Patent classifications
C07D223/22
Selective inhibitors of constitutive androstane receptor
The compounds of the invention are antagonists of CAR, with specificity for CAR over other proteins including PXR. The disclosed compounds are useful in treating or controlling cell proliferative disorders, in particular oncological disorders, such as cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Selective inhibitors of constitutive androstane receptor
The compounds of the invention are antagonists of CAR, with specificity for CAR over other proteins including PXR. The disclosed compounds are useful in treating or controlling cell proliferative disorders, in particular oncological disorders, such as cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
BLUE FLUORESCENT EMITTERS
The present invention relates to compounds of the formula (I)
##STR00001## where C, D, A, m and n are as defined herein, and to their use in optoelectronic components and to optoelectronic components comprising them.
BLUE FLUORESCENT EMITTERS
The present invention relates to compounds of the formula (I)
##STR00001## where C, D, A, m and n are as defined herein, and to their use in optoelectronic components and to optoelectronic components comprising them.
Process for the preparation of eslicarbazepine and eslicarbazepine acetate
Object of the present invention is an improved process for the preparation of Elsicarbazepine and Eslicarbazepine acetate by means of chiral Ruthenium catalysts.
ASYMMETRIC CATALYTIC REDUCTION OF OXCARBAZEPINE
A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-()-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX.sub.2(L)].sub.2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B):
##STR00001##
wherein R.sup.1 is chosen from C.sub.1-6 alkoxy and C.sub.1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R.sup.1 can be the same or different, and R.sup.2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR.sup.3R.sup.4R.sup.5 and formic acid, [R.sup.3R.sup.4R.sup.5NH][OOCH] and optionally formic acid, or [M][OOCH].sub.x and formic acid, wherein R.sup.3, R.sup.4 and R.sup.5 are C.sub.1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.
BIOCATALYTIC PROCESS FOR PREPARING ESLICARBAZEPINE AND ANALOGS THEREOF
The present disclosure relates to biocatalysts and its uses for the efficient preparation of eslicarbazepine, eslicarbazepine acetate, and analogs thereof.
Asymmetric catalytic reduction of oxcarbazepine
A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-()-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX.sub.2(L)].sub.2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): ##STR00001##
wherein R.sup.1 is chosen from C.sub.1-6 alkoxy and C.sub.1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R.sup.1 can be the same or different, and R.sup.2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR.sup.3R.sup.4R.sup.5 and formic acid, [R.sup.3R.sup.4R.sup.5NH][OOCH] and optionally formic acid, or [M][OOCH].sub.x and formic acid, wherein R.sup.3, R.sup.4 and R.sup.5 are C.sub.1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.
Asymmetric catalytic reduction of oxcarbazepine
A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-()-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX.sub.2(L)].sub.2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): ##STR00001##
wherein R.sup.1 is chosen from C.sub.1-6 alkoxy and C.sub.1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R.sup.1 can be the same or different, and R.sup.2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR.sup.3R.sup.4R.sup.5 and formic acid, [R.sup.3R.sup.4R.sup.5NH][OOCH] and optionally formic acid, or [M][OOCH].sub.x and formic acid, wherein R.sup.3, R.sup.4 and R.sup.5 are C.sub.1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.
Biocatalytic process for preparing eslicarbazepine and analogs thereof
The present disclosure relates to biocatalysts and its uses for the efficient preparation of eslicarbazepine, eslicarbazepine acetate, and analogs thereof.