Patent classifications
C07B37/10
LIGAND-CONTROLLED DIVERGENT DEHYDROGENATIVE REACTIONS OF ALIPHATIC ACIDS
Disclosed herein are palladium-catalyzed dehydrogenation processes of carboxylic acids to make ?, ?-unsaturated carboxylic acids or ?-alkylidene butenolides. The processes allow the chemoselective dehydrogenation of carboxylic acids in the presence of other enolizable functionalities such as ketones, providing reactivity that is inaccessible with existing carbonyl desaturation protocols.
POLYNITROGEN COMPOUNDS AND USES THEREOF AS FLUORESCENT CHROMOPHORES
The present invention relates to the use, as a fluorescent chromophore, of a compound with formula (I) wherein: A.sub.1 is N or C(Y.sub.1); A.sub.2 is N or C(Y.sub.2); A.sub.3 is N or C(Y.sub.3); A.sub.4 is N or C(Y.sub.4); at least one of A.sub.1, A.sub.2, A.sub.3 and A.sub.4 representing N; X.sub.1 is N or C(Y.sub.5); X.sub.2 is N or C(Y.sub.6); X.sub.3 is N or C(Y.sub.7); and Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Y.sub.5, Y.sub.6 and Y.sub.7 are in particular chosen independently of one another from the group made up of: H, electron-donor groups and electron-attracting groups.
ETHYLENE-TO-LIQUIDS SYSTEMS AND METHODS
The present disclosure provides petrochemical processing methods and systems, including ethylene conversion processes and systems, for the production of higher hydrocarbon compositions, for example liquid hydrocarbon compounds, with reduced amount of unsaturated hydrocarbons.
ETHYLENE-TO-LIQUIDS SYSTEMS AND METHODS
The present disclosure provides petrochemical processing methods and systems, including ethylene conversion processes and systems, for the production of higher hydrocarbon compositions, for example liquid hydrocarbon compounds, with reduced amount of unsaturated hydrocarbons.
SYNTHESIS OF A COMPOUND THAT MODULATES THE ACTIVITY OF BROMODOMAIN-CONTAINING PROTEINS
The present disclosure provides processes for the preparation of a compound of formula I:
##STR00001##
or a salt or co-crystal thereof, that modulates the activity of bromodomain-containing proteins. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.
SYNTHESIS OF A COMPOUND THAT MODULATES THE ACTIVITY OF BROMODOMAIN-CONTAINING PROTEINS
The present disclosure provides processes for the preparation of a compound of formula I:
##STR00001##
or a salt or co-crystal thereof, that modulates the activity of bromodomain-containing proteins. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.
METHODS OF PREPARING OXA-BICYCLOALKENE
Disclosed is a method of preparing an oxa-bicycloalkene via the reaction of a cycloalkanone and an allyl alcohol compound in the presence of an organic acid, a manganese catalyst, and oxygen at a predetermined temperature.
METHODS OF PREPARING OXA-BICYCLOALKENE
Disclosed is a method of preparing an oxa-bicycloalkene via the reaction of a cycloalkanone and an allyl alcohol compound in the presence of an organic acid, a manganese catalyst, and oxygen at a predetermined temperature.
AN IMPROVED PROCESS FOR THE PREPARATION OF CLOBAZAM AND ITS INTERMEDIATE
The present invention provides an improved process for the preparation of 8-chloro-1-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione (hereafter referred to as the compound (IV)), which is useful as a key intermediate for the synthesis of Clobazam (referred to as the compound (I)) 7-chloro-1-methyl-5-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione. The process of the present invention further involves transformation of the compound (IV) into Clobazam (I), comprising (a) reacting the compound (II) (as described herein) with monoalkyl malonate in the presence of a coupling agent to obtain the compound (III) (as described herein); followed by the cyclization using a base; (b) reacting the compound-IV (as described herein) obtained from step (a) with methylating agent. The process of the present invention involves formation of novel intermediates methyl 3-((4-chloro-2-(phenylamino) phenyl)amino)-3-oxopropanoate (IIIa) and 3-((4-chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoic acid (V).
AN IMPROVED PROCESS FOR THE PREPARATION OF CLOBAZAM AND ITS INTERMEDIATE
The present invention provides an improved process for the preparation of 8-chloro-1-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione (hereafter referred to as the compound (IV)), which is useful as a key intermediate for the synthesis of Clobazam (referred to as the compound (I)) 7-chloro-1-methyl-5-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione. The process of the present invention further involves transformation of the compound (IV) into Clobazam (I), comprising (a) reacting the compound (II) (as described herein) with monoalkyl malonate in the presence of a coupling agent to obtain the compound (III) (as described herein); followed by the cyclization using a base; (b) reacting the compound-IV (as described herein) obtained from step (a) with methylating agent. The process of the present invention involves formation of novel intermediates methyl 3-((4-chloro-2-(phenylamino) phenyl)amino)-3-oxopropanoate (IIIa) and 3-((4-chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoic acid (V).