857040-74-5Relevant academic research and scientific papers
Enzyme-Loaded Hemin/G-Quadruplex-Modified ZIF-90 Metal–Organic Framework Nanoparticles: Bioreactor Nanozymes for the Cascaded Oxidation of N-hydroxy-l-arginine and Sensing Applications
Chen, Chaochao,O'Hagan, Michael P.,Ouyang, Yu,Vázquez-González, Margarita,Wang, Zhanhui,Willner, Itamar
, (2022/01/19)
Biocatalytic cascades are challenging to operate in homogeneous solution, where diffusional mass transport hinders efficient communication between the reactive components. There is great interest in developing devices to perform such transformations in co
ISOINDOLE DERIVATIVE
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Paragraph 0226, (2021/02/25)
Disclosed is a compound of formula (I) and a stereoisomer thereof: wherein R1, R2, R3 and R4 are as defined in the present disclosure.
Visible-Light-Mediated Dearomatisation of Indoles and Pyrroles to Pharmaceuticals and Pesticides
Schilling, Waldemar,Zhang, Yu,Riemer, Daniel,Das, Shoubhik
supporting information, p. 390 - 395 (2019/12/15)
Dearomatisation of indole derivatives to the corresponding isatin derivatives has been achieved with the aid of visible light and oxygen. It should be noted that isatin derivatives are highly important for the synthesis of pharmaceuticals and bioactive compounds. Notably, this chemistry works excellently with N-protected and protection-free indoles. Additionally, this methodology can also be applied to dearomatise pyrrole derivatives to generate cyclic imides in a single step. Later this methodology was applied for the synthesis of four pharmaceuticals and a pesticide called dianthalexin B. Detailed mechanistic studies revealed the actual role of oxygen and photocatalyst.
Synthesis method of methyl 2-acetyl-6-aminobenzoate
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Paragraph 0055; 0057; 0058; 0069; 0071; 0072, (2020/05/01)
The invention provides a synthesis method of methyl 2-acetyl-6-aminobenzoate. The target product methyl 2-acetyl-6-aminobenzoate is prepared from cheap and easily available 3-nitrophthalic acid through a six-step reaction. The synthesis method has the characteristics of easily available raw materials, short route, high yield, easiness in operation, small environmental pollution and the like, and is suitable for large-scale industrial production.
Palladium Supported on Carbon Nanoglobules as a Promising Catalyst for Selective Hydrogenation of Nitroarenes
Mironenko,Belskaya,Stepanova,Gulyaeva,Trenikhin,Likholobov
, p. 888 - 900 (2019/11/11)
The catalysts 1?wt% palladium supported on carbon nanoglobules (CNGs) were shown to be highly active in the liquid-phase hydrogenation of various nitroarenes and provided nearly 100% selectivity to aromatic amines at complete conversion under mild conditions (323?K, 0.5?MPa, 1?h). The catalytic activity (in terms of turnover frequency and substrate conversion) and selectivity depend on the kind of CNGs support, catalyst preparation method and the reaction conditions (solvent nature). The Pd/CNGs catalyst can be repeatedly used while maintaining the same catalytic performance. The excellent performances of Pd/CNGs catalysts can be due to the globular morphology of the supports as well as the absence of micropores and pronounced surface defects. Graphic Abstract: [Figure not available: see fulltext.]
METHODS FOR THE TREATMENT OF OBESITY USING APREMILAST
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Paragraph 0079, (2019/05/22)
Methods of treating, managing or preventing obesity and overweight are disclosed. Specific methods encompass the administration of apremilast, alone or in combination with additional active agents or treatment regimens.
APREMILAST FOR THE TREATMENT OF A LIVER DISEASE OR A LIVER FUNCTION ABNORMALITY
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Paragraph 0098, (2019/09/15)
Methods of treating, managing or preventing liver disease are disclosed. Specific methods encompass the administration of apremilast, alone or in combination with additional active agents or treatment regimens.
NOVEL PROCESS TO PREPARE N-[2-[(1S)-1-(3-ETHOXY-4-METHOXYPHENYL)-2-(METHYLSULPHONYL) ETHYL]-1, 3-DIOXO-2,3-DIHYDRO-1H-ISOINDOL-4-YL]ACETAMIDE
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Page/Page column 11; 12, (2018/12/03)
An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.
NOVEL PROCESS FOR PREPARATION OF APREMILAST
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Page/Page column 16, (2018/02/03)
The present invention related to a novel compound of Formula II, its enantiomers or acid addition salts thereof and process for its preparation. The compound of Formula II can be used for preparation of N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2- (methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide also known as apremilast.
Preparation method for 3-aminophthalic acid and derivative thereof
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Paragraph 0019, (2017/04/11)
The invention discloses a preparation method for an apremilast intermediate, i.e., 3-aminophthalic acid, and a derivative thereof. The preparation method comprises a step of reducing 3-nitrophthalic acid or a derivative thereof in the presence of a reducing agent selected from a group consisting of elemental sulfur, sulfide and a mixture of elemental sulfur and sulfide. The method has the advantages of high yield, simple operation, environmental protection and suitability for industrial production.
