摘要:
This disclosure is directed to methods of preparing organic aldehydes, each method comprising contacting a terminal olefin with an oxidizing mixture comprising: (a) a dichloro-palladium complex; (b) a copper complex; (c) a source of nitrite; under aerobic reaction conditions sufficient to convert at least a portion of the terminal olefin to an aldehyde.
摘要:
Present invention relates to a method of preparing a chiral α- or β-substituted ketone from the corresponding β- or γ-substituted aldehyde, wherein the ketone has formula (I), (III) or (V), and the corresponding aldehyde has formula (II), (IV) or (VI), respectively, the method comprising reacting the aldehyde of formula (II), (IV) or (VI) in the presence of an amine, oxygen and an organic solvent, wherein the reaction is carried out in the absence of a metal-based catalyst or a metal-based oxidant, wherein: R is H, a substituted or unsubstituted C1-C10 alkyl, substituted or unsubstituted C2-C15 alkenyl, substituted or unsubstituted C2-C15 alkynyl, substituted or unsubstituted C3-C15 cycloalkyl, substituted or unsubstituted C3-C15 cycloalkenyl, substituted or unsubstituted C3-C15 heterocycloalkyl, substituted or unsubstituted C3-C15 heterocycloalkenyl, substituted or unsubstituted C6-C15 aryl, or substituted or unsubstituted C6-C15 heteroaryl; and R′ is H, a substituted or unsubstituted C1-C10 alkyl, substituted or unsubstituted C2-C15 alkenyl, substituted or unsubstituted C2-C15 alkynyl, substituted or unsubstituted C3-C15 cycloalkyl, substituted or unsubstituted C3-C15 cycloalkenyl, substituted or unsubstituted C3-C15 heterocycloalkyl, substituted or unsubstituted C3-C15 heterocycloalkenyl, substituted or unsubstituted C6-C15 aryl, or substituted or unsubstituted C6-C15 heteroaryl.
摘要:
The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren Inter alia the invention relates to a process for the manufacture of a compound of the formula I. or a salt thereof, wherein R1 as well as Act are as defined in the specification, and processes of manufacturing this compound as well as intermediates in this process.
摘要:
A process for oxidizing primary and secondary alcohols to the corresponding aldehydes and ketones is disclosed. The oxidation is carried out by reacting the primary or secondary alcohol with an organic N-chloro compound oxidizing agent in the presence of a catalyst of the formula: ##STR1## wherein the substituent groups are as defined in the specification.
摘要:
An antibody molecule or molecule containing antibody combining site portions (catalytic molecule) that catalytically hydrolyzes a preselected carboxylic acid amide or ester bond of a reactant ligand, methods of making and using the catalytic molecule, and cells that produce those molecules are disclosed. The catalytic molecules bind to a reactant ligand containing the bond to be hydrolyzed and also to a haptenic ligand. The haptenic ligand is structurally analogous to the reactant ligand and contains a tetrahedral carbon atom that is bonded to a hydroxyl group and to a saturated carbon atom at a position in the haptenic ligand that corresponds to position of the carbonyl group and its bonded heteroatom of the reactant ligand. The haptenic ligand also contains a group that bears an ionic charge in aqueous solution at physiological pH values that is not present at a corresponding position of the reactant ligand. The ionic charge-bearing group is located in the hapten within 7 .ANG.ngstroms of the tetrahedral carbon atom.
摘要:
N-substituted 3,4,5,6-tetrahydrophthalimides and their intermediates of the general formula I ##STR1## where A is --NO.sub.2, --NH.sub.2 or ##STR2## corresponding to the compounds Ia, Ib and Ic, B is --CH.sub.2 --, --CH.sub.2 --CHR.sup.1 --, --CH.sub.2 --CHR.sup.1 --CH.sub.2 --, --CH.dbd., --CH.dbd.CR.sup.1 -- or --CH.dbd.CR.sup.1 --CH.dbd., R.sup.1 being --H, --Cl, --Br or --CH.sub.3, D is ##STR3## depending on the terminal group B, X is --H, --Cl or --Br, Y is --H, C.sub.1 -C.sub.7 --alkyl, --Cl, --Br, --CN, --CONH.sub.2 --CO.sub.2 R.sup.2, where R.sup.2 is H, C.sub.1 -C.sub.6 -alkyl, C.sub.5 -- or C.sub.6 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylmercapto-C.sub.2 -C.sub.4 -alkyl, propargyl, benzyl, .alpha.-phenylethyl, .alpha.-phenylpropyl, C.sub.2 -C.sub.4 -alkyl which is monosubstituted, disubstituted or trisubstituted by F or Cl, or CH.sub.3 -substituted or Cl-substituted allyl, and Z is --COOR.sup.2, --CONR.sup.3 R.sup.4, ##STR4## where R.sup.3 and R.sup.4 are each H or C.sub.1 -C.sub.4 -alkyl or together form a 5-membered or 6-membered cycloaliphatic ring whose carbon chain may be interrupted by an oxygen atom.