摘要:
A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.
摘要:
The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
摘要:
The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
摘要:
The invention is an improved method for the preparation of tertiary phosphines by way of cross-coupling of aryl, alkenyl, cycloalkenyl or aralkyl halides or aryl, alkenyl, cycloalkenyl or aralkyl sulfonate esters with chlorophosphines in the presence of a catalyst and a reductant. The general reaction scheme is shown below: ##STR1## wherein R.sup.1 is aryl, alkenyl, cycloalkenyl or aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl, or CONR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; R.sup.2 and R.sup.3 are independently aryl, alkyl, aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl or CoNR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; and n is 2 where R.sup.1 is a difunctional moiety and 1 for any other R.sup.1 ; and X is Cl, Br, I, or OSO.sub.2 Y; wherein Y is alkyl, trihalomethyl, phenyl, halophenyl, or alkylphenyl.
摘要翻译:本发明是通过芳基,链烯基,环烯基或芳烷基卤化物或芳基,烯基,环烯基或芳烷基磺酸酯与氯膦在催化剂和还原剂存在下交叉偶联来制备叔膦的改进方法。 一般反应方案如下所示:其中R 1为芳基,烯基,环烯基或芳烷基,其中任何一个可被一个或多个下列基团取代:烷基,芳基,芳烷基,烷氧基,烷酰基,氯,氟, 烷氧基羰基,氰基,三氟甲基,环烷基或CONR 4 R 5,其中R 4和R 5独立地是氢,烷基,芳基或芳烷基; R 2和R 3独立地为芳基,烷基,芳烷基,其中任一个可以被一个或多个下列基团取代:烷基,芳基,芳烷基,烷氧基,烷酰基,氯,氟,烷氧基羰基,氰基,三氟甲基,环烷基或CoNR 4 R 5,其中R 4 和R 5独立地是氢,烷基,芳基或芳烷基; 并且n为2,其中R 1为双官能部分,1为任何其它R 1; X为Cl,Br,I或OSO 2 Y; 其中Y是烷基,三卤代甲基,苯基,卤代苯基或烷基苯基。
摘要:
Novel homogeneous bimetallic hydroformylation catalysts, and processes utilizing these catalysts to convert alkenes, particularly alpha olefins, under mild conditions to a product rich in aldehydes, particularly a product containing a high ratio of linear:branched chain aldehydes. The catalysts can be produced from a binucleating tetratertiaryphosphine ligand capable of strongly coordinating two metal centers and holding them in general proximity to one another. Bimetallic catalyst precursors are produced which, on reaction with carbon monoxide and hydrogen, form the active bimetallic hydroformylation catalyst system.
摘要:
A ruthenium-phosphine complex represented by the formula:[RuXY(BINAP].sub.nwherein n is an integer of from 1 to about 10; and X and Y independently represent nonchelating anionic ligands.
摘要:
The invention is an improved method for the preparation of tertiary phosphines by way of cross-coupling of aryl, alkenyl, cycloalkenyl or aralkyl halides or aryl, alkenyl, cycloalkenyl or aralkyl sulfonate esters with chlorophosphines in the presence of a catalyst and a reductant. The general reaction scheme is shown below: ##STR1## wherein R.sup.1 is aryl, alkenyl, cycloalkenyl or aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl, or CONR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; R.sup.2 and R.sup.3 are independently aryl, alkyl, aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl or CONR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; and n is 2 where R.sup.1 is a difunctional moiety and 1 for any other R.sup.1 ; and X is Cl, Br, I, or OSO.sub.2 Y; wherein Y is alkyl, trihalomethyl, phenyl, halophenyl, or alkylphenyl.
摘要翻译:本发明是通过芳基,链烯基,环烯基或芳烷基卤化物或芳基,烯基,环烯基或芳烷基磺酸酯与氯膦在催化剂和还原剂存在下交叉偶联来制备叔膦的改进方法。 一般反应方案如下所示:其中R1是芳基,烯基,环烯基或芳烷基,其中任何一个可以被一个或多个下列基团取代:烷基,芳基,芳烷基,烷氧基,烷酰基,氯,氟,烷氧基羰基,氰基 ,三氟甲基,环烷基或CONR 4 R 5,其中R 4和R 5独立地是氢,烷基,芳基或芳烷基; R 2和R 3独立地是芳基,烷基,芳烷基,其中任何一个可以被一个或多个下列基团取代:烷基,芳基,芳烷基,烷氧基,烷酰基,氯,氟,烷氧基羰基,氰基,三氟甲基,环烷基或CONR 4 R 5,其中R 4 和R 5独立地是氢,烷基,芳基或芳烷基; 并且n为2,其中R 1为双官能部分,1为任何其它R 1; X为Cl,Br,I或OSO 2 Y; 其中Y是烷基,三卤代甲基,苯基,卤代苯基或烷基苯基。
摘要:
The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
摘要:
Novel homogeneous bimetallic hydroformylation catalysts, and processes utilizing these catalysts to convert alkenes, particularly alpha olefins, under mild conditions to a product rich in aldehydes, particularly a product containing a high ratio of linear:branched chain aldehydes. The catalysts can be produced from a binucleating tetratertiaryphosphine ligand capable of strongly coordinating two metal centers and holding them in general proximity to one another. Bimetallic catalyst precursors are produced which, on reaction with carbon monoxide and hydrogen forms the active bimetallic hydroformylation catalyst system.
摘要:
A ruthenium-phosphine complex represented by the formula:[RuXY(BINAP)].sub.nwherein n is an integer of from 1 to about 10; and X and Y independently represent nonchelating anionic ligands.