Abstract: The invention relates to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid which is in a crystalline form or in at least partially crystalline form as a monohydrate or anhydrate, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor).

Abstract: The invention relates to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid, and to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid which is in a crystalline form or in at least partially crystalline form, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor).

Abstract: The present invention relates to a process for the preparation of a compound of the formula I, which comprises reacting a compound of the formula IV with the compound of formula VII R15-A2-CHO and to novel intermediate compounds used therein.

Abstract: The invention relates to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid, and to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid which is in a crystalline form or in at least partially crystalline form, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor).

Abstract: The invention relates to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid which is in a crystalline form or in at least partially crystalline form as a monohydrate or anhydrate, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor).

Abstract: The present invention relates to a process for the preparation of a compound of the formula I, which comprises reacting a compound of the formula IV with the compound of formula VII R15-A2-CHO and to novel intermediate compounds used therein.

Abstract: Process for preparing nitriles by reacting N-alkylcarboxamides (RCO—NHR1) or ammonium salts of carboxylic acids (RCOO—NH3R1+) or carboxylic acids in the presence of alkylamines or ammonium salts (RCOOH+NH2R1, RCOOH+NH3R1+), respectively, R being an arbitrarily substituted linear or branched C1-C12-alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl, alkynyl or aryl or heteroaryl radical and R1 being an arbitrary substituted, linear or branched C2-C1 alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl or alkynyl radical, with phosphonic anhydrides in the presence of an optional base in an organic solvent at a temperature in the range from ?30 to 180° C.

Abstract: A method for producing unprotected or carbamate-protected amines of formulae (II) and (III) or R1—NH2 (II) or R1—NHCO2R2 (III) by reacting hydroxamic acids of formula (I) (R1 CONHOH) with a) alkylpliosphonic acid anhydrite's, b) alcohol R2OH and c) optionally with a base, at a temperature ranging from 100 to +120°C., wherein the hydroxainic acid (I) is produced prior to or during reacting (in situ) and R1 is an optionally substituted linear or branched C1-C12 alkyl radical, substituted C3-C10 cycloalkyl, alkenyl, aryl or heteroaryl radical and R2 is an open-chain, cyclic or branched allyl, aryl or C1 to C12-alkyl radicals, or aryloxy, allyloxy or alkoxy radical possibly substituted with open-chain, cyclic or branched C1 to C12-alkyl radicals.

Abstract: Process for preparing nitriles by reacting N-alkylcarboxamides (RCO—NHR1) or ammonium salts of carboxylic acids (RCOO—NH3R1+) or carboxylic acids in the presence of alkylamines or ammonium salts (RCOOH+NH2R1, RCOOH+NH13R1+) respectively, R being an arbitrarily substituted linear or branched C1-C12-alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl, alkynyl or aryl or heteroaryl radical and R1 being an arbitrary substituted, linear or branched C2-C1 alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl or alkynyl radical, with phosphonic anhydrides in the presence of an optional base in an organic solvent at a temperature in the range from ?30 to 180° C.

Abstract: A method for producing unprotected or carbamate-protected amines of formulae (II) and (III) or R1—NH2 (II) or R1—NHCO2R2 (III) by reacting hydroxamic acids of formula (I) (R1CONHOH) with a) alkylphosphonic acid anhydrite's, b) alcohol R2OH and c) optionally with a base, at a temperature ranging from 100 to +120° C., wherein the hydroxamic acid (I) is produced prior to or during reacting (in situ) and R1 is an optionally substituted linear or branched C1-C12 alkyl radical, substituted C3-C10 cycloalkyl, alkenyl, aryl or heteroaryl radical and R2 is an open-chain, cyclic or branched allyl, aryl or C1 to C12-alkyl radicals, or aryloxy, allyloxy or alkoxy radical possibly substituted with open-chain, cyclic or branched C1 to C12-alkyl radicals.

Abstract: The invention relates to a method for producing single enantiomer epoxides by reducing ?-leaving group-substituted ketones with (R)- or (S)-selective alcohol dehydrogenases in the presence of a cofactor and optionally a suitable system for regenerating the oxidised cofactor, to produce the corresponding single enantiomer alcohols and subsequently, by means of cyclisation induced by a base, the corresponding single enantiomer epoxides (EQUATION 1) wherein LG may stand for F, Cl, Br, I, OSO2Ar, OSO2CH3, OSO2R or OP(O)OR2, and R1, R2 and R3, independently of one another, stand for hydrogen, a branched or unbranched, optionally substituted C1-C20-alkyl radical, symbolize an optionally randomly substituted C3-C1-10-cycloalkyl or alkenyl radical or a randomly substituted carbo- or heterocyclic aryl radical, or correspond to a radical from the group CO2R, CONR2, COSR, CS2R, C(NH)NR2, CN, CHaI3, ArO, ArS, RO, RS, CHO, OH, NHR, NR2, Cl, F, Br, I or SiR3.

Abstract: The invention relates to a method for producing the nitrites of formula: R1—CN by reacting aldehyde oximes (R1CN?N—OH) with cyclic alkylphosphonic anhydrides at a temperature ranging from ?100 to +120° C., wherein R1 represents H, a linear or branched C1-C12 alkyl group, a C3-C10 cycloalkyl, alkenyl or an aryl or heteroaryl group. The cyclic phosphonic anhydride preferably used is a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide of formula (I), wherein R? independently represents allyl, aryl or open-chain or branched C1 to C12 alkyl groups.

Abstract: The invention relates to a method for producing the nitrites of formula: R1—CN by reacting aldehyde oximes (R1CN?N—OH) with cyclic alkylphosphonic anhydrides at a temperature ranging from ?100 to +120° C., wherein R1 represents H, a linear or branched C1-C12 alkyl group, a C3-C10 cycloalkyl, alkenyl or an aryl or heteroaryl group. The cyclic phosphonic anhydride preferably used is a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide of formula (I), wherein R? independently represents allyl, aryl or open-chain or branched C1 to C12 alkyl groups.

Abstract: The invention relates to a method for producing alkenes of formula R1R2C?CR3R4 by the reaction of a) primary alcolhols (R1R2CHCH2—OH) or b) secondary alcohols (R1R2CHCHR3—OH) or c) tertiary alcohols (R1R2CH—CR3R4OH) with cyclic alkylphosphonic acid anhydrides at a temperature ranging between ?100 and +120° C., whereby R and/or R1 and/or R2 and/or R3 and/or R4 represent H, a linear or branched C1-C12 alkyl group, or a C3-C10 cycloalkyl group, alkenyl group or an aryl group or heteroaryl group. Preferably, a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide of formula (I) is used as the cyclic phosphonic acid anhydride, where R? represents, (independently of one another), allyl, aryl or open-chained or branched C1-C12 alkyl groups. Optionally the reaction can be carried out in the presence of a tertiary amine base NR53.

Abstract: The invention relates to a method for the production of a.) aldehydes of formula (II): R1—CHO and b.) aldehydes of formula (III): R1—C(O)—R2 by reacting a.) primary alcohols (R1CH2—OH) or b.) secondary alcohols (R1—CH(OH)—R2) with cyclic phosphonic acid anhydrides in the presence of dialkyl-, diaryl- and/or alkyl-aryl sulphonic oxides at a temperature in the region of between ?100 to +120° C., whereby R1 and/or R2 represent H, a substituted linear or branched C1-C12-alkyl radical, a substituted C3-C10 cycloalkyl-, alkenyl-, aryl- or heteroaryl radical. A cyclic phosphonic acid anhydride is used, preferably, as a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane of formula (I), wherein R? independently represents allyl, aryl or open-chained or branched C1-C12-alkyl-radicals.

Abstract: The invention relates to a method for the production of a.) aldehydes of formula (II): R1—CHO and b.) aldehydes of formula (III): R1—C(O)—R2 by reacting a.) primary alcohols (R1CH2—OH) or b.) secondary alcohols (R1—CH(OH)—R2) with cyclic phosphonic acid anhydrides in the presence of dialkyl-, diaryl- and/or alkyl-aryl sulphonic oxides at a temperature in the region of between ?100 to +120° C., whereby R1 and/or R2 represent H, a substituted linear or branched C1-C12-alkyl radical, a substituted C3-C10 cycloalkyl-, alkenyl-, aryl- or heteroaryl radical. A cyclic phosphonic acid anhydride is used, preferably, as a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane of formula (I), wherein R? independently represents allyl, aryl or open-chained or branched C1-C12-alkyl-radicals. Optionally, the reaction can be carried out in the presence of a tertiary amine base NR53.