Patent classifications
C07C231/08
CRYSTAL FORM OF 6-(CYCLOPROPANECARBOXAMIDO)-4-((2-METHOXY-3-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)AMINO)-N-(METHYL-D3) PYRIDAZINE-3-CARBOXAMIDE
Disclosed is crystalline Form A of 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl) amino)-N-(methyl-d.sub.3)pyridazine-3-carboxamide. Form A is a neat crystalline form. Characterization data for Form A are disclosed.
PROCESS FOR THE PREPARATION OF 6-(CYCLOPROPANEAMIDO)-4-((2-METHOXY-3-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)AMINO)-N-(METHYL-D3)PYRIDAZINE-3-CARBOXAMIDE
The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-5N-(methyl-d3)pyridazine-3-carboxamide of the formula:
##STR00001##
Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.
PROCESS FOR THE PREPARATION OF 6-(CYCLOPROPANEAMIDO)-4-((2-METHOXY-3-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)AMINO)-N-(METHYL-D3)PYRIDAZINE-3-CARBOXAMIDE
The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-5N-(methyl-d3)pyridazine-3-carboxamide of the formula:
##STR00001##
Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.
RADIOPAQUE MONOMERS, POLYMERS, MICROSPHERES, AND METHODS RELATED THERETO
Radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of using the radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of manufacturing radiopaque monomers, polymers, and microspheres are disclosed herein.
RADIOPAQUE MONOMERS, POLYMERS, MICROSPHERES, AND METHODS RELATED THERETO
Radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of using the radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of manufacturing radiopaque monomers, polymers, and microspheres are disclosed herein.
RADIOPAQUE MONOMERS, POLYMERS, MICROSPHERES, AND METHODS RELATED THERETO
Radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of using the radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of manufacturing radiopaque monomers, polymers, and microspheres are disclosed herein.
RAPID SYNTHESIS METHOD FOR BIOMASS-BASED AMINE
A rapid synthesis method for a biomass-based amine, including: using formamide as an amine source, formic acid as a hydrogen source, and biomass aldehyde or ketone as a raw material, conduct rapid heating promoting direct addition of formamide and aldehyde or ketone compound through microwave-assisted heating and without a solvent and catalyst, and carrying out formic acid reduction preparing and obtaining a corresponding formamide derivative; selectively converting the formamide derivative under the action of a base into a corresponding primary amine through alcoholysis. The microwave-assisted heating reaction system has a significantly higher catalytic efficiency than a corresponding oil bath system, greatly shortens a reaction time, and significantly improves selectivity, where a conversion rate of a biomass aldehyde or ketone compound may reach at least 99%, and a formamide derivative yield may reach 85-99%; the formamide derivative is synthesized to a primary amine through alcoholysis, where a yield may reach 92-99%.
RAPID SYNTHESIS METHOD FOR BIOMASS-BASED AMINE
A rapid synthesis method for a biomass-based amine, including: using formamide as an amine source, formic acid as a hydrogen source, and biomass aldehyde or ketone as a raw material, conduct rapid heating promoting direct addition of formamide and aldehyde or ketone compound through microwave-assisted heating and without a solvent and catalyst, and carrying out formic acid reduction preparing and obtaining a corresponding formamide derivative; selectively converting the formamide derivative under the action of a base into a corresponding primary amine through alcoholysis. The microwave-assisted heating reaction system has a significantly higher catalytic efficiency than a corresponding oil bath system, greatly shortens a reaction time, and significantly improves selectivity, where a conversion rate of a biomass aldehyde or ketone compound may reach at least 99%, and a formamide derivative yield may reach 85-99%; the formamide derivative is synthesized to a primary amine through alcoholysis, where a yield may reach 92-99%.
RAPID SYNTHESIS METHOD FOR BIOMASS-BASED AMINE
A rapid synthesis method for a biomass-based amine, including: using formamide as an amine source, formic acid as a hydrogen source, and biomass aldehyde or ketone as a raw material, conduct rapid heating promoting direct addition of formamide and aldehyde or ketone compound through microwave-assisted heating and without a solvent and catalyst, and carrying out formic acid reduction preparing and obtaining a corresponding formamide derivative; selectively converting the formamide derivative under the action of a base into a corresponding primary amine through alcoholysis. The microwave-assisted heating reaction system has a significantly higher catalytic efficiency than a corresponding oil bath system, greatly shortens a reaction time, and significantly improves selectivity, where a conversion rate of a biomass aldehyde or ketone compound may reach at least 99%, and a formamide derivative yield may reach 85-99%; the formamide derivative is synthesized to a primary amine through alcoholysis, where a yield may reach 92-99%.
COMPOUND COMPRISING 1-ACETYL-6-FLUORO-2,2,4-TRIMETHYL-1,2,3,4-TETRAHYDROQUINOLINE
A compound of Formula (VI), wherein ‘n’ and ‘R’ are selected so that the compound comprises 1-acetyl-6-fluoro-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline of Formula (IX):
##STR00001##