C07D263/22

BENZOTHIOPHENE DERIVATIVE REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
20230002364 · 2023-01-05 ·

A nitrogen-containing ring derivative regulator, a preparation method therefor and use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a G protein-coupled receptor regulator in the treatment or prevention of central nervous system diseases and/or mental diseases.

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METHODS FOR PRACTICAL SYNTHESIS OF DEUTERATED AMINO ACIDS
20230023607 · 2023-01-26 ·

Disclosed are a deuterated compound of fomula (I), or a salt thereof, and methods for preparation thereof. The present disclosure may provide a mild, versatile organophotoredox method for the preparation of diverse, enantioenriched α-deuterated α-amino acids. In particular, the present disclosure may address the long-standing challenge of installing sterically demanding side chains into α-amino acids, including late-stage modifications on medicinal agents and natural products.

OXAZOLIDINONE COMPOUNDS, LIPOSOME COMPOSITIONS COMPRISING OXAZOLIDINONE COMPOUNDS AND METHODS OF USE THEREOF

Compositions and methods for the treatment of tuberculosis, as well as other mycobacterial and gram positive bacterial infections are disclosed. These compositions contain a highly potent and selective oxazolidinone encapsulated with high efficiency to maximize dosing potential of low toxicity drugs, and are stable in the presence of plasma. The compositions are long circulating and retain their encapsulated drug while in the circulation following intravenous dosing to allow for efficient accumulation at the site of the bacterial or mycobacterial infection. The high doses that can be achieved when combined with the long circulating properties and highly stable retention of the drug allow for a reduced frequency of administration when compared to daily or twice daily administrations of other drugs typically utilized to treat these infections.

Catalysts for making oxazolidinone materials

A catalyst composition comprising at least a catalyst compound selected from multi metal cyanide compounds for the selective production of oxazolidinone compounds by reacting an isocyanate compound with an epoxide compound and oxazolidinone comprising materials obtained using said catalyst compound.

Catalysts for making oxazolidinone materials

A catalyst composition comprising at least a catalyst compound selected from multi metal cyanide compounds for the selective production of oxazolidinone compounds by reacting an isocyanate compound with an epoxide compound and oxazolidinone comprising materials obtained using said catalyst compound.

Nickel-based metal-organic framework as catalyst for chemical fixation of CO.SUB.2 .in oxazolidinone synthesis

A method of fixating CO.sub.2 to form a substituted oxazolidinone is described. The method includes mixing a nickel-based metal-organic framework (Ni-MOF) catalyst of formula [Ni.sub.3(BTC).sub.2(H.sub.2O).sub.3].Math.(DMF).sub.3(H.sub.2O).sub.3, a cocatalyst, an aromatic amine, and at least one epoxide to form a reaction mixture, and further contacting the reaction mixture with a gas stream containing carbon dioxide to react the carbon dioxide in the gas stream with the epoxide and the aromatic amine to form a substituted oxazolidinone mixture. The method further includes adding a polar protic solvent to the substituted oxazolidinone mixture, centrifuging, and filtering to produce a recovered Ni-MOF; and further washing the recovered Ni-MOF with an organochloride solvent and drying for at least 5 hours to produce a recycled Ni-MOF.

Nickel-based metal-organic framework as catalyst for chemical fixation of CO.SUB.2 .in oxazolidinone synthesis

A method of fixating CO.sub.2 to form a substituted oxazolidinone is described. The method includes mixing a nickel-based metal-organic framework (Ni-MOF) catalyst of formula [Ni.sub.3(BTC).sub.2(H.sub.2O).sub.3].Math.(DMF).sub.3(H.sub.2O).sub.3, a cocatalyst, an aromatic amine, and at least one epoxide to form a reaction mixture, and further contacting the reaction mixture with a gas stream containing carbon dioxide to react the carbon dioxide in the gas stream with the epoxide and the aromatic amine to form a substituted oxazolidinone mixture. The method further includes adding a polar protic solvent to the substituted oxazolidinone mixture, centrifuging, and filtering to produce a recovered Ni-MOF; and further washing the recovered Ni-MOF with an organochloride solvent and drying for at least 5 hours to produce a recycled Ni-MOF.

Method of fixating carbon dioxide to substituted oxazolidinones

A method of fixating carbon dioxide (CO.sub.2) to a substituted oxazolidinone. The method includes mixing a metal-organic framework (MOF), a co-catalyst, at least one para-substituted aromatic amine, and at least one epoxide to form a mixture. The method further includes contacting the mixture with a gas stream containing CO.sub.2 to react the CO.sub.2 in the gas stream with the epoxide and para-substituted aromatic amine to form a substituted oxazolidinone mixture. The MOF is a UiO-66-X MOF, where X is of formula (I) wherein at least one of R.sup.1 to R.sup.4 is an allyloxy group, and R.sup.1 to R.sup.4 are independently an allyloxy group or a hydrogen. ##STR00001##

Method of fixating carbon dioxide to substituted oxazolidinones

A method of fixating carbon dioxide (CO.sub.2) to a substituted oxazolidinone. The method includes mixing a metal-organic framework (MOF), a co-catalyst, at least one para-substituted aromatic amine, and at least one epoxide to form a mixture. The method further includes contacting the mixture with a gas stream containing CO.sub.2 to react the CO.sub.2 in the gas stream with the epoxide and para-substituted aromatic amine to form a substituted oxazolidinone mixture. The MOF is a UiO-66-X MOF, where X is of formula (I) wherein at least one of R.sup.1 to R.sup.4 is an allyloxy group, and R.sup.1 to R.sup.4 are independently an allyloxy group or a hydrogen. ##STR00001##

Necrosis inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.