Patent classifications
C07C211/52
Preparation method of 4-(heptafluoro-2-propyl)-2-trifluoromethylaniline and application thereof
The present disclosure provides a preparation method of 4-(heptafluoro-2-propyl)-2-trifluoromethylaniline and an application thereof. The preparation method comprises the following steps: reacting 2-aminobenzotrifluoride and 2-bromoheptafluoropropane in the presence of sodium formate or hydrates thereof and a SO.sub.2 reagent, so as to obtain 4-(heptafluoro-2-propyl)-2-trifluoromethylaniline. The present disclosure adds sodium formate or hydrate thereof and the SO.sub.2 reagent during the reaction of 2-aminobenzotrifluoride and 2-bromoheptafluoropropane. Under the cooperation of these two compounds, the yield of the reaction is high. And the purity of the product is high, the operation method is simple, the cost is relatively low, and the pH of the reaction doesn't need to be controlled.
Preparation method of 4-(heptafluoro-2-propyl)-2-trifluoromethylaniline and application thereof
The present disclosure provides a preparation method of 4-(heptafluoro-2-propyl)-2-trifluoromethylaniline and an application thereof. The preparation method comprises the following steps: reacting 2-aminobenzotrifluoride and 2-bromoheptafluoropropane in the presence of sodium formate or hydrates thereof and a SO.sub.2 reagent, so as to obtain 4-(heptafluoro-2-propyl)-2-trifluoromethylaniline. The present disclosure adds sodium formate or hydrate thereof and the SO.sub.2 reagent during the reaction of 2-aminobenzotrifluoride and 2-bromoheptafluoropropane. Under the cooperation of these two compounds, the yield of the reaction is high. And the purity of the product is high, the operation method is simple, the cost is relatively low, and the pH of the reaction doesn't need to be controlled.
Preparation method of 4-(heptafluoro-2-propyl)-2-trifluoromethylaniline and application thereof
The present disclosure provides a preparation method of 4-(heptafluoro-2-propyl)-2-trifluoromethylaniline and an application thereof. The preparation method comprises the following steps: reacting 2-aminobenzotrifluoride and 2-bromoheptafluoropropane in the presence of sodium formate or hydrates thereof and a SO.sub.2 reagent, so as to obtain 4-(heptafluoro-2-propyl)-2-trifluoromethylaniline. The present disclosure adds sodium formate or hydrate thereof and the SO.sub.2 reagent during the reaction of 2-aminobenzotrifluoride and 2-bromoheptafluoropropane. Under the cooperation of these two compounds, the yield of the reaction is high. And the purity of the product is high, the operation method is simple, the cost is relatively low, and the pH of the reaction doesn't need to be controlled.
3,4-DISUBSTITUTED 3-CYCLOBUTENE-1,2-DIONES AND USE THEREOF
Described herein are compounds, or pharmaceutically acceptable salts thereof, of the following formula:
##STR00001##
The compounds are useful for treating inflammatory and autoimmune diseases.
3,4-DISUBSTITUTED 3-CYCLOBUTENE-1,2-DIONES AND USE THEREOF
Described herein are compounds, or pharmaceutically acceptable salts thereof, of the following formula:
##STR00001##
The compounds are useful for treating inflammatory and autoimmune diseases.
METHOD FOR PREPARING DIAMINOBIPHENYL COMPOUND
The object of the present invention is to provide a method which provides a diaminobiphenyl compound in a high yield and in a short period of time by a benzidine rearrangement reaction of a hydrazobenzene having a bulky substituent group at the meta position. Specifically, the present invention provides a method for preparing a diaminobiphenyl compound represented by the following formula (1):
##STR00001##
wherein, X.sub.1 and X.sub.2 are, independently of each other, a group selected from the group consisting of a trifluoromethyl group and, optionally fluorinated, isopropyl, isobutyl, sec-butyl, tert-butyl and neopentyl groups, comprising a step of subjecting a diphenylhydrazine compound represented by the following formula (2)
##STR00002##
wherein X.sub.1 and X.sub.2 are as defined above,
to a benzidine rearrangement reaction in the presence of an organic solvent and an inorganic acid at a temperature of from −70° C. to −11° C.
to obtain the diaminobiphenyl compound represented by the formula (1).
METHOD FOR PREPARING DIAMINOBIPHENYL COMPOUND
The object of the present invention is to provide a method which provides a diaminobiphenyl compound in a high yield and in a short period of time by a benzidine rearrangement reaction of a hydrazobenzene having a bulky substituent group at the meta position. Specifically, the present invention provides a method for preparing a diaminobiphenyl compound represented by the following formula (1):
##STR00001##
wherein, X.sub.1 and X.sub.2 are, independently of each other, a group selected from the group consisting of a trifluoromethyl group and, optionally fluorinated, isopropyl, isobutyl, sec-butyl, tert-butyl and neopentyl groups, comprising a step of subjecting a diphenylhydrazine compound represented by the following formula (2)
##STR00002##
wherein X.sub.1 and X.sub.2 are as defined above,
to a benzidine rearrangement reaction in the presence of an organic solvent and an inorganic acid at a temperature of from −70° C. to −11° C.
to obtain the diaminobiphenyl compound represented by the formula (1).
PROCESS FOR THE PREPARATION OF BIPHENYLAMINES
The invention relates to a method for the preparation of 2-aminobiphenyls, key intermediates in the preparation of compounds of interest in the agrochemical industry. The process comprises reacting an ortho-substituted aniline and a phenylboro derivative in the presence of a base and a palladium catalyst, said palladium catalyst comprising a palladium source and a biphenyl phosphine ligand of formula (III) or a salt thereof.
##STR00001##
PROCESS FOR THE PREPARATION OF BIPHENYLAMINES
The invention relates to a method for the preparation of 2-aminobiphenyls, key intermediates in the preparation of compounds of interest in the agrochemical industry. The process comprises reacting an ortho-substituted aniline and a phenylboro derivative in the presence of a base and a palladium catalyst, said palladium catalyst comprising a palladium source and a biphenyl phosphine ligand of formula (III) or a salt thereof.
##STR00001##
Inhibitors of histone deacetylase
The present invention relates to compounds of formula (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.