Patent classifications
C07D263/22
Method for producing fluorovinyl amide compound
An object of this disclosure provides a novel method for producing a fluorovinyl amide compound and the like. The object is achieved by a method for producing a compound represented by formula (1): ##STR00001##
wherein
Rf is F or fluoroalkyl,
R.sup.a1 is H or an organic group, and
R.sup.a2 is H or an organic group, or
(i) R.sup.a1 and R.sup.a2, (ii) R.sup.a1 and Rf, or (iii) Rf and R.sup.a2, may be linked to each other,
R.sup.b1 is H or an organic group, and
R.sup.b2 is H or an organic group, or
R.sup.b1 and R.sup.b2 may be linked together with their adjacent atoms to form a nitrogen-containing ring optionally having one or more substituents,
the method comprising
step A of reacting a compound represented by formula (2): ##STR00002##
wherein
R.sup.x is a leaving group,
with a compound represented by formula (3) or a salt thereof: ##STR00003##
in the presence of a transition metal catalyst.
Method for producing fluorovinyl amide compound
An object of this disclosure provides a novel method for producing a fluorovinyl amide compound and the like. The object is achieved by a method for producing a compound represented by formula (1): ##STR00001##
wherein
Rf is F or fluoroalkyl,
R.sup.a1 is H or an organic group, and
R.sup.a2 is H or an organic group, or
(i) R.sup.a1 and R.sup.a2, (ii) R.sup.a1 and Rf, or (iii) Rf and R.sup.a2, may be linked to each other,
R.sup.b1 is H or an organic group, and
R.sup.b2 is H or an organic group, or
R.sup.b1 and R.sup.b2 may be linked together with their adjacent atoms to form a nitrogen-containing ring optionally having one or more substituents,
the method comprising
step A of reacting a compound represented by formula (2): ##STR00002##
wherein
R.sup.x is a leaving group,
with a compound represented by formula (3) or a salt thereof: ##STR00003##
in the presence of a transition metal catalyst.
OXAZOLIDONE RING CONTAINING ADDUCTS
Embodiments include oxazolidone ring containing adducts obtainable by combining an aliphatic epoxy compound, an aromatic epoxy compound, and a diisocyanate. Embodiments further include a curable powder coating composition including a resin component and a hardener component, where the resin component includes the oxazolidone ring containing adduct.
METHOD FOR PRODUCING FLUOROVINYL AMIDE COMPOUND
An object of this disclosure provides a novel method for producing a fluorovinyl amide compound and the like. The object is achieved by a method for producing a compound represented by formula (1):
##STR00001## wherein Rf is F or fluoroalkyl, R.sup.a1 is H or an organic group, and R.sup.a2 is H or an organic group, or (i) R.sup.a1 and R.sup.a2, (ii) R.sup.a1 and Rf, or (iii) Rf and R.sup.a2, may be linked to each other, R.sup.b1 is H or an organic group, and R.sup.b2 is H or an organic group, or R.sup.b1 and R.sup.b2 may be linked together with their adjacent atoms to form a nitrogen-containing ring optionally having one or more substituents, the method comprising step A of reacting a compound represented by formula (2):
##STR00002## wherein R.sup.x is a leaving group, with a compound represented by formula (3) or a salt thereof:
##STR00003## in the presence of a transition metal catalyst.
METHOD FOR PRODUCING FLUOROVINYL AMIDE COMPOUND
An object of this disclosure provides a novel method for producing a fluorovinyl amide compound and the like. The object is achieved by a method for producing a compound represented by formula (1):
##STR00001## wherein Rf is F or fluoroalkyl, R.sup.a1 is H or an organic group, and R.sup.a2 is H or an organic group, or (i) R.sup.a1 and R.sup.a2, (ii) R.sup.a1 and Rf, or (iii) Rf and R.sup.a2, may be linked to each other, R.sup.b1 is H or an organic group, and R.sup.b2 is H or an organic group, or R.sup.b1 and R.sup.b2 may be linked together with their adjacent atoms to form a nitrogen-containing ring optionally having one or more substituents, the method comprising step A of reacting a compound represented by formula (2):
##STR00002## wherein R.sup.x is a leaving group, with a compound represented by formula (3) or a salt thereof:
##STR00003## in the presence of a transition metal catalyst.
Triazole compounds and preparation method therefor and use thereof
Certain triazole compounds have good LPAR1 antagonistic activity and selectivity, low toxicity, and good metabolic stability, and can be used for preventing or treating the LPAR1-related disease or disorder. The IC.sub.50 value of some triazole compounds can be below 300 nM, even 50 nM. The range of CC.sub.50 of the triazole compounds can be greater than 200 M. They also show good metabolic stability in human, fancy rats, and house mice.
Triazole compounds and preparation method therefor and use thereof
Certain triazole compounds have good LPAR1 antagonistic activity and selectivity, low toxicity, and good metabolic stability, and can be used for preventing or treating the LPAR1-related disease or disorder. The IC.sub.50 value of some triazole compounds can be below 300 nM, even 50 nM. The range of CC.sub.50 of the triazole compounds can be greater than 200 M. They also show good metabolic stability in human, fancy rats, and house mice.
RXFP1 AGONISTS
The disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension).
##STR00001##
Alpha, Beta-UNSATURATED AMIDE COMPOUND, AND PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
Provided in the present invention are an ,-unsaturated amide compound, and a preparation method therefor, and a pharmaceutical composition and the use thereof. Specifically, provided in the present invention is a compound as represented by formula I, wherein the definition of each group is as described in the description. The compound can be used as a compound for improving cerebral blood flow and is used for preparing a pharmaceutical composition for treating neurodegenerative diseases such as Alzheimer's disease and vascular dementia and strokes.