C07C275/26

5-HT2A RECEPTOR INHIBITOR OR INVERSE AGONIST, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
20230348421 · 2023-11-02 ·

The present invention relates to a novel compound as a 5-HT.sub.2A receptor inhibitor or inverse agonist, a preparation method therefor, and a pharmaceutical composition thereof. The present invention also relates to an application of the compound or the pharmaceutical composition in the preparation of a drug for treating 5-HT.sub.2A receptor-related diseases, the diseases comprising: non-motor symptoms caused by Parkinson's disease: delusion, illusion, depression, anxiety, cognitive disorder, and sleep disorder; dementia-related mental diseases; major depressive disorder; or negative symptoms of schizophrenia, etc.

CYCLIC DIONES AS HERBICIDAL COMPOUNDS

The present invention relates to compounds of Formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4x, R.sup.4y, m, n and G are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), to their use for controlling weeds, in particular in crops of useful plants.

##STR00001##

CYCLIC DIONES AS HERBICIDAL COMPOUNDS

The present invention relates to compounds of Formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4x, R.sup.4y, m, n and G are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), to their use for controlling weeds, in particular in crops of useful plants.

##STR00001##

METHOD FOR PRODUCING HALOGENATED CARBONYL

The objective of the present invention is to provide a method for producing a halogenated carbonyl safely and efficiently. The method for producing a halogenated carbonyl according to the present invention is characterized in comprising the step of applying ultrasound to a composition containing a C.sub.1-4 halogenated hydrocarbon having one or more halogeno groups selected from the group consisting of chloro, bromo and iodo in the presence of oxygen to decompose the C.sub.1-4 halogenated hydrocarbon.

METHOD FOR PRODUCING HALOGENATED CARBONYL

The objective of the present invention is to provide a method for producing a halogenated carbonyl safely and efficiently. The method for producing a halogenated carbonyl according to the present invention is characterized in comprising the step of applying ultrasound to a composition containing a C.sub.1-4 halogenated hydrocarbon having one or more halogeno groups selected from the group consisting of chloro, bromo and iodo in the presence of oxygen to decompose the C.sub.1-4 halogenated hydrocarbon.

Coating composition comprising a thermoset resin and a thermoplastic resin

A powder coating composition comprising: a) a thermoset resin comprising an acid functional polyester material, b) a thermoplastic resin and c) a crosslinker material,
wherein the coating composition is substantially free of bisphenol A (BPA), bisphenol F (BPF), bisphenol A diglycidyl ether (BADGE) and bisphenol F diglycidyl ether (BFDGE).

Coating composition comprising a thermoset resin and a thermoplastic resin

A powder coating composition comprising: a) a thermoset resin comprising an acid functional polyester material, b) a thermoplastic resin and c) a crosslinker material,
wherein the coating composition is substantially free of bisphenol A (BPA), bisphenol F (BPF), bisphenol A diglycidyl ether (BADGE) and bisphenol F diglycidyl ether (BFDGE).

Industrial process for the preparation of cariprazine

In the process of the present invention, cariprazine is prepared by converting (trans-4-amino-cyclohexyl)-acetic acid ethyl ester hydrochloride to trans-4-aminocyclohexyl) acetic acid or its hydrochloride by hydrolysis, from the obtained product with addition of dimethylcarbamoyl derivative as a suitable reagent (trans-4-{[(dimethylamino)carbonyl]amino}cyclohexyl) acetic acid is formed, then the obtained compound is linked to 1-{2,3-dichlorophenyl)˜piperazine in the presence of carboxylic acid activating coupling reagent, and so 1,1-dimethyl-3-[trans-4-(2-oxo-2-(4-(2,3-dichlorophenyl)piperazin-1-yl-ethyl)cyclohexyl] urea is formed, which is converted to cariprazine borane adduct of formula (2) in the presence of reducing agent, and finally the product itself is eliminated directly or is obtained from its salt by a known method. The invention also relates to a group of intermediate compounds that are formed and/or used in the process according to the present invention.

HYDROXY FUNCTIONAL ALKYL POLYUREA CROSSLINKERS

A hydroxy functional alkyl polyurea is disclosed having the formula presented in claim 1, wherein R comprises an isocyanurate moiety, biuret moiety, allophonate moiety, glycoluril moiety, benzoguanamine moiety, polyetheramine moiety, and/or polymeric moiety different from a polyetheramine and having an Mn of 500 or greater; wherein each RI is independently a hydrogen, alkyl having at least 1 carbon, or a hydroxy functional alkyl having 2 or more carbons and at least one R.sub.1 is a hydroxy functional alkyl having 2 or more carbons; and n is 2-6. Further disclosed is a coating comprising: a film-forming resin; and a hydroxy functional alkyl polyurea crosslinker having the formula presented in claim 4, wherein R.sub.2 is a substituted or unsubstituted C.sub.1 to C.sub.36 alkyl group, an aromatic group, an isocyanurate moiety, biuret moiety, allophonate moiety, glycoluril moiety, benzoguanamine moiety, polyetheramine moiety, and/or polymeric moiety different from a polyetheramine having an Mn of 500 or greater, wherein each R.sub.1 is independently a hydrogen, an alkyl having at least 1 carbon, or a hydroxy functional alkyl having 2 or more carbons and at least one R.sub.1 is a hydroxy functional alkyl having 2 or more carbons; and n is 2-6, and when R.sub.2 is a substituted or unsubstituted C.sub.1 to C.sub.36 alkyl group the film-forming resin comprises COOH functionality that reacts with the polyurea to form an ester linkage.

Other hydroxy functional alkyl polyurea compounds, polymers made with the same, and compositions comprising the same are also disclosed as are substrates coated at least in part with or formed with any of the compositions described herein.

HYDROXY FUNCTIONAL ALKYL POLYUREA CROSSLINKERS

A hydroxy functional alkyl polyurea is disclosed having the formula presented in claim 1, wherein R comprises an isocyanurate moiety, biuret moiety, allophonate moiety, glycoluril moiety, benzoguanamine moiety, polyetheramine moiety, and/or polymeric moiety different from a polyetheramine and having an Mn of 500 or greater; wherein each RI is independently a hydrogen, alkyl having at least 1 carbon, or a hydroxy functional alkyl having 2 or more carbons and at least one R.sub.1 is a hydroxy functional alkyl having 2 or more carbons; and n is 2-6. Further disclosed is a coating comprising: a film-forming resin; and a hydroxy functional alkyl polyurea crosslinker having the formula presented in claim 4, wherein R.sub.2 is a substituted or unsubstituted C.sub.1 to C.sub.36 alkyl group, an aromatic group, an isocyanurate moiety, biuret moiety, allophonate moiety, glycoluril moiety, benzoguanamine moiety, polyetheramine moiety, and/or polymeric moiety different from a polyetheramine having an Mn of 500 or greater, wherein each R.sub.1 is independently a hydrogen, an alkyl having at least 1 carbon, or a hydroxy functional alkyl having 2 or more carbons and at least one R.sub.1 is a hydroxy functional alkyl having 2 or more carbons; and n is 2-6, and when R.sub.2 is a substituted or unsubstituted C.sub.1 to C.sub.36 alkyl group the film-forming resin comprises COOH functionality that reacts with the polyurea to form an ester linkage.

Other hydroxy functional alkyl polyurea compounds, polymers made with the same, and compositions comprising the same are also disclosed as are substrates coated at least in part with or formed with any of the compositions described herein.