Patent classifications
C07D239/06
Chiral 1,3-diarylimidazolium salt carbene precursor, synthesis method therefor, metal salt compound and application thereof
Chiral 1, 3-diarylimidazole salt carbene precursors, their methods of preparation, particularly transition metal complexes and their use in chemical synthesis are provided. In particular, an air and moisture stable chiral 1, 3-diarylimidazole carbene precursor Cu (I) complex has been prepared and applied to highly regio- and enantioselective Markovnikov hydroboration of unactivated terminal alkenes to form chiral boronic esters. Moreover, these new chiral NHCs can be potentially applied in various metal-catalyzed asymmetric transformations. ##STR00001##
Chiral 1,3-diarylimidazolium salt carbene precursor, synthesis method therefor, metal salt compound and application thereof
Chiral 1, 3-diarylimidazole salt carbene precursors, their methods of preparation, particularly transition metal complexes and their use in chemical synthesis are provided. In particular, an air and moisture stable chiral 1, 3-diarylimidazole carbene precursor Cu (I) complex has been prepared and applied to highly regio- and enantioselective Markovnikov hydroboration of unactivated terminal alkenes to form chiral boronic esters. Moreover, these new chiral NHCs can be potentially applied in various metal-catalyzed asymmetric transformations. ##STR00001##
GEM-DISUBSTITUTED PYRROLIDINES, PIPERAZINES, AND DIAZEPANES, AND COMPOSITIONS AND METHODS OF MAKING THE SAME
Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).
GEM-DISUBSTITUTED PYRROLIDINES, PIPERAZINES, AND DIAZEPANES, AND COMPOSITIONS AND METHODS OF MAKING THE SAME
Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).
Gem-disubstituted pyrrolidines, piperazines, and diazepanes, and compositions and methods of making the same
Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).
Gem-disubstituted pyrrolidines, piperazines, and diazepanes, and compositions and methods of making the same
Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).
HETEROGENEOUS CATALYZED PROCESS FOR THE PRODUCTION OF 2,2,4,6,6-PENTAMETHYL-1,2,5,6-TETRAHYDRO-PYRIMIDINE
The present invention relates to a process for the production of 2,2,4,6,6-pentamethyl-1,2,5,6-tetrahydro-pyrimidine comprising (i) providing a reactor containing a catalyst comprising a zeolitic material, wherein the zeolitic material comprises YO.sub.2 and optionally comprises X.sub.2O.sub.3 in its framework structure, wherein Y is a tetravalent element and X is a trivalent element; (ii) preparing a reaction mixture comprising acetone and ammonia; (iii) contacting the catalyst in the reactor with the reaction mixture prepared in (ii) for obtaining a reaction product comprising 2,2,4,6,6-pentamethyl-1,2,5,6-tetrahydro-pyrimidine; wherein the temperature programmed desorption of ammonia (NH.sub.3-TPD) profile of the zeolitic material comprised in the catalyst provided in (i) optionally displays one or more bands associated with medium acid sites, said one or more bands having maxima in the temperature range of from 250 to 500° C., wherein the integration of said one or more bands affords a total value of 0.5 mmol/g or less, and wherein the mixture prepared in (ii) and contacted with the catalyst in (iii) contains less than 10 wt.-% of water based on 100 wt.-% of the reaction mixture.
HETEROGENEOUS CATALYZED PROCESS FOR THE PRODUCTION OF 2,2,4,6,6-PENTAMETHYL-1,2,5,6-TETRAHYDRO-PYRIMIDINE
The present invention relates to a process for the production of 2,2,4,6,6-pentamethyl-1,2,5,6-tetrahydro-pyrimidine comprising (i) providing a reactor containing a catalyst comprising a zeolitic material, wherein the zeolitic material comprises YO.sub.2 and optionally comprises X.sub.2O.sub.3 in its framework structure, wherein Y is a tetravalent element and X is a trivalent element; (ii) preparing a reaction mixture comprising acetone and ammonia; (iii) contacting the catalyst in the reactor with the reaction mixture prepared in (ii) for obtaining a reaction product comprising 2,2,4,6,6-pentamethyl-1,2,5,6-tetrahydro-pyrimidine; wherein the temperature programmed desorption of ammonia (NH.sub.3-TPD) profile of the zeolitic material comprised in the catalyst provided in (i) optionally displays one or more bands associated with medium acid sites, said one or more bands having maxima in the temperature range of from 250 to 500° C., wherein the integration of said one or more bands affords a total value of 0.5 mmol/g or less, and wherein the mixture prepared in (ii) and contacted with the catalyst in (iii) contains less than 10 wt.-% of water based on 100 wt.-% of the reaction mixture.
GEM-DISUBSTITUTED PYRROLIDINES, PIPERAZINES, AND DIAZEPANES, AND COMPOSITIONS AND METHODS OF MAKING THE SAME
Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).
GEM-DISUBSTITUTED PYRROLIDINES, PIPERAZINES, AND DIAZEPANES, AND COMPOSITIONS AND METHODS OF MAKING THE SAME
Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).