The invention provides 2-(substituted phenylhetero) aromatic formate FTO inhibitors, a preparation method thereof, and applications thereof. Specifically, disclosed in the present invention are a 2-(substituted phenylhetero) aromatic formate compound represented by the following formula (I), and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, which can be used as an FTO targeting inhibitor for treating diseases associated with FTO targets, including obesity, metabolic syndrome (MS), type 2 diabetes (T2D), Alzheimer's diseases, and cancers such as breast cancers, small-cell lung cancers, human bone marrow rhabdomyosarcoma, pancreatic cancer, malignant glioblastoma and the like.

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The invention relates to the chemical synthesis of pharmaceutical API, and specifically to a method of synthesizing diclofenac sodium, which is a kind of nonsteroidal anti-inflammatory drug for relieving pain. The method includes: nitrating phenylacetate to prepare o-nitrophenylacetate (2); hydrogenating o-nitrophenylacetate (2) to prepare o-aminophenylacetate (3); amidating an amino group of o-aminophenylacetate (3) to obtain 2-(2-benzoylaminophenyl) acetate (4); 2-(2-benzoylaminophenyl) acetate (4) reacting with thionyl chloride to prepare a chloroimine intermediate, and then condensing the intermediate of chloroimine with 2,6-dichlorophenol using an inorganic base to prepare (E)-methyl-2-(2-((2,6-dichlorophenoxy)(phenyl)methyleneamino) phenyl ester (5); subjecting (E)-methyl-2-(2-((2,6-dichlorophenoxy)(phenyl)methyleneamino) phenyl ester (5) to Chapman rearrangement to afford methyl 2-(2-(N-(2,6-dichlorophenyl)benzoylamino)phenyl) ester (6); and hydrolyzing methyl 2-(2-(N-(2,6-dichlorophenyl)benzoylamino)phenyl) ester (6) to provide the target compound as of diclofenac sodium API. The overall yield is up to 67% based on methyl phenylacetate.

The invention relates to the chemical synthesis of pharmaceutical API, and specifically to a method of synthesizing diclofenac sodium, which is a kind of nonsteroidal anti-inflammatory drug for relieving pain. The method includes: nitrating phenylacetate to prepare o-nitrophenylacetate (2); hydrogenating o-nitrophenylacetate (2) to prepare o-aminophenylacetate (3); amidating an amino group of o-aminophenylacetate (3) to obtain 2-(2-benzoylaminophenyl) acetate (4); 2-(2-benzoylaminophenyl) acetate (4) reacting with thionyl chloride to prepare a chloroimine intermediate, and then condensing the intermediate of chloroimine with 2,6-dichlorophenol using an inorganic base to prepare (E)-methyl-2-(2-((2,6-dichlorophenoxy)(phenyl)methyleneamino) phenyl ester (5); subjecting (E)-methyl-2-(2-((2,6-dichlorophenoxy)(phenyl)methyleneamino) phenyl ester (5) to Chapman rearrangement to afford methyl 2-(2-(N-(2,6-dichlorophenyl)benzoylamino)phenyl) ester (6); and hydrolyzing methyl 2-(2-(N-(2,6-dichlorophenyl)benzoylamino)phenyl) ester (6) to provide the target compound as of diclofenac sodium API. The overall yield is up to 67% based on methyl phenylacetate.

The present invention provides methods for producing cannabinoid prodrugs. Also described are pharmaceutically acceptable compositions of the prodrugs and a system for the large-scale production of the prodrugs.

The present invention provides methods for producing cannabinoid prodrugs. Also described are pharmaceutically acceptable compositions of the prodrugs and a system for the large-scale production of the prodrugs.

The present disclosure discloses a method for synthesizing quinolones intermediates by a continuous flow reaction. Specifically, according to the method, a microchannel reactor is used, which improves the selectivity and conversion rate of the reaction, and the conversion rate of compound ii is increased to more than 95% and the yield is increased to more than 85%; avoids the use of a solvent such as methanol, and methyl tert-butyl ether, etc., in the intermittent reaction process, which simplifies the post-processing method, shortens the overall operation time from about 24 hours to a few minutes, greatly improving the production efficiency, and realizing the continuity and automation of the whole process; and thus makes the product have high purity and high yield, which is suitable for industrial production.

The present disclosure discloses a method for synthesizing quinolones intermediates by a continuous flow reaction. Specifically, according to the method, a microchannel reactor is used, which improves the selectivity and conversion rate of the reaction, and the conversion rate of compound ii is increased to more than 95% and the yield is increased to more than 85%; avoids the use of a solvent such as methanol, and methyl tert-butyl ether, etc., in the intermittent reaction process, which simplifies the post-processing method, shortens the overall operation time from about 24 hours to a few minutes, greatly improving the production efficiency, and realizing the continuity and automation of the whole process; and thus makes the product have high purity and high yield, which is suitable for industrial production.

The present invention provides a fluorine-containing liquid crystal polymer of Formula (1). The present invention also discloses a fluorine-containing liquid crystal elastomer, which comprises a copolymer of a fluorine-containing liquid crystal polymer of Formula (1) with a near-infrared dye of Formula (2). The fluorine-containing liquid crystal elastomer of the present invention shrinks due to the photothermal conversion effect of the material under the irradiation of near-infrared light, and thus is widely applicable to the field of actuators. The fluorine-containing liquid crystal polymer of the present invention introduces fluorine-containing segments into the cross-linked network of the liquid crystal polymer, to improve the mechanical performance of the material, and greatly extend the service time of light-controlled actuators.

The present invention provides a fluorine-containing liquid crystal polymer of Formula (1). The present invention also discloses a fluorine-containing liquid crystal elastomer, which comprises a copolymer of a fluorine-containing liquid crystal polymer of Formula (1) with a near-infrared dye of Formula (2). The fluorine-containing liquid crystal elastomer of the present invention shrinks due to the photothermal conversion effect of the material under the irradiation of near-infrared light, and thus is widely applicable to the field of actuators. The fluorine-containing liquid crystal polymer of the present invention introduces fluorine-containing segments into the cross-linked network of the liquid crystal polymer, to improve the mechanical performance of the material, and greatly extend the service time of light-controlled actuators.

A compound of general formula I

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wherein A is selected from the group of an unbranched or branched alky group with 1 to 12 carbon atoms, an R.sup.1OR.sup.2 group, an R.sup.1Si(R.sup.3R.sup.4R.sup.5) group, an R.sup.1OSi(R.sup.3R.sup.4R.sup.5) group, a C(O)OR.sup.9Si(R.sup.3R.sup.4R.sup.5) group, a CH(OR.sup.6)(OR.sup.7) group, an R.sup.1CH(OR.sup.6)(OR.sup.7) group, or an R.sup.1OC(O)OR.sup.8 group; SG is a protective group; R.sup.1 is a divalent hydrocarbon residue with 1 to 12 carbon atoms; R.sup.2 is a monovalent hydrocarbon residue with 1 to 12 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 each independently are a monovalent hydrocarbon residue with 1 to 12 carbon atoms; R.sup.6 and R.sup.7 each independently are a monovalent hydrocarbon residue with 1 to 12 carbon atoms; R.sup.8 is a monovalent hydrocarbon residue with 1 to 12 carbon atoms; and R.sup.9 is a divalent hydrocarbon residue with 1 to 12 carbon atoms.