- AN IMPROVED PROCESS FOR THE PREPARATION OF TRIAZOLE DERIVATIVES
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The present invention relates to an improved process for the preparation of triazole derivatives such as ravuconazole and isavuconazole.
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- Asymmetric Catalytic Epoxidation of Terminal Enones for the Synthesis of Triazole Antifungal Agents
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An enantioselective epoxidation of α-substituted vinyl ketones was realized to construct the key epoxide intermediates for the synthesis of various triazole antifungal agents. The reaction proceeded efficiently in high yields with good enantioselectivities by employing a chiral N,N′-dioxide/ScIII complex as the chiral catalyst and 35% aq. H2O2 as the oxidant. It enabled the facile transformation for optically active isavuconazole, efinaconazole, and other potential antifungal agents.
- Feng, Xiaoming,He, Qianwen,Liu, Xiaohua,Zhang, Dong,Zhang, Fengcai
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p. 6961 - 6966
(2021/09/11)
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- Crystal form of isavuconazole and preparation method thereof
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The invention relates to a crystal form I of isavuconazole, a preparation method and application thereof. X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, hygroscopicity analysis and other means are employed for comprehensive characterization of the crystal form I of isavuconazole, and the invention finds that the crystal form I has more excellent stability than amorphism. The preparation method of the crystal form I of isavuconazole has the characteristics of simple operation, easy control and good reproducibility.
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Paragraph 0106-0117; 0120-0125
(2019/01/24)
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- Preparation method of liconazole sulfate and intermediate thereof (by machine translation)
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The preparation method disclosed by the invention has, the advantages that the preparation process efficiency of the idazooconazole sulfate and the. intermediate thereof is higher by no need C2 for column A4 chromatography and purification . and the method disclosed by, the invention only needs. to be subjected to deprotecting A4 and ion exchange by simple purification. (by machine translation)
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- Method for manufacturing isavuconazole or ravuconazole
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The invention provides a method for manufacturing a triazole compound isavuconazole or ravuconazole which is enriched by a diastereoisomer and enantiomer. The method comprises the following steps: a Reformatsky reaction is carried out between ketone and dihalogeno metal propionitrile; an enantiomer mixture is generated, and separation is carried out. The method can obviously reduce steps for synthesis of isavuconazole or ravuconazole, yield of products is improved, and production cost is reduced.
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- Preparation method of isavuconazole and isavuconazole prepared through method
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The invention relates to a preparation method of isavuconazole and isavuconazole prepared through the method.The preparation method comprises the following steps that 1, diflurophenyl acetylchloride, triazole, CuI, potassium carbonate and first organic solvent are sequentially added into a reaction kettle, reacting under stirring is performed at the temperature of 80 DEG C-100 DEG C, and then purifying is performed to obtain a first product; 2, propionitrile, a catalyst and second organic solvent are added into a reaction container, the temperature is lowered to minus 20 DEG C-minus 5 DEG C, the second organic solvent containing the first product is dropwise added, reacting and purifying are performed to obtain a second product, and a mixture composed of C-9 primary amine quinine and copper pigment alkali is adopted as the catalyst; 3, the second product is added into another reaction container, diethylphosphorodithioate, water and mixed isopropanol solvent are added into the reaction container, heating is performed until the temperature is increased to 80 DEG C-90 DEG C, reacting under stirring and purifying are sequentially performed, and a third product is obtained; 4, the third product, 2-bromo-4'-acetylbenzonitrile and third organic solvent are mixed, react under stirring at the temperature of 60 DEG C-70 DEG C and then purified, and the isavuconazole is obtained.Accordingly, a novel synthetic route is redesigned, and the reaction steps are reduced.
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Paragraph 0019; 0026
(2016/10/10)
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- NOVEL STABLE POLYMORPHS OF ISAVUCONAZOLE OR ITS SALT THEREOF
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The present invention relates to novel stable novel stable polymorphs of Isavuconazole or its salt thereof, having purity more than 90 % when measured by HPLC. In particular the present invention directs process for the preparation of solid amorphous and crystalline form of Isavuconazole base. In a further embodiment present invention directs to crystalline form Isavuconazole Hydrobromide salt and oxalate salt of 2-(2,5-difluoro- phenyl)-1-[1,2,4]triazol-1-yl-butane-2,3-diol.
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Page/Page column 15
(2016/05/02)
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- Process for the manufacture of enantiomerically pure antifungal azoles as ravuconazole and isavuconazole
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A new technical process for preparation of enantiomerically pure antifungal compounds of formula I by resolution of the racemates has been disclosed.
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- Azoles for treatment of fungal infections
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Azole derivatives of the formula I wherein R14, R15are each independently hydrogen or fluorine, T is a group of the formula: wherein R9is pyrrolidinyl or a group A—NH—B—, A is hydrogen or straight-chain or branched C1-C5alkyl; B is straight-chain or branched C1-C4alkylene, —CH2—CONH—CH2or —CH2CH2CH2—CH(NH2); and X?is a pharmaceutically acceptable anion; and pharmaceutically acceptable salts of said compounds, and hydrates and solvates of the compounds of formula I and the salts thereof can be used in the production of medicaments for treating fungal infections and mycoses.
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