Abstract:
The present invention provides enzymatic processes for preparing optically active compounds of Formula (I) wherein X, E and * have the meanings defined in the specification. The invention also provides chiral intermediates useful for preparing compound of Formula (I) and enzymatic processes for preparing such chiral intermediates.
Abstract:
Phenyl acetic acid derivatives of formula (I) in which the substituents and index have the following meanings: X is oxygen or sulphur; R is hydrogen and alkyl; R is hydrogen and alkyl; R is cyano, nitro, trifluoromethyl, halogen, alkyl and alkoxy; m is 0, 1 ou 2, in which the radicals R may be different if m is 2; R is hydrogen, cyano, nitro, hydroxy, amino, halogen, alkyl, halogen alkyl, alkoxy, halogen alkoxy, alkylthio, alkylamino or dialkylamino; R is hydrogen, cyano, nitro, hydroxy, amino, halogen, possibly substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, alkenyl, alkenyloxy, alkenylthio, alkenylamino, N-alkenyl-N-alkylamino, alkinyl, alkinyloxy, alkinylthio, alkinylamino, N-alkinyl-N-alkylamino; optionally substituted cycloalkyl, cycloalkyloxy, cycloalkylthio, cycloalkylamino, N-cycloalkyl-N-alkylamino, cycloalkenyl, cycloalkenyloxy, cycloalkenylthio, cycloalkenylamino, N-cycloalkenyl-N-alkylamino, heterocyclyl, heterocyclyloxy, heterocyclylthio, heterocyclylamino, N-heterocylcyl-N-alkylamino, aryl, aryloxy, arylthio, arylamino, n-aryl-n-alkylamino, hetaryl, hetaryloxy, hetarylthio, hetarylamino, N-hetaryl-N-alkylamino; R is hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, alkinyl, alkylcarbonyl, alkenylcarbonyl, alkinylcarbonyl or alkylsulfonyl; optionally substituted aryl, arylcarbonyl, arylsulfonyl, hetaryl, hetarylcarbonyl or hetarylsulphonyl; and their salts, process and intermediate products for their production, and their use.
Abstract:
The present invention relates to an optically active (2S,3R)-4-cyanobutan-1,2,3-triol derivative, a process for preparing same, and a process for preparing 2-deoxy-L-ribose from same.
Abstract:
A method for generating a selected set of codons is disclosed; the method includes the steps of: (a) providing a first set of mononucleosides, mononucleotides, dinucleotides, or mixture thereof, where a subset A of the first set is protected with a protecting group A', and a subset B of the first set is protected with a protecting group B', where A' and B' are orthogonal protecting groups; (b) selectively removing the protecting group A' from subset A; (c) coupling the products of step (b) with a second set of mononucleosides, mononucleotides, dinucleotides, or a mixture thereof, where the second set is protected with protecting group A'; (d) optionally removing protecting group A' from the products of step (c); (e) optionally coupling the products of step (d) with a third set of mononucleosides, where the third set is protected with protecting group A'; (f) selectively removing the protecting group B' from subset B; (g) coupling the products of step (f) with a fourth set of mononucleosides, mononucleotides, dinucleotides, or a mixture thereof, where the fourth set is protected with protecting group A' or protecting group B'; (h) optionally selectively removing protecting group B' from the products of step (g); and (i) optionally coupling the products of step (h) with a fifth set of mononucleosides, to yield a selected set of codons.
Abstract:
The present invention pertains to a process for preparing 3-hydroxy-3-methylbutyrate (HMB) or a salt thereof, the method comprising (a) reacting isobutylene oxide with cyanide in order to obtain 3- hydroxy-3-methylbutyronitrile, and (b) hydrolyzing the 3-hydroxy-3-methylbutyronitrile obtained in step (a) in order to obtain HMB, wherein hydrolysis step (b) is performed using either at least one nitrilase enzyme or, alternatively, using a combination of enzymes, said combination comprising at least one nitrile hydratase and at least one amidase.
Abstract:
A method for generating a selected set of codons is disclosed; the method includes the steps of: (a) providing a first set of mononucleosides, mononucleotides, dinucleotides, or mixture thereof, where a subset A of the first set is protected with a protecting group A', and a subset B of the first set is protected with a protecting group B', where A' and B' are orthogonal protecting groups; (b) selectively removing the protecting group A' from subset A; (c) coupling the products of step (b) with a second set of mononucleosides, mononucleotides, dinucleotides, or a mixture thereof, where the second set is protected with protecting group A'; (d) optionally removing protecting group A' from the products of step (c); (e) optionally coupling the products of step (d) with a third set of mononucleosides, where the third set is protected with protecting group A'; (f) selectively removing the protecting group B' from subset B; (g) coupling the products of step (f) with a fourth set of mononucleosides, mononucleotides, dinucleotides, or a mixture thereof, where the fourth set is protected with protecting group A' or protecting group B'; (h) optionally selectively removing protecting group B' from the products of step (g); and (i) optionally coupling the products of step (h) with a fifth set of mononucleosides, to yield a selected set of codons.
Abstract:
Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents optionally substituted phenyl, naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or indazolyl; Z represents O, S or NR8; X and Y are H or are together =O; R?1 and R2¿ are H; optionally substituted C¿1-6?alkyl; optionally substituted phenyl(C1-4alkyl); COR?c; CO¿2R?c; CONRcRd; CONRcCOORd¿; or SO¿2R?c; R3 is H or C¿1-6?alkyl, R?4¿ is H, C¿1-6?alkyl or optionally substituted phenyl; and R?5¿ represents optionally substituted phenyl; are tachykinin antagonists. They and compositions thereof are useful in therapy.