63069-50-1Relevant articles and documents
Synthesis method of tedizolid phosphate intermediate 3-fluoro-4-bromoaniline
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Paragraph 0051-0053; 0062-0065; 0076-0079; 0086-0089, (2020/12/09)
The invention provides a synthesis method of a tedizolid phosphate intermediate 3-fluoro-4-bromoaniline. The synthesis method comprises the following steps: (1) performing reacting of a compound 1 with ammonia gas to obtain a compound 2; (2) performing reacting of the compound 2 with hydrobromic acid to obtain a compound 3; and (3) reducing a cyano group in the compound 3 into an amino group to obtain a compound 4. The raw material adopted by the method is cheap and easy to obtain, and the method is mild in reaction condition, simple in equipment requirement, high in safety index and suitablefor large-scale commercial production. The yield of the tedizolid phosphate intermediate 3-fluoro-4-bromoaniline prepared by the process provided by the invention is up to 56.61% or above, the purityis up to 99.70% or above, and the content of isomer impurities in the product is as low as 0.17% or below. The invention provides the cheap and easily available high-quality intermediate for commercial production of tedizolid phosphate bulk drugs, and a wide application prospect is achieved.
NOVEL GPR119 AGONIST COMPOUNDS
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Paragraph 0533-0535, (2017/10/26)
The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.
Ethyl cyanoacetate: A new cyanating agent for the palladium-catalyzed cyanation of aryl halides
Zheng, Shuyan,Yu, Chunhui,Shen, Zhengwu
supporting information; experimental part, p. 3644 - 3647 (2012/08/28)
A new Pd-catalyzed cyanation reaction has been discovered using ethyl cyanoacetate as the cyanating reagent. A variety of electron-rich and electron-deficient aryl halides were efficiently converted into their corresponding nitriles in good to excellent yields.
