2148-56-3Relevant articles and documents
Synthetic method for Laquinimod intermediate 2-amino-6-chlorobenzoic acid
-
, (2019/10/01)
The invention discloses a synthetic method for a Laquinimod intermediate 2-amino-6-chlorobenzoic acid. The synthetic method is characterized in that the 2-amino-6-chlorobenzoic acid can be obtained through the reaction of 3-chloro-2-methylaniline under the action of a protective agent and an oxidizing agent; and a reaction process includes the following steps: 1) uniformly mixing the 3-chloro-2-methylaniline, the protective agent and a solvent S1, performing stirring reaction for 1-2 h under 40-50 DEG C, and obtaining a mixture I at the end; 2) uniformly mixing the oxidizing agent, water and asolvent S2, introducing a protection gas, controlling a reaction temperature to be 145-155 DEG C and reaction pressure to be 5-7 atmospheric pressure so that a mixture II can be obtained, dropping the mixture I into the mixture II, controlling dropping time to be 50-70 min, then controlling the temperature to be 160-175 DEG C and the reaction pressure to be 8-10 atmospheric pressure, performing continuous reaction for 6-8 h, and obtaining a mixture III after cooling; 3) adding hydrochloric acid and a solvent S3 into the mixture III, controlling the reaction temperature to be 75-90 DEG C and the reaction pressure to be normal pressure, performing reaction for 0.5-1 h, and obtaining a mixture IV after cooling; and 4) adding a solvent S4 into the mixture IV, performing standing and layering,and concentrating, steaming and removing the solvents to obtain a product after an organic phase is washed by water and dried by a drying agent. The method is low in raw material cost and high in yield.
Dihydropteridin-one derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and pharmaceutical composition for use in preventing or treating PI3 kinase related diseases
-
Paragraph 0175-0178, (2017/09/12)
The present invention relates to dihydropteridin-one derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an effective component for preventing or treating PI3 kinase-related diseases. According to the present invention, the dihydropteridin-one derivatives have excellent selective inhibitory effects on PI3 kinase, and thus may be beneficially used in preventing or treating PI3 kinase-related diseases such as the following: cancers including blood cancer, ovarian cancer, cervical cancer, breast cancer, large intestine cancer, liver cancer, stomach cancer, pancreatic cancer, colon cancer, periotoneal cancer, skin cancer, bladder cancer, prostate cancer, lung cancer, osteosarcoma, fibrous tumor, and brain tumor; autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, type 1 diabetes, hyperthyroidism, myasthenia gravis, Crohnandprime;s disease, ankylosing spondylitis, psoriasis, pernicious anemia, and Sjogrenandprime;s syndrome; and respiratory diseases including chronic obstructive pulmonary disease (COPD), rhinitis, asthma, chronic bronchitis, chronic pulmonary inflammatory diseases, silicosis, pulmonary sarcoidosis, pleuritis, alveolitis, vasculitis, emphysema, pneumonia, and bronchiectasis.COPYRIGHT KIPO 2017
A High-Throughput Assay for Arylamine Halogenation Based on a Peroxidase-Mediated Quinone-Amine Coupling with Applications in the Screening of Enzymatic Halogenations
Hosford, Joseph,Shepherd, Sarah A.,Micklefield, Jason,Wong, Lu Shin
supporting information, p. 16759 - 16763 (2016/02/12)
Arylhalides are important building blocks in many fine chemicals, pharmaceuticals and agrochemicals, and there has been increasing interest in the development of more "green" halogenation methods based on enzyme catalysis. However, the screening and development of new enzymes for biohalogenation has been hampered by a lack of high-throughput screening methods. Described herein is the development of a colorimetric assay for detecting both chemical and enzymatic arylamine halogenation reactions in an aqueous environment. The assay is based on the unique UV/Vis spectrum created by the formation of an ortho-benzoquinone-amine adduct, which is produced by the peroxidase-catalysed benzoquinone generation, followed by Michael addition of either a halogenated or non-halogenated arylamine. This assay is sensitive, rapid and amenable to high-throughput screening platforms. We have also shown this assay to be easily coupled to a flavin-dependent halogenase, which currently lacks any convenient colorimetric assay, in a "one-pot" workflow.
