Patent classifications
C07C253/00
PROCESS FOR MAKING MIXTURES OF ENANTIOMERS, AND MIXTURES OF ENANTIOMERS
Process for preparation of a mixture of methyl glycine diacetic acid (MGDA) or its respective mono-, di-, trialkali metal salt or its respective mono-, di- or tri-ammonium salt or mixtures thereof, and glutamic acid diacetic acid (GLDA) or its respective mono-, di-, tri-, or tetra-alkali metal or mono-, di-, tri- or tetra-ammonium salt or mixtures thereof, wherein said process com-prises the steps of: (a) dissolution in water of (a1) alanine in its L- or D-enantiomeric form or its respective monoalkali metal salt or mixtures thereof, and (a2) glutamic acid as L- or D-enantiomer or its respective mono-, or dialkali metal or mixtures thereof, wherein the molar ratio of alanine to glutamic acid is in the range of from 1:9 to 9:1, (b) converting the mixture obtained in step (a) with formaldehyde and hydrocyanic acid or alkali metal cyanide to the corresponding dinitriles, (c) saponification of the dinitriles resulting from step (b).
PROCESS FOR MAKING MIXTURES OF ENANTIOMERS, AND MIXTURES OF ENANTIOMERS
Process for preparation of a mixture of methyl glycine diacetic acid (MGDA) or its respective mono-, di-, trialkali metal salt or its respective mono-, di- or tri-ammonium salt or mixtures thereof, and glutamic acid diacetic acid (GLDA) or its respective mono-, di-, tri-, or tetra-alkali metal or mono-, di-, tri- or tetra-ammonium salt or mixtures thereof, wherein said process com-prises the steps of: (a) dissolution in water of (a1) alanine in its L- or D-enantiomeric form or its respective monoalkali metal salt or mixtures thereof, and (a2) glutamic acid as L- or D-enantiomer or its respective mono-, or dialkali metal or mixtures thereof, wherein the molar ratio of alanine to glutamic acid is in the range of from 1:9 to 9:1, (b) converting the mixture obtained in step (a) with formaldehyde and hydrocyanic acid or alkali metal cyanide to the corresponding dinitriles, (c) saponification of the dinitriles resulting from step (b).
Oxidation Catalysts
Disclosed are catalysts comprised of platinum and gold. The catalysts are generally useful for the selective oxidation of compositions comprised of a primary alcohol group and at least one secondary alcohol group wherein at least the primary alcohol group is converted to a carboxyl group. More particularly, the catalysts are supported catalysts including particles comprising gold and particles comprising platinum, wherein the molar ratio of platinum to gold is in the range of about 100:1 to about 1:4, the platinum is essentially present as Pt(0) and the platinum-containing particles are of a size in the range of about 2 to about 50 nm. Also disclosed are methods for the oxidative chemocatalytic conversion of carbohydrates to carboxylic acids or derivatives thereof. Additionally, methods are disclosed for the selective oxidation of glucose to glucaric acid or derivatives thereof using catalysts comprising platinum and gold. Further, methods are disclosed for the production of such catalysts.
Oxidation Catalysts
Disclosed are catalysts comprised of platinum and gold. The catalysts are generally useful for the selective oxidation of compositions comprised of a primary alcohol group and at least one secondary alcohol group wherein at least the primary alcohol group is converted to a carboxyl group. More particularly, the catalysts are supported catalysts including particles comprising gold and particles comprising platinum, wherein the molar ratio of platinum to gold is in the range of about 100:1 to about 1:4, the platinum is essentially present as Pt(0) and the platinum-containing particles are of a size in the range of about 2 to about 50 nm. Also disclosed are methods for the oxidative chemocatalytic conversion of carbohydrates to carboxylic acids or derivatives thereof. Additionally, methods are disclosed for the selective oxidation of glucose to glucaric acid or derivatives thereof using catalysts comprising platinum and gold. Further, methods are disclosed for the production of such catalysts.
Oxidation Catalysts
Disclosed are catalysts comprised of platinum and gold. The catalysts are generally useful for the selective oxidation of compositions comprised of a primary alcohol group and at least one secondary alcohol group wherein at least the primary alcohol group is converted to a carboxyl group. More particularly, the catalysts are supported catalysts including particles comprising gold and particles comprising platinum, wherein the molar ratio of platinum to gold is in the range of about 100:1 to about 1:4, the platinum is essentially present as Pt(0) and the platinum-containing particles are of a size in the range of about 2 to about 50 nm. Also disclosed are methods for the oxidative chemocatalytic conversion of carbohydrates to carboxylic acids or derivatives thereof. Additionally, methods are disclosed for the selective oxidation of glucose to glucaric acid or derivatives thereof using catalysts comprising platinum and gold. Further, methods are disclosed for the production of such catalysts.
A NOVEL PROCESS FOR THE PREPARATION OF TERIFLUNOMIDE
The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride.
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A NOVEL PROCESS FOR THE PREPARATION OF TERIFLUNOMIDE
The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride.
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SYNTHESIS OF RAS INHIBITORS
The present invention relates to Ras inhibitors and to methods for preparing Ras inhibitors.
Process for separating an isocyanate prepared by phosgenation of a primary amine in the gas phase from the gaseous crude product of the phosgenation
The present invention relates to a process for separating an isocyanate prepared by reaction of a primary amine with an excess of phosgene in the gas phase from the gaseous crude product obtained in the reaction, wherein (i) the gaseous crude product is partially liquefied by contacting with a quenching liquid, (ii) the gas phase obtained in step (i) is partially condensed, (iii) the condensate obtained in step (ii) is used as the quenching liquid in step (i), (iv) the portions of the gas phase that were not condensed in step (ii) are at least partially liquefied, (v) the liquid phase obtained in step (iv) is likewise used as the quenching liquid in step (i), and (vi) the liquid phase obtained in step (i) is worked up to the pure isocyanate without previously being used as quenching liquid.
Synthesis of thiohydantoins
A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.