Patent classifications
C07C233/15
METHOD FOR PRODUCING ANTIBODY-DRUG CONJUGATE
A method for producing a compound represented by formula (C) wherein R.sup.1 represents an amino group protected with a protecting group, the method comprising a step of subjecting a compound represented by formula (B) wherein R.sup.1 represents the same meaning as above, to intramolecular cyclization to convert the compound into the compound represented by formula (C).
##STR00001##
Method for synthesizing diclofenac sodium
A method of synthesizing diclofenac sodium, including: subjecting aniline and chloroacetic acid to amidation to obtain 2-chloro-N-phenylacetamide; subjecting 2-chloro-N-phenylacetamide and 2,6-dichlorophenol to condensation reaction to obtain 2-(2,6-dichlorophenoxy)-N-phenylacetamide; subjecting 2-(2,6-dichlorophenoxy)-N-phenylacetamide to Smiles rearrangement in the presence of an inorganic base to obtain N-(2,6-dichlorophenyl)-2-hydroxy-N-phenylacetamide; subjecting N-(2,6-dichlorophenyl)-2-hydroxy-N-phenylacetamide and thionyl chloride to chlorination to obtain N-(2,6-dichlorophenyl)-2-chloro-N-phenylacetamide; subjecting N-(2,6-dichlorophenyl)-2-chloro-N-phenylacetamide to Friedel-Crafts alkylation in the presence of a Lewis acid catalyst to obtain 1-(2,6-dichlorophenyl)-1,3-dihydro-2H-indol-2-one; and subjecting 1-(2,6-dichlorophenyl)-1,3-dihydro-2H-indol-2-one to hydrolysis in the presence of an inorganic base to obtain diclofenac sodium.
Method for synthesizing diclofenac sodium
A method of synthesizing diclofenac sodium, including: subjecting aniline and chloroacetic acid to amidation to obtain 2-chloro-N-phenylacetamide; subjecting 2-chloro-N-phenylacetamide and 2,6-dichlorophenol to condensation reaction to obtain 2-(2,6-dichlorophenoxy)-N-phenylacetamide; subjecting 2-(2,6-dichlorophenoxy)-N-phenylacetamide to Smiles rearrangement in the presence of an inorganic base to obtain N-(2,6-dichlorophenyl)-2-hydroxy-N-phenylacetamide; subjecting N-(2,6-dichlorophenyl)-2-hydroxy-N-phenylacetamide and thionyl chloride to chlorination to obtain N-(2,6-dichlorophenyl)-2-chloro-N-phenylacetamide; subjecting N-(2,6-dichlorophenyl)-2-chloro-N-phenylacetamide to Friedel-Crafts alkylation in the presence of a Lewis acid catalyst to obtain 1-(2,6-dichlorophenyl)-1,3-dihydro-2H-indol-2-one; and subjecting 1-(2,6-dichlorophenyl)-1,3-dihydro-2H-indol-2-one to hydrolysis in the presence of an inorganic base to obtain diclofenac sodium.
METHOD FOR PRODUCING N-(HETERO)ARYL (METH)ACRYLAMIDE COMPOUND
Provided is a method for producing an N-(hetero)aryl (meth)acrylamide compound, including reacting a compound represented by General Formula (1) with a compound represented by General Formula (2) at a temperature higher than 120 C. to carry out amidation and to obtain a compound represented by General Formula (3).
##STR00001##
R.sup.1 represents a hydrogen atom or an aliphatic group, R.sup.2 and R.sup.4 represent a hydrogen atom, a chain-like aliphatic group, an aliphatic hydrocarbon ring group, an aryl group, or a heterocyclic group, Ar represents an aromatic ring, R.sup.3 represents an electron withdrawing group, m represents an integer of 1 or more, and n represents an integer of 0 or more. R.sup.4 is not an -hydroxybenzyl group.
Compound for Use in Enzymatic Reaction and Mass Spectrometry Method
A compound used in the conventional enzymatic reactions and mass spectrometry methods needs to be altered with respect to the structure thereof as a substrate compound, such as the length of an alkyl chain contained therein, depending on the type of a target enzyme, and therefore has the problem that the conditions for the mass spectrometry on a product compound are undesirably varied and the sensitivity is deteriorated. In the present invention, a compound is provided, which can be used in an enzymatic reaction and a microanalysis method both for detecting a trace component stably and with high sensitivity. The compound according to the present invention is characterized by having a nitrogen atom, an amide bond and a glycosidic bond at specific sites, respectively, has high reactivity with an enzyme, and can provide a compound capable of being detected very easily with a mass spectrometer.
Compound for Use in Enzymatic Reaction and Mass Spectrometry Method
A compound used in the conventional enzymatic reactions and mass spectrometry methods needs to be altered with respect to the structure thereof as a substrate compound, such as the length of an alkyl chain contained therein, depending on the type of a target enzyme, and therefore has the problem that the conditions for the mass spectrometry on a product compound are undesirably varied and the sensitivity is deteriorated. In the present invention, a compound is provided, which can be used in an enzymatic reaction and a microanalysis method both for detecting a trace component stably and with high sensitivity. The compound according to the present invention is characterized by having a nitrogen atom, an amide bond and a glycosidic bond at specific sites, respectively, has high reactivity with an enzyme, and can provide a compound capable of being detected very easily with a mass spectrometer.
Preparation process of perfluoroalkyl compound with monohydroperfluoroalkane as starting material
A simple production process is provided of a perfluoroalkyl compound that uses monohydroperfluoroalkane as a starting material, the perfluoroalkyl compound being an important intermediate of organic electronic materials, medicine, agricultural chemicals, functional polymer materials and the like. With monohydroperfluoroalkane is reacted a base and then a carbonyl compound to produce an alcohol having a perfluoroalkyl group. For example, potassium hydroxide is made to interact with trifluoromethane, and a reaction with a carbonyl compound is induced to produce an alcohol having a trifluoromethyl group.
Preparation process of perfluoroalkyl compound with monohydroperfluoroalkane as starting material
A simple production process is provided of a perfluoroalkyl compound that uses monohydroperfluoroalkane as a starting material, the perfluoroalkyl compound being an important intermediate of organic electronic materials, medicine, agricultural chemicals, functional polymer materials and the like. With monohydroperfluoroalkane is reacted a base and then a carbonyl compound to produce an alcohol having a perfluoroalkyl group. For example, potassium hydroxide is made to interact with trifluoromethane, and a reaction with a carbonyl compound is induced to produce an alcohol having a trifluoromethyl group.
Preparation process of perfluoroalkyl compound with monohydroperfluoroalkane as starting material
A simple production process is provided of a perfluoroalkyl compound that uses monohydroperfluoroalkane as a starting material, the perfluoroalkyl compound being an important intermediate of organic electronic materials, medicine, agricultural chemicals, functional polymer materials and the like. With monohydroperfluoroalkane is reacted a base and then a carbonyl compound to produce an alcohol having a perfluoroalkyl group. For example, potassium hydroxide is made to interact with trifluoromethane, and a reaction with a carbonyl compound is induced to produce an alcohol having a trifluoromethyl group.
Radiolabeling Agents, Methods of Making, and Methods of Use Thereof
Described herein are labeling agents, specifically [.sup.11C]fluoroform, [.sup.11C]difluoromethane, [.sup.11C]fluoromethyl iodide, [.sup.11C]fluoromethyl bromide, [.sup.11C]fluoromethyl chloride, [.sup.11C]fluoromethyl trifluoromethansulfonate, [.sup.11C]difluoromethyl iodide, [.sup.11C]difluoromethyl bromide, [.sup.11C]difluoromethyl chloride, [.sup.11C]difluoromethyl trifluoromethansulfonate, [.sup.11C]trifluoromethyl iodide, [.sup.11C]trifluoromethyl bromide, [.sup.11C]trifluoromethyl chloride, [.sup.11C]trifluoromethyl trifluoromethansulfonate, [.sup.18F]fluoroform, [.sup.18F]difluoromethane, [.sup.18F]difluoromethyl bromide or [.sup.18F]trifluoromethyl bromide. Also included are methods of labeling precursors to provide labeled fluoroalkanes and imaging methods.