Abstract:
Catalysts suitable for asymmetric hydrogenation reactions is described comprising the reaction product of a group (8) transition metal compound a chiral phosphine and a chiral diamine of formula (1) in which R 1 , R 2 R 3 or R 4 are independently hydrogen, a saturated or unsaturated alkyl, or cycloalkyl group, an aryl group, a urethane or sulphonyl group and R 5 , R 6 , R 7 or R 8 are independently hydrogen, a saturated or unsaturated alkyl or cycloalkyl group, or an aryl group, at least one of R 1 , R 2 , R 3 or R 4 is hydrogen and A is a linking group comprising one or two substituted or unsubstituted carbon atoms.
Abstract:
The present invention provides a process for the preparation of a Pd(0)L n complex, where L is a ligand and n is 2, 3 or 4, comprising the steps of: (a) reacting a Pd(II) complex in at least one solvent with a base and ligand L; and (b) if required, adding further base, optionally in at least one solvent, to form the Pd(0)L n complex; wherein the at least one solvents in steps a and b are independently the same or different, and provided that when n = 2, the Pd(II) complex is not bis[tri(ortho-tolyl)phosphine] palladium chloride. The invention also provides novel Pd(0)L 2 and Pd(II) complexes.
Abstract:
A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH 2 , oxygen or sulphur; R- 1 , R 2 and R 3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R 4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.
Abstract:
A process for preparing (S)-(+)- 10,11 -dihydro-10-hydroxy-5H- dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,l l-dihydro-10-hydroxy-5H- dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX 2 (L)] 2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R 1 is chosen from C 1-6 alkoxy and C 1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R 1 can be the same or different, and R 2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR 3 R 4 R 5 and formic acid, [R 3 R 4 R 5 NH][OOCH] and optionally formic acid, or [M][OOCH] x and formic acid, wherein R 3 , R 4 and R 5 are C 1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.
Abstract translation:制备(S) - (+) - 10,11-二氢-10-羟基-5H-二苯并/ b,f /吖庚因-5-甲酰胺或(R) - ( - ) - 10,11-二氢 公开了在催化剂和氢化物源的存在下还原奥卡西平的方法,将10-羟基-5H-二苯并/ b,f /吖庚因-5-甲酰胺。 催化剂由[RuX 2(L)] 2 N的组合制备,其中X是氯,溴或碘,L是芳基或芳基 - 脂族配体, 与式(A)或式(B)的配位体反应:其中R 1选自C 1-6烷氧基和C 1-6 - >烷基,n是0至5的数,当n是2至5的数时,R 1可以相同或不同,R 2是 烷基,取代的烷基,芳基,取代的芳基,烷芳基或取代的烷芳基。 氢化物源是NR 3 S 4 R 5和甲酸,[R 3 S 3 R 5] 4 O 5 H] [OOCH]和任选的甲酸或[M] [OOCH] x X和甲酸,其中R 3, R 4,R 4和R 5是C 1-6烷基,M是碱金属或碱土金属,x是1 或2.在该过程中维持6.5至8的pH。
Abstract:
Catalysts suitable for asymmetric hydrogenation reactions is described comprising the reaction product of a group (8) transition metal compound a chiral phosphine and a chiral diamine of formula (1) in which R , R R or R are independently hydrogen, a saturated or unsaturated alkyl, or cycloalkyl group, an aryl group, a urethane or sulphonyl group and R , R , R or R are independently hydrogen, a saturated or unsaturated alkyl or cycloalkyl group, or an aryl group, at least one of R , R , R or R is hydrogen and A is a linking group comprising one or two substituted or unsubstituted carbon atoms.
Abstract translation:描述了适合于不对称氢化反应的催化剂,其包含组(8)过渡金属化合物,手性膦和式(1)的手性二胺的反应产物,其中R 1,R 2 R 3或R R 4,R 7或R 8独立地为氢,饱和或不饱和的烷基或环烷基,芳基,氨基甲酸酯或磺酰基,并且R 5,R 6,R 7或R 8独立地为氢, 饱和或不饱和的烷基或环烷基,或芳基,R 1,R 2,R 3或R 4中的至少一个为氢且A为包含一个或两个取代基 或未被取代的碳原子。
Abstract:
A diamine of formula (I) is described, in which A is hydrogen or a saturated or unsaturated C1-C20 alkyl group or an aryl group; B is a substituted or unsubstituted C1-C20 alkyl, cycloalkyl, alkaryl, alkaryl or aryl group or an alkylamino group and at least one of X 1 , X 2 , Y 1 , Y 2 or Z is a C1-C10 alkyl, cycloalkyl, alkaryl, aralkyl or alkoxy substituting group. The chiral diamine may be used to prepare catalysts suitable for use in transfer hydrogenation reactions.
Abstract:
The present invention provides a process for the preparation of a complex of formula (I) comprising the steps of: (a) mixing Pd(diolefin)Br 2 and t Bu 3 P in a solvent; and (b) adding an alkali hydroxide to form the complex of formula (I).
Abstract:
A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH 2 , oxygen or sulphur; R- 1 , R 2 and R 3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R 4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.