and intermediates for the manufacture of dyestuffs, plastics and pharmaceuticals. Furthermore they can be used for the formation of metal complexes and as metal extracting agents, solution intermediaries and solvents.

Abstract: 1,3-Bridged-2-amino tetralins, having spiro substitution or the bridge, and intermediates thereto. The final products have analgesic activity.

Abstract: Preparing indoles and intermediates therefor by reacting an N-haloaniline with a .beta.-carbonylic hydrocarbon sulfide to form an azasulfonium halide, reacting the azasulfonium halide with a strong base to form a thio-ether indole derivative, and then reducing the thio-ether indole, e.g. with Raney nickel, to form the indole compound. When an acetal or ketal of the .beta.-carbonyl hydrocarbon sulfide is used, the azasulfonium salt is treated with a base, and then with an acid to form the thio-ether indole derivative. When an .alpha.-ethyl-.beta.-carbonylic hydrocarbon sulfide is used, the resulting azosulfonium salt reacts with strong base to form a thio-ether indolenine derivative, which on reduction with Raney nickel or complex metal hydrides yields 3-substituted indoles. The aniline may be an aminopyridine to form an aza-indole compound in the process. The azasulfonium salts and thio-ether indole or thio-ether indolenine derivatives can be isolated and recovered from their respective reaction mixtures.

Abstract: Process for the manufacture of a heterocyclic compound of the formula I ##STR1## in which Y denotes a --CN, --COOR' or ##STR2## group, in which R' can be an optionally substituted alkyl or aryl radical and R" and R"' independently of one another can have the same meaning as R' or can be hydrogen or, conjointly with the nitrogen atom, can form a heterocyclic 5-membered or 6-membered ring and X denotes a --S-- or --O-- atom or a --NR"-- group and the ring A can carry non-ionic substituents or optionally substituted fused rings, wherein a nitrile of the formula IInc -- ch.sub.2 -- y (ii)is reacted, in organic solvents, with a lower alcohol of the formula IIIr -- oh (iii)using a molar ratio of nitrile to alcohol of 1:0.9 to 1:1.2, in the presence of an anhydrous strong acid at temperatures of -10.degree. to +40.degree.

Abstract: A new compound represented by the formula ##STR1## WHEREIN X represents hydrogen atom, chlorine atom, bromine atom, methyl group or nitro group, Y represents hydrogen atom, methyl group, an alkylcarbonyl group where the alkyl group has from 1 to 12 carbon atoms and may be substituted by one or more halogen atoms, a lower alkoxy carbonyl group, a lower alkylamino carbonyl group or a metal atom of which the valence is 1 or 2, Z represents hydrogen atom or chlorine atom and n represents 2 when Y represents a metal atom of which valence is 2 and n represents 1 when Y represents said group or said atom except a metal atom of which valence is 2 but when X and Z represent hydrogen atom, Y does not represent hydrogen atom or a metal atom is employed to control the growth of bacteria, fungi and algae which propagate on industrial raw materials and products or in water in circulating water systems.

Abstract: This invention relates to novel water-soluble esters of oxalic acid, and to compositions that are useful for generating chemiluminescent emission by reacting said esters of oxalic acid with hydrogen peroxide in the presence of water and a fluorescent compound, and to a process for generating chemiluminescent emission by using said compositions.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is alkyl of 6 to 19 carbon atoms, andR.sub.2 is methyl or ethyl,And their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as the salts are useful as pharmaceuticals for the treatment of cardiac and circulatory insufficiencies.

Abstract: The invention provides novel 5- and 6-benzoxazolyl alkanoic acids, optionally substituted in the 2-position, and derivatives thereof which possess anti-inflammatory, anti-pyretic and analgesic activity. Also provided is a process for preparing such compounds by cyclizing an appropriately substituted o-aminophenol and, if necessary, converting the resultant benzoxazole to the desired compound.