99368-66-8Relevant articles and documents
Novel micro-channel preparation process of 2-hydroxy-3-trifluoromethyl-5-nitropyridine
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Paragraph 0031-0071; 0081-0082, (2021/08/14)
The invention discloses a novel micro-channel preparation process of 2-hydroxy-3-trifluoromethyl-5-nitropyridine, and belongs to the technical field of pharmaceutical chemicals. The novel micro-channel preparation process comprises the following steps of: (1) stirring 2-hydroxy-3-trifluoromethylpyridine and a solvent sulfuric acid for 10-30 minutes; (2) stirring nitric acid and sulfuric acid for 30-60 minutes to obtain nitro-sulfur mixed acid; (3) filling a micro-channel pipeline with the mixed solution obtained in the step (1) at a low speed; (4) introducing the nitro-sulfur mixed acid obtained in the step (2) into the micro-channel, controlling the material flow rate to be 9-15mL/min and the reaction time to be 10-40s, and introducing a nitryl positive ion group on 2-hydroxy-3-trifluoromethylpyridine; (5) introducing the reaction liquid obtained in the step (4) into ice water from the outlet end of a reactor for quenching; and (6) carrying out suction filtration on the solid-liquid mixed solution obtained in the step (5), and repeatedly washing with water to obtain the 2-hydroxy-3-trifluoromethyl-5-nitropyridine. The method has the advantages of excellent production safety, high yield, high product purity, simple steps and production cost saving.
Solid dispersions containing an apoptosis-inducing agent
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Page/Page column 208-209, (2019/03/15)
A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
IMIDAZOLE DIKETONE COMPOUND AND USE THEREOF
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Paragraph 0073; 0074; 0075, (2016/06/28)
Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds possess androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.