394-18-3Relevant articles and documents
Synthesis method of osimertinib intermediate
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Paragraph 0045-0047; 0050-0052; 0055-0057; 0060-0062; 0065, (2021/02/10)
The invention relates to a synthesis method of an osimertinib intermediate. The synthesis method comprises the following steps: 1, with 3-fluoroanisole as an initial raw material, adding 3-fluoroanisole into concentrated sulfuric acid, dropwise adding the concentrated nitric acid in a low-temperature environment, carrying out primary heating and stirring after completion of the addition, injectingthe formed system into ice water for quenching, carrying out secondary heating and stirring, and carrying out filtering to obtain a product, namely 3-fluoro-4, 6-dinitroanisole; and 2, adding the compound 3-fluoro-4,6-dinitroanisole obtained in the step 1 into water, adding alkali, conducting heating, adding a weak reducing agent in batches, performing stirring while keeping the temperature untila reaction endpoint is reached, carrying out filtering to obtain a crude product, and successively conducting washing, recrystallizing with methanol, crystallizing and filtering at a low temperatureand drying to finally obtain 4-fluoro-2-methoxy-5-nitroaniline. The method of the invention solves the problems that raw materials are expensive and hardly-available in the market, process is complexand yield is low in conventional synthesis methods of the osimertinib intermediate.
Benzimidazole-based compounds kill Mycobacterium tuberculosis
Gong, Yaling,Somersan Karakaya, Selin,Guo, Xiaoyong,Zheng, Purong,Gold, Ben,Ma, Yao,Little, David,Roberts, Julia,Warrier, Thulasi,Jiang, Xiuju,Pingle, Maneesh,Nathan, Carl F.,Liu, Gang
, p. 336 - 353 (2014/03/21)
Tuberculosis remains one of the deadliest infectious diseases, killing 1.4 million people annually and showing a rapid increase in cases resistant to multiple drugs. New antibiotics against tuberculosis are urgently needed. Here we describe the design, sy
