Patent classifications
C07C62/38
Process method for producing pesticide by using carbon dioxide
A process method for producing a pesticide by using carbon dioxide includes: weighing a 1,3-cyclohexanedione substrate 1(a-e), a catalyst and Cs.sub.2CO.sub.3 in a Schlenk bottle, degassing, and continuously introducing 1 atm of carbon dioxide; adding a solvent and reacting for 48 h in an oil bath at 50° C. After the reaction was completed, post-treatment was carried out to obtain a 2-carboxyl-1,3-cyclohexanedione compound 2(a-e). The obtained acid is acylated and then added dropwise to a dichloromethane solution containing aniline to react for 2 h at room temperature. After the reaction, column chromatography was performed to obtain a pesticide compound 3(a-e). Adding the pesticide compound 3(a-e) into 50% concentrated sulfuric acid and refluxing at 80° C. for 8 hours. Through separation, a pesticide product compound 4(a-e) was obtained. The process method is simple, with low requirements on equipment, wide sources of raw materials, low cost, low toxicity and easy industrial scale-up production.
Process method for producing pesticide by using carbon dioxide
A process method for producing a pesticide by using carbon dioxide includes: weighing a 1,3-cyclohexanedione substrate 1(a-e), a catalyst and Cs.sub.2CO.sub.3 in a Schlenk bottle, degassing, and continuously introducing 1 atm of carbon dioxide; adding a solvent and reacting for 48 h in an oil bath at 50° C. After the reaction was completed, post-treatment was carried out to obtain a 2-carboxyl-1,3-cyclohexanedione compound 2(a-e). The obtained acid is acylated and then added dropwise to a dichloromethane solution containing aniline to react for 2 h at room temperature. After the reaction, column chromatography was performed to obtain a pesticide compound 3(a-e). Adding the pesticide compound 3(a-e) into 50% concentrated sulfuric acid and refluxing at 80° C. for 8 hours. Through separation, a pesticide product compound 4(a-e) was obtained. The process method is simple, with low requirements on equipment, wide sources of raw materials, low cost, low toxicity and easy industrial scale-up production.
PROCESS FOR PREPARING CARBAMOYLOXYMETHYL TRIAZOLE CYCLOHEXYL ACID COMPOUNDS
Improved methods and intermediates thereof for preparing carbamoyloxy methyl triazole cyclohexyl acid compounds are described. These compounds are useful as LPA antagonists. Formula (I).
##STR00001##
PROCESS FOR PREPARING CARBAMOYLOXYMETHYL TRIAZOLE CYCLOHEXYL ACID COMPOUNDS
Improved methods and intermediates thereof for preparing carbamoyloxy methyl triazole cyclohexyl acid compounds are described. These compounds are useful as LPA antagonists. Formula (I).
##STR00001##
Non-Cryogenic, Ammonia-Free Reduction of Aryl Compounds
A method of reducing an aromatic ring or a cyclic, allylic ether in a compound includes preparing a reaction mixture including a compound including an aromatic moiety or a cyclic, allylic ether moiety, an alkali metal, and either ethylenediamine, diethylenetriamine, triethylenetetramine, or a combination thereof, in an ether solvent; and reacting the reaction mixture at from −20° C. to 30° C. for a time sufficient to reduce a double bond in the aromatic moiety to a single bond or to reduce the cyclic, allylic ether moiety.
Non-Cryogenic, Ammonia-Free Reduction of Aryl Compounds
A method of reducing an aromatic ring or a cyclic, allylic ether in a compound includes preparing a reaction mixture including a compound including an aromatic moiety or a cyclic, allylic ether moiety, an alkali metal, and either ethylenediamine, diethylenetriamine, triethylenetetramine, or a combination thereof, in an ether solvent; and reacting the reaction mixture at from −20° C. to 30° C. for a time sufficient to reduce a double bond in the aromatic moiety to a single bond or to reduce the cyclic, allylic ether moiety.
Therapeutic compounds and methods of use thereof
The invention provides compounds having the general formula I: ##STR00001## and pharmaceutically acceptable salts thereof, wherein the variables R.sup.AA, n, ring A, X.sup.1, L, m, X.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, and R.sup.6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Therapeutic compounds and methods of use thereof
The invention provides compounds having the general formula I: ##STR00001## and pharmaceutically acceptable salts thereof, wherein the variables R.sup.AA, n, ring A, X.sup.1, L, m, X.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, and R.sup.6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
A PROCESS METHOD FOR PRODUCING PESTICIDE BY USING CARBON DIOXIDE
A process method for producing pesticide by using carbon dioxide comprises the following steps: Weighing 1, 3-cyclohexanedione substrate, catalyst and Cs2CO3 in Schleck bottle, degassing, and continuously introducing 1 atm of carbon dioxide. Add solvent and react for 48 h in an oil bath at 50° C. After the reaction was completed, post-treatment was carried out to obtain 2(a-e). The obtained acid is acylated and then added dropwise to dichloromethane solution containing aniline to react for 2 h at normal temperature. After the reaction, column chromatography was performed to obtain 3(a-e). Add 3 (a-e) into 50% concentrated sulfuric acid and reflux at 80° C. for 8 hours. Through separation, 4(a-e) was obtained. The invention has the advantages that the catalyst is simple to prepare, has high catalytic activity, can be recycled, realizes industrial circulation, and achieves the goal of sustainable production. The preparation process of 3(a-e) and 4 (a-e) is simple, with low requirements on equipment, wide sources of raw materials, low cost, low toxicity and easy industrial scale-up production.
A PROCESS METHOD FOR PRODUCING PESTICIDE BY USING CARBON DIOXIDE
A process method for producing pesticide by using carbon dioxide comprises the following steps: Weighing 1, 3-cyclohexanedione substrate, catalyst and Cs2CO3 in Schleck bottle, degassing, and continuously introducing 1 atm of carbon dioxide. Add solvent and react for 48 h in an oil bath at 50° C. After the reaction was completed, post-treatment was carried out to obtain 2(a-e). The obtained acid is acylated and then added dropwise to dichloromethane solution containing aniline to react for 2 h at normal temperature. After the reaction, column chromatography was performed to obtain 3(a-e). Add 3 (a-e) into 50% concentrated sulfuric acid and reflux at 80° C. for 8 hours. Through separation, 4(a-e) was obtained. The invention has the advantages that the catalyst is simple to prepare, has high catalytic activity, can be recycled, realizes industrial circulation, and achieves the goal of sustainable production. The preparation process of 3(a-e) and 4 (a-e) is simple, with low requirements on equipment, wide sources of raw materials, low cost, low toxicity and easy industrial scale-up production.