Patent classifications
C07D213/127
Complexes
The present invention provides a palladium(II) complex of formula (1) or a palladium(II) complex of formula (2).
##STR00001##
R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.18, R.sub.19, R.sub.20, R.sub.21, R.sub.22, R.sub.23 and R.sub.24, m, E and X are described in the specification.
The invention also provides a process for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.
Complexes
The present invention provides a palladium(II) complex of formula (1) or a palladium(II) complex of formula (2).
##STR00001##
R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.18, R.sub.19, R.sub.20, R.sub.21, R.sub.22, R.sub.23 and R.sub.24, m, E and X are described in the specification.
The invention also provides a process for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.
NOVEL FERROCENE-BASED UNSYMMETRICAL LIGANDS BEARING BULKY DI(ADAMANTLY)PHOSPHINO MOTIF AND THEIR METAL CATALYSTS
Ferrocenyl-based unsymmetrical ligands containing di(1-adamantyl)phosphino groups with general formula, Fc(Ad.sub.2P) (R.sub.2P) and corresponding metal complexes, include metal halide complexes, N-biphenyl metal cationic complexes and R-allyl metal cationic complexes, useful in catalysis. The ligands and complexes overcome problems with conventional catalysts, providing new routes to previously challenging cross-coupling reactions, including CP coupling, C.sub.sp2C.sub.sp3 coupling and other conventional cross-coupling applications, while being scalable so that they can be provided in sufficient quantity and purity for industrial applications.
Complexes
A palladium(II) complex of formula (1) or a palladium(II) complex of formula (2). ##STR00001## Also, a process for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.
Complexes
A palladium(II) complex of formula (1) or a palladium(II) complex of formula (2). ##STR00001## Also, a process for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.
NOVEL MANUFACTURING PROCESS FOR TRIAZINE, PYRIMIDINE AND PYRIDINE DERIVATIVES
The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I)
##STR00001##
wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.
NOVEL MANUFACTURING PROCESS FOR TRIAZINE, PYRIMIDINE AND PYRIDINE DERIVATIVES
The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I)
##STR00001##
wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.
STABILIZATION OF ACTIVE METAL CATALYSTS AT METAL-ORGANIC FRAMEWORK NODES FOR HIGHLY EFFICIENT ORGANIC TRANSFORMATIONS
Metal-organic framework (MOFs) compositions based on postsynthetic metalation of secondary building unit (SBU) terminal or bridging OH or OH.sub.2 groups with metal precursors or other post-synthetic manipulations are described. The MOFs provide a versatile family of recyclable and reusable single-site solid catalysts for catalyzing a variety of asymmetric organic transformations, including the regioselective boryiation and siiylation of benzyiic CH bonds, the hydrogenation of aikenes, imines, carbonyls, nitroarenes, and heterocycles, hydroboration, hydrophosphination, and cyclization reactions. The solid catalysts can also be integrated into a flow reactor or a supercritical fluid reactor.
STABILIZATION OF ACTIVE METAL CATALYSTS AT METAL-ORGANIC FRAMEWORK NODES FOR HIGHLY EFFICIENT ORGANIC TRANSFORMATIONS
Metal-organic framework (MOFs) compositions based on postsynthetic metalation of secondary building unit (SBU) terminal or bridging OH or OH.sub.2 groups with metal precursors or other post-synthetic manipulations are described. The MOFs provide a versatile family of recyclable and reusable single-site solid catalysts for catalyzing a variety of asymmetric organic transformations, including the regioselective boryiation and siiylation of benzyiic CH bonds, the hydrogenation of aikenes, imines, carbonyls, nitroarenes, and heterocycles, hydroboration, hydrophosphination, and cyclization reactions. The solid catalysts can also be integrated into a flow reactor or a supercritical fluid reactor.
Isoxazole derivatives as FXR agonists and methods of use thereof
The present invention provides compounds of Formula I: ##STR00001##
and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR and methods for their preparation and use.