Abstract: Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.

Abstract: One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.

Abstract: The present invention relates to a process for continuously preparing a mononitrated organic compound, especially a process for preparing mononitrobenzene. The invention relates more particularly to an improved continuous adiabatic process for preparing nitrobenzene.

Abstract: This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.

Abstract: An alkali metal fluoride dispersion of an alkali metal fluoride and an aprotic organic solvent is obtainable by (A) separating a liquid phase from an alkali metal fluoride dispersion comprising an alcohol solvent and an alkali metal fluoride, and mixing the separated liquid phase with an aprotic organic solvent having a boiling point of 85° C. or higher at normal pressure; (B) obtaining a mixture containing the alkali metal fluoride by (b1) concentrating the mixture containing the alkali metal fluoride to obtain a concentrated fraction and a concentrated residue; (b2) mixing a residue of the alkali metal fluoride dispersion with the concentrated fraction obtained in (b1); and (b3) separating a liquid phase from the mixture containing an alkali metal fluoride obtained in (b2) and mixing the separated liquid phase with the concentrated residue; and (C) removing the alcohol solvent from the mixture containing the alkali metal fluoride.

Abstract: A potassium fluoride dispersion essentially consisting of potassium fluoride and an aprotic organic solvent having a boiling point higher than that of methanol, which is obtainable by mixing a mixture containing potassium fluoride and 5 to 50 parts by weight of methanol per 1 part by weight of potassium fluoride with the aprotic organic solvent followed by concentrating the obtained mixture, and a process for producing a fluorine-containing organic compound comprising contacting an organic compound having at least one group capable of being substituted nucleophilically with a fluorine atom with the potassium fluoride dispersion.

Abstract: A potassium fluoride dispersion essentially consisting of potassium fluoride and an aprotic organic solvent having a boiling point higher than that of methanol, which is obtainable by mixing a mixture containing potassium fluoride and 5 to 50 parts by weight of methanol per 1 part by weight of potassium fluoride with the aprotic organic solvent followed by concentrating the obtained mixture, and a process for producing a fluorine-containing organic compound comprising contacting an organic compound having at least one group capable of being substituted nucleophilically with a fluorine atom with the potassium fluoride dispersion.

Abstract: Methods for fluorinating organic compounds are described herein.

Abstract: Disclosed herein are methods of performing microchemical reactions and electro- wetting-on-dielectric devices (EWOD devices) for use in performing those reactions. These devices and method are particularly suited for preparing radiochemical compounds, particularly compounds containing 18F.

Abstract: A substituted alkenylbenzene compound of formula (4): wherein X1 is a halogen atom, —SF5, C1-C6haloalkyl, hydroxy C1-C6haloalkyl, C1-C6alkoxy C1-C6haloalkyl, C3-C8halocycloalkyl, C1-C6haloalkoxy, C1-C3haloalkoxy C1-C3haloalkoxy, C1-C6haloalkylthio, C1-C6haloalkylsulfinyl or C1-C6haloalkylsulfonyl; X3 is a hydrogen, halogen, cyano, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6alkylthio; X4 is a hydrogen, halogen, cyano, C1-C4alkyl, C1-C4alkoxy or C1-C4haloalkoxy; R3 is —C(R3a)(R3b)R3c, where R3a and R3b are a halogen, or R3a and R3b together form a 3- to 6-membered ring together with the carbon bonding them by forming a C2-C5haloalkylene chain, and R3c is a hydrogen, halogen, C1-C5alkyl, C1-C5haloalkyl, C1-C4haloalkoxy or C1-C4haloalkylthio, with a proviso that where X1 is a fluorine, chlorine or trifluoromethyl, and X2 and X3 are hydrogen, where X1 and X2 are fluorine and X3 is a hydrogen, or where X1 and X2 are trifluoromethyl and X3 is a hydrogen, R3c is a hydrogen, chlorine, bromine, iodine,

Abstract: Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No-carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F-18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F-18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F-18]fluoro-L-dopa.

Abstract: Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18]fluoride ion derived from anhydrous [F-18](F/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me4NF, Et4NF, n-Bu4NF, (PhCH2)4NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F-18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa.

Abstract: Compounds represented by the following structural formulas can be used as photoacid generators: Such compounds are useful, for example, in fabricating arrays of polymers.

Abstract: Compounds represented by the following structural formulas can be used as photoacid generators: Such compounds are useful, for example, in fabricating arrays of polymers.

Abstract: The present invention provides an efficient, safe and cost effective way to prepare 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzenamine which is a key intermediate for the preparation of substituted pyrimidinylaminobenzamides of formula (II):

Abstract: The invention relates to methods for producing sulfonamides of formula I, wherein the variables have the designations cited in the description, by reacting m-nitro-benzoic acid chlorides of formula II with aminosulfons of formula III, under the influence of B equivalents of base IV. Said method is characterised in that, during step a) the aminosulfon of formula III is reacted with B1 equivalents of base IV, and during step b), the reaction mixture resulting from step a) is reacted with m-nitro-benzoic acid chlorides of formula II and B2 equivalents of base IV; B, B1 and B2 having the designations cited in the description.

Abstract: Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.

Abstract: The invention concerns novel catalysts for aromatic nucleophilic substitution. Said catalysts are compounds of the general formula (I), wherein: R1, R2, R3, R4, R5, and R6, identical or different, are selected among hydrocarbon radicals; the Pn's, advantageously the same, are selected among metalloid elements of column V of a period higher than nitrogen; Z is a metalloid element of column V, advantageously distinct from Pn; preferably a nitrogen (N, P, As, Sb). The invention is applicable to organic synthesis.

Abstract: A preparation process of 3-chloro-5-nitrotoluene is provided in mild conditions. It is a process for preparing 3-chloro-5-nitrotoluene, which involves the steps of reacting 2-methyl-4-nitroaniline with a chlorinating agent such as 5-butyl hypochlorite in a neutral condition to obtain 2-chloro-4-nitro-6-methylaniline and deaminating the 2-chloro-4-nitro-6-methylaniline to obtain 3-chloro-5-nitrotoluene.

Abstract: The invention provides polyfluorinated aromatic or heterocyclic compounds comprising at least three ring substituents, at least one of which comprises a sulfurpentafluoride group and at least one of which comprises a labile group; methods for their preparation are also disclosed. Preferably, the compounds comprise either two sulfurpentafluoride groups or one sulfurpentafluoride group and one other polyfluorinated group, such as a trifluoromethyl group. Said labile group preferably comprises an amino, bromo or nitro group. Said compounds are useful in the preparation of medicaments.

Abstract: The present invention relates to a continuous adiabatic process for preparing nitrochlorobenzene in the presence of phosphoric acid. The waste acid produced during the practice of the process is reconcentrated and recycled into the nitration reaction.

Abstract: A preparation process of 3-chloro-5-nitrotoluene is provided in mild conditions. It is a process for preparing 3-chloro-5-nitrotoluene, which comprises reacting 2-methyl-4-nitroaniline with a chlorinating agent such as 5-butyl hypochlorite in a neutral condition to obtain 2-chloro-4-nitro-6-methylaniline and deaminating the 2-chloro-4-nitro-6-methylaniline to obtain 3-chloro-5-nitrotoluene.

Abstract: The present invention relates to a continuous adiabatic process for preparing nitrochlorobenzene in the presence of phosphoric acid. The waste acid produced during the practice of the process is reconcentrated and recycled into the nitration reaction.

Abstract: The present invention relates to a continuous adiabatic process for preparing nitrochlorobenzene, in which the waste sulfuric acid produced during the practice of the process is reconcentrated and recycled into the nitration reaction.

Abstract: The invention relates to an optimized tubular reactor for adiabatically mononitrating aromatics, halogenated aromatics and halogenated hydrocarbons, which tubular reactor is divided into from 4 to 12 chambers by plates which have openings and effect a pressure drop of from 0.5 to 4 bar per plate.

Abstract: The present invention relates to a continuous adiabatic process for preparing nitrochlorobenzene, in which the waste sulfuric acid produced during the practice of the process is reconcentrated and recycled into the nitration reaction.

Abstract: Process for the preparation of 3-bromoanisole comprising methoxydenitrating 3-bromonitrobenzene in the presence of a phase-transfer catalyst (PTC), and the preparation of 3-bromonirtobenzene by the bromination of nitrobenzene with bromine in oleum. The methoxydenitration reagent in an alkali metal methoxide, which is selected from sodium methoxide and potassium methoxide. The amount of methoxide used is 1-1.5 mol per mol of 3-bromonitrobenzene. The alkali methoxide can be a pre-prepared solid or it can be prepared in situ, by the reaction of the corresponding alkali hydroxide and methanol. In the case when pre-prepared solid methoxide is used, the effective amount of alkali hydroxide is between 1.2-1.7 mol per mol of 3-bromonitrobenzebe. The reaction temperatures are between about 40 to 80° C., with preference to reaction temperatures of 50 to 55° C. In the case in which methoxide is prepared in situ, the effective amount of alkali hydroxide is between 2.2-2.4 mol per mol of 3-bromonitrobenzene.

Abstract: The present invention provides a process for producing halogenated benzene compounds. In the process, an organometallic compound represented by the general formula [I]: wherein M represents an R13Sn group, an R13Si group, an R13Ge group, an (R2CO2)Hg group, a ClHg group or an (R3O)2B group wherein each R1 independently represents a C1-C8 alkyl group, R2 represents a C1-C3 alkyl group or a C1-C3 haloalkyl group, R3 represents a hydrogen atom or a C1-C3 alkyl group, n represents an integer of from 0 to 4, m represents an integer of from 0 to 1, each A independently represents a fluorine atom, a nitro group, a cyano group, a C1-C8 alkyl group, a C1-C8 alkoxy group or a C2-C8 acyloxy group, and Q represents an organic residue, is reacted in a solvent with a halide ion represented by the general formula X−, under light irradiation conditions in the presence of a semiconductor catalyst with a photocatalytic activity.

Abstract: A process for the preparation of an allylic aromatic compound in which an aromatic amine is reacted first with a nitrite and then with an allylic olefin having an eliminatable terminal substituent. Novel allylic derivatives of disubstituted benzene compounds are also described.

Abstract: A process for preparing 2-chloro-4-nitroalkylbenzenes is provided which comprises a ring chlorination of 4-nitroalkylbenzenes with elemental chlorine or chlorine-releasing compounds in liquid phase and in the presence of Friedel-Crafts catalysts and specific sulphur-containing aromatic compounds as co-catalysts.

Abstract: Process for the preparation of fluorine-containing compounds by reduction in a container provided with a stirrer, the stirrer being constructed entirely or partly of a carbon material.

Abstract: A process for preparing a nitrated arene which comprises reacting an arene and nitric acid in the presence of a water tolerant Lewis acid catalyst under process conditions sufficient to form the nitrated arene and recovering the nitrated arene. Suitable Lewis acid catalysts are represented by the formula M.sup.n (A.sub.1).sub.x (A.sub.2).sub.n-x whereinM is selected from the group consisting of La, Pr, Nd, Sm, Eu, Gd, Dy, Ho, Er, Tm, Yb, Sc, Hf, Lu and Li;A.sub.1 and A.sub.2 are independently selected from a perfluoroalkylsulfonate, a fluorosulfonate, a hexafluorophosphate or a nitrate;n is the common oxidation state of M andx is 1, 2, 3 or 4 with the proviso that x is never greater than n.The catalysts of the process are isolatable from water and can be recycled for subsequent process cycles.

Abstract: Mononitrohalogenobenzenes can be prepared by mixing halogenobenzene, nitric acid, sulphuric acid and water intensively with one another, simultaneously or in succession in their total quantity, and by redispersing them at least twice in the case of continuous preparation, applying a mixing energy of 1-40 watts per liter of the overall reaction mixture, preferably 3-30 W/l, largely suppressing back-mixing in the continuous procedure, and observing adiabatic reaction conditions.

Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.

Abstract: 2-Trifluoromethyl-4-chloro-benzalchloride and 2-methyl-3-nitro-5-chlorobenzotrifluoride, are intermediates in a process of preparing 2-methyl-3-aminobenzo-trifluoride. In this process, 2-trifluoromethyl-4-chlorobenzal-chloride is prepared by chlorinating o-trifluoromethylbenzalhalide, and 2-methyl-3-nitro-5-chlorobenzotrifluoride is prepared at first by hydrogenating the 2-trifluoro-methyl-4-chlorobenzalhalide to form a 2-methyl-5-monochlorobenzotrifluoride and then by nitrating the 2-methyl-5-monochlorobenzotrifluoride. Following this process, 2-methyl-3-aminobenzotrifluoride (MA-BTF) is prepared by hydrogenating the 2-methyl-3-nitro-5-chlorobenzotrifluoride. The thus prepared 2-methyl-3-aminobenzotrifluoride is useful as an intermediate in preparing medicines, agricultural chemicals and other chemical products.

Abstract: A process for the preparation of chlorofluoronitrobenzenes and difluoronitrobenzenes, which comprises heating dichloronitrobenzene to not more than 200.degree. C. in excess with an alkali metal fluoride having a total water content of about 0.2 to about 2.5% by weight in the presence of a quaternary ammonium and/or phosphonium salt, crown ether and/or polyethylene glycol dimethyl ether as catalyst in the absence of a solvent.

Abstract: 2,3-dichloro-nitrobenzene can be prepared by nitration of 1,2-dichlorobenzene using an anhydrous mixture of phosphoric acid, sulphuric acid and nitric acid. The conditions according to the invention displace the ratio of 2,3,-dichloro-nitrobenzene and 3,4-dichloro-nitrobenzene in favor of the 2,3-isomer.

Abstract: A process for the preparation of chlorofluoronitrobenzenes in high yields, by reacting dichloronitrobenzenes with alkali metal fluorides having a water content of up to about 2.5% by weight in the presence of a quaternary ammonium and/or phosphonium salt, a crown ether and/or polyethylene glycol dimethyl ether as catalyst in the presence of an aprotic solvent, the boiling point of which is below the reaction temperature under the pressure conditions chosen, at temperatures of about 125.degree. to about 200.degree. C.

Abstract: 2-methyl-3-aminobenzo-trifluoride is prepared with high yields and high productivity by first halogenating o-trifluoromethylbenzalhalide, then secondly hydrogenating 2-trifluoromethyl-4-halogeno-benzalhalide formed by the first reaction, then thirdly nitrating 2-methyl-monohalogenobenzotrifluoride formed by the second reaction, and then fourthly hydrogenating 2-methyl-3-nitro-5-halogenobenzotrifluoride formed by the third reaction.

Abstract: A process for halogen exchange fluorination or fluoro-denitration of aromatic compounds having at least one replaceable non-fluorine halogen or nitro substituent with an anhydrous substantially molten alkali metal acid fluoride composition wherein the alkali metal is potassium, rubidium or cesium.

Abstract: A continuous process to nitrate a nitratable aromatic compound in a nitronium ion solution in a nitrator. The process comprises feeding into the nitrator nitronium ion solution of a composition within an area defined by connecting three points in a ternary phase diagram of nitric acid, sulfuric acid and water. The three points correspond to first about 82% of sulfuric acid and 18% nitric acid, secondly about 55% sulfuric acid and about 45% water and, thirdly, 100% sulfuric acid, with the nitric acid preferably being below about 3%. The nitratable aromatic compound is introduced in a manner such that a fine emulsion of hydrocarbon in the nitronium ion solution is formed with the hydrocarbon evenly distributed in the acid phase. The acid and the nitratable aromatic compound are brought into intimate contact in a plug-flow nitrator that contains mixing elements.

Abstract: A process for preparing a substituted styrene by reacting a bisarylalkyl ether in the presence of an acid catalyst is disclosed. The process is preferably used for the preparation of 4-acetoxystyrene from 4,4'-(oxydiethylidene)bisphenol diacetate and 4-methoxystyrene from 4,4'-(oxydiethylidene)bisphenol dimethyl ether. A process for preparing a bisarylalkyl ether by reacting a corresponding arylalkanol in the presence of an acid catalyst is also disclosed.

Abstract: The present invention relates to a process for producing an aromatic nitro compound by introducing a nitrogen oxide gas and ozone-containing oxygen or air into a halogenated organic solvent dissolving or suspending therein an aromatic compound, thereby subjecting the aromatic compound to nitration. By the use of a system comprising the nitrogen oxide and ozone-containing oxygen or air as the nitrating agent, the aromatic nitro compound can be produced under mild conditions without using any mineral acid. In addition, the various disadvantages due to the use of mineral acid in the conventional process can be avoided by the process of the present invention.

Abstract: A process for preparing a substituted styrene by reacting a bisarylalkyl ether in the presence of an acid catalyst is disclosed. The process is preferably used for the preparation of 4-acetoxystyrene from 4,4'-(oxydiethylidene)bisphenol diacetate and 4-methoxystyrene from 4,4'-(oxydiethylidene)bisphenol dimethyl ether. A process for preparing a bisarylalkyl ether by reacting a corresponding arylalkanol in the presence of an acid catalyst is also disclosed.

Abstract: Disclosed herein are the derivative of benzyl ether represented by the formula (I) ##STR1## which is useful as an intermediate compound of the derivatives of 1,5-diphenyl-1H-1,2,4- triazole-3-carboxamide represented by the formula (II), ##STR2## wherein R is a straight-chain alkyl group having 1 to 10 carbon atoms which is non-substituted or substituted with 1 to 19 fluorine atoms, a branched alkyl group having 3 to 10 carbon atoms which is non-substituted or substituted with 1 to 19 fluorine atoms, a cyclic alkyl group having 3 to 10 carbon atoms, an alkyl group having 1 to 3 carbon atoms which is substituted with an alicyclic structure having 3 to 7 carbon atoms, a phenyl group or an aralkyl group having 7 to 9 carbon atoms; X.sup.1 is a halogen or an alkyl group having 1 to 3 carbon atoms; X.sup.2 is a hydrogen, a halogen or an alkyl group having 1 to 3 carbon atoms; Y.sup.1 is a hydrogen or a fluorine; Y.sup.2 is a hydrogen or a fluorine; and Z is a nitro group or an amino group.

Abstract: A method of preparing 2-bromo-4,6-dinitromesitylene having only small amounts of impurities, by first mixing fuming sulfuric acid with bromomesitylene, and then adding concentrated nitric acid.

Abstract: In the preparation of 2-chloro-4-nitro-alkylbenzene by reaction of 4-nitro-alkylbenzene with elemental chlorine or chlorine-releasing compounds in the presence of a Friedel-Crafts catalyst in the liquid phase, particularly high selectivities in respect of the target compounds chlorinated exclusively in the 2-position are achieved if a dibenzo-condensed sulphur heterocycle of the formula ##STR1## having the meanings given in the description for R.sup.1 to R.sup.8, X and n, is used as co-catalyst.

Abstract: In the process for the separation of substances by cooling crystallization, the mixture remaining in the crystallizer after separation of the crystal layer is removed and the crystal layer is melted. The process is distinguished in that the mixture, which completely fills the crystallizer, is set into vibration during the process of solidification by movements of oscillation imparted to it and is left in the crystallizer until a degree of solidification of from 50% to 90% has been obtained.

Abstract: A process for producing a 4-benzoyl-5-hydroxylpyrazole of the formula III: ##STR1## which comprises reacting carbon monoxide and a 5-hydroxypyrazole of the formula II: ##STR2## with a substituted benzene of the formula I: ##STR3## in the presence of a base and a catalyst of Group VIII of the Periodic Table.

Abstract: A process for producing a 4-benzoyl-5-hydroxylpyrazole of the formula III: ##STR1## which comprises reacting carbon monoxide and a 5-hydroxypyrazole of the formula II: ##STR2## with a substituted benzene of the formula I: ##STR3## in the presence of a base and a catalyst of Group VIII of the Periodic Table.