Patent classifications
C07C49/813
Method for aromatic fluorination
Disclosed is a fluorination method comprising providing an aryl fluorosulfonate and a fluorinating reagent to a reaction mixture; and reacting the aryl fluorosulfonate and the fluorinating reagent to provide a fluorinated aryl species. Also disclosed is a fluorination method comprising providing, a salt comprising a cation and an aryloxylate, and SO.sub.2F.sub.2 to a reaction mixture; reacting the SO.sub.2F.sub.2 and the ammonium salt to provide a fluorinated aryl species. Further disclosed a fluorination method comprising providing a compound having the structure Ar—OH to a reaction mixture; where Ar is an aryl or heteroaryl; providing SO.sub.2F.sub.2 to the reaction mixture; providing a fluorinating reagent to the reaction mixture; reacting the SO.sub.2F.sub.2, the fluorinating reagent and the compound having the structure Ar—OH to provide a fluorinated aryl species having the structure Ar—F.
Process for the halogenation at the alpha-h position of alkylarenes variously substituted on the aromatic ring
A process that allows halogenation at the alpha-H position of alkylarenes, optionally further substituted on the aromatic or heteroaromatic ring, is described.
Process for the halogenation at the alpha-h position of alkylarenes variously substituted on the aromatic ring
A process that allows halogenation at the alpha-H position of alkylarenes, optionally further substituted on the aromatic or heteroaromatic ring, is described.
Method for decreasing the concentration of a metal in a monomer composition comprising bis(benzoyl)benzene
Disclosed are methods of decreasing the concentration of a metal in a monomer composition including a bis(benzoyl)benzene, bis(benzoyl)benzene monomer compositions having a low total metal concentration, di-ketone polymers made from low metal bis(benzoyl)benzene monomers, and polymer compositions and shaped articles including the di-ketone polymers. It was surprisingly found that di-ketone polymers made by nucleophilic substitution of low metal bis(benzoyl)benzene monomers exhibit greater crystallinity, as compared with di-ketone polymers made with conventional monomers.
Method for decreasing the concentration of a metal in a monomer composition comprising bis(benzoyl)benzene
Disclosed are methods of decreasing the concentration of a metal in a monomer composition including a bis(benzoyl)benzene, bis(benzoyl)benzene monomer compositions having a low total metal concentration, di-ketone polymers made from low metal bis(benzoyl)benzene monomers, and polymer compositions and shaped articles including the di-ketone polymers. It was surprisingly found that di-ketone polymers made by nucleophilic substitution of low metal bis(benzoyl)benzene monomers exhibit greater crystallinity, as compared with di-ketone polymers made with conventional monomers.
Ketamine flow synthesis
The invention provides a method for synthesizing a compound of formula ##STR00001##
wherein each R independently represents an optionally substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy, acyl, carboxyl, hydroxyl, halogen, amino, nitro, cyano, sulfo or sulfhydryl group, in ortho, meta or para position to the cycloalkylamine moiety; R.sup.1 and R.sup.2 each independently represents a hydrogen atom, a lower alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen group, substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy group; Y represents an oxygen atom, a sulfur atom, a NH group, a NR.sup.4 group or a CH.sub.2 group; R.sup.4 represents a hydrogen atom or an alkyl, aryl or a heteroaryl group; and n and m each independently represents an integer from 1 to 5; or a pharmaceutically acceptable salt thereof; or a precursor thereof; wherein the method comprises one or more of the following steps: (a) reacting a compound of formula (II) ##STR00002##
wherein R, R.sup.3, Y, n and m are as defined above in relation to the compound of formula (I) with an oxygenating agent, a first additive and a second additive in a solvent in a fluidic network or in a batch process under thermal and/or photochemical conditions to form a compound of formula (III): ##STR00003##
wherein R, R.sup.3, Y, n and m are as defined above in relation to the compound of formula (I), (b) reacting a compound of formula (III) with a nitrogen containing nucleophile in the presence of a third additive and/or a solvent in the fluidic network or in a batch process under thermal conditions to form a compound of formula (IV): ##STR00004##
wherein R, R.sub.1, R.sub.2, R.sub.3, Y, n and m are as defined above in relation to the compound of formula (I); and/or (c) reacting a compound of formula (IV) in a fluidic network or in a batch process, optionally in the presence of a fourth additive, under thermal conditions to form a compound of formula (I); wherein one or more of steps (a), (b) and/or (c) is carried out in a fluidic network that comprises micro- and/or meso-channels having an internal dimension of from 100 μm to 2000 μm.
Ketamine flow synthesis
The invention provides a method for synthesizing a compound of formula ##STR00001##
wherein each R independently represents an optionally substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy, acyl, carboxyl, hydroxyl, halogen, amino, nitro, cyano, sulfo or sulfhydryl group, in ortho, meta or para position to the cycloalkylamine moiety; R.sup.1 and R.sup.2 each independently represents a hydrogen atom, a lower alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen group, substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy group; Y represents an oxygen atom, a sulfur atom, a NH group, a NR.sup.4 group or a CH.sub.2 group; R.sup.4 represents a hydrogen atom or an alkyl, aryl or a heteroaryl group; and n and m each independently represents an integer from 1 to 5; or a pharmaceutically acceptable salt thereof; or a precursor thereof; wherein the method comprises one or more of the following steps: (a) reacting a compound of formula (II) ##STR00002##
wherein R, R.sup.3, Y, n and m are as defined above in relation to the compound of formula (I) with an oxygenating agent, a first additive and a second additive in a solvent in a fluidic network or in a batch process under thermal and/or photochemical conditions to form a compound of formula (III): ##STR00003##
wherein R, R.sup.3, Y, n and m are as defined above in relation to the compound of formula (I), (b) reacting a compound of formula (III) with a nitrogen containing nucleophile in the presence of a third additive and/or a solvent in the fluidic network or in a batch process under thermal conditions to form a compound of formula (IV): ##STR00004##
wherein R, R.sub.1, R.sub.2, R.sub.3, Y, n and m are as defined above in relation to the compound of formula (I); and/or (c) reacting a compound of formula (IV) in a fluidic network or in a batch process, optionally in the presence of a fourth additive, under thermal conditions to form a compound of formula (I); wherein one or more of steps (a), (b) and/or (c) is carried out in a fluidic network that comprises micro- and/or meso-channels having an internal dimension of from 100 μm to 2000 μm.
Zwitterion-ruthenium complex for catalytic aerobic oxidation reactions
Zwitterion ligand metal complexes and methods of aerobic oxidation using a zwitterion ligand metal complex are provided. The zwitterion ligand metal complexes can include a transition metal salt and a zwitterion ligand, which can comprise a non-conjugated amide anion-phosphonium cation, an amide anion-ammonium cation, or an iminium cation. The methods of aerobic oxidation can include combining the zwitterion ligand metal complex with an oxidizable compound and molecular oxygen to allow the isolation of an oxidized compound from the oxidizable compound.
Zwitterion-ruthenium complex for catalytic aerobic oxidation reactions
Zwitterion ligand metal complexes and methods of aerobic oxidation using a zwitterion ligand metal complex are provided. The zwitterion ligand metal complexes can include a transition metal salt and a zwitterion ligand, which can comprise a non-conjugated amide anion-phosphonium cation, an amide anion-ammonium cation, or an iminium cation. The methods of aerobic oxidation can include combining the zwitterion ligand metal complex with an oxidizable compound and molecular oxygen to allow the isolation of an oxidized compound from the oxidizable compound.
NOVEL PROCESSES
The present invention relates to processes of preparing N-((1,2,3,4,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-1-iso-propyl-1H-pyrazole-3-sulfonamide and salts thereof. The present invention further relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.