Patent classifications
C07D487/22
SOLVENT-FREE CROSS-COUPLING REACTION, AND PRODUCTION METHOD USING SAID REACTION
Disclosed is a cross-coupling reaction method which forms a chemical bond selected from C—N, C—B, C—C, C—O and C—S bonds, the method comprising: preparing an aromatic compound (1) having a leaving group; preparing a compound (2) capable of undergoing a cross-coupling reaction selected from an aromatic amino compound (2-1), a diboronic acid ester or the like (2-2), an aromatic boronic acid or the like (2-3), an aromatic compound (2-4) having a hydroxyl group and an aromatic compound (2-5) having a thiol group; and performing a cross-coupling reaction of the compound (1) with the compound (2) in the presence of a palladium catalyst, a base and a compound (4) having a carbon-carbon double bond or a carbon-carbon triple bond, in the absence of a solvent.
SOLVENT-FREE CROSS-COUPLING REACTION, AND PRODUCTION METHOD USING SAID REACTION
Disclosed is a cross-coupling reaction method which forms a chemical bond selected from C—N, C—B, C—C, C—O and C—S bonds, the method comprising: preparing an aromatic compound (1) having a leaving group; preparing a compound (2) capable of undergoing a cross-coupling reaction selected from an aromatic amino compound (2-1), a diboronic acid ester or the like (2-2), an aromatic boronic acid or the like (2-3), an aromatic compound (2-4) having a hydroxyl group and an aromatic compound (2-5) having a thiol group; and performing a cross-coupling reaction of the compound (1) with the compound (2) in the presence of a palladium catalyst, a base and a compound (4) having a carbon-carbon double bond or a carbon-carbon triple bond, in the absence of a solvent.
Method for producing ester group-containing compound
The present invention provides a novel method for producing an ester group-containing compound and a derivative produced using the compound as a synthetic intermediate. The invention also provides a polymerizable composition containing the compound obtained by the production method and a film-shaped polymer obtained by polymerizing the polymerizable composition. The present invention is a method for producing an ester group-containing compound, the method including a mixing step of mixing a condensing agent, a Bronsted acid, a carboxylic acid, and a phenol or an alcohol to prepare a reaction mixture. The Bronsted acid selected is other than the condensing agent, the carboxylic acid, and the phenol.
Method for producing ester group-containing compound
The present invention provides a novel method for producing an ester group-containing compound and a derivative produced using the compound as a synthetic intermediate. The invention also provides a polymerizable composition containing the compound obtained by the production method and a film-shaped polymer obtained by polymerizing the polymerizable composition. The present invention is a method for producing an ester group-containing compound, the method including a mixing step of mixing a condensing agent, a Bronsted acid, a carboxylic acid, and a phenol or an alcohol to prepare a reaction mixture. The Bronsted acid selected is other than the condensing agent, the carboxylic acid, and the phenol.
TETRAPYRROLIC CONJUGATES AND USES THEREOF FOR IMAGING
Compounds for tumor imaging (e g , magnetic resonance (MR) and fluorescence) that may be used in combination with other methods to treat an individual having or suspected of having cancer (e.g., various forms of cancer, such as, for example, solid tumors). Compounds may have the following structure: (I) or a salt, a partial salt, a hydrate, a polymorph, an isomer (e.g., a structural or stereoisomer), or a mixture thereof, where R′ is an aryl group or heteroaryl group having a halogen group (e.g., I or .sup.124I), X is chosen from O, S, or NH, n is 1-6 (e.g., 1, 2, 3, 4, 5, or 6), the dotted carbon is chiral and is R or S.
TETRAPYRROLIC CONJUGATES AND USES THEREOF FOR IMAGING
Compounds for tumor imaging (e g , magnetic resonance (MR) and fluorescence) that may be used in combination with other methods to treat an individual having or suspected of having cancer (e.g., various forms of cancer, such as, for example, solid tumors). Compounds may have the following structure: (I) or a salt, a partial salt, a hydrate, a polymorph, an isomer (e.g., a structural or stereoisomer), or a mixture thereof, where R′ is an aryl group or heteroaryl group having a halogen group (e.g., I or .sup.124I), X is chosen from O, S, or NH, n is 1-6 (e.g., 1, 2, 3, 4, 5, or 6), the dotted carbon is chiral and is R or S.
COMPOSITIONS AND METHODS FOR TREATING RAS-MUTANT CANCERS
The present disclosure relates generally to compositions and methods for the treatment of a RAS-mutant cancer. In particular, the present technology relates to administering a therapeutically effective amount of one or more TXNRD1 inhibitors to a subject diagnosed with, or at risk for a RAS-mutant cancer (e.g., RAS-mutant pancreatic cancer).
Heterocyclic amides useful as protein modulators
Disclosed are compounds having the formula: ##STR00001## wherein q, r, s, A, B, C, R.sup.A1, R.sup.A2, R.sup.B1, R.sup.B2, R.sup.C1, R.sup.C2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.14, R.sup.15, R.sup.16, and R.sup.17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
Heterocyclic amides useful as protein modulators
Disclosed are compounds having the formula: ##STR00001## wherein q, r, s, A, B, C, R.sup.A1, R.sup.A2, R.sup.B1, R.sup.B2, R.sup.C1, R.sup.C2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.14, R.sup.15, R.sup.16, and R.sup.17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
Di(hetero)aryl macrocyclic compound for inhibiting protein kinase activity
A di(hetero)aryl macrocyclic compound having an inhibitory effect on protein kinase activity, preparation and the use thereof. Specifically, disclosed are a di(hetero)aryl macrocyclic compound represented by formula (I), or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a racemate, a solvate, a hydrate, a polymorph, a prodrug or an active metabolite thereof, a pharmaceutical composition comprising said compound and the derivative thereof, and methods of using the same, including methods of treating cancers, pain, neurological diseases, autoimmune diseases and inflammation. ##STR00001##