72402-14-3Relevant articles and documents
MEAYAMYCIN ANALOGUES AND METHODS OF USE
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Page/Page column 5, (2021/10/15)
Compounds according to formula (I), where R is as defined herein, have anti-cancer properties.
Preparation method of ticagrelor key intermediate iodide
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Paragraph 0038-0043, (2020/05/01)
The invention discloses a preparation method of ticagrelor key intermediate iodide, which comprises the following steps of: (1) synthesis of an intermediate 1: taking D-ribose as a raw material, methanol and acetone as solvents, adding thionyl chloride as a catalyst, and concentrating to remove the solvents after the reaction is finished, so as to obtain the intermediate 1, and (3) synthesis of the key intermediate iodide: by taking acetonitrile as a solvent, adding the intermediate 1 and sodium iodide into a reaction system, dropwise adding trimethylchlorosilane, adding a small amount of water for quenching reaction after the reaction is finished, evaporating to remove acetonitrile, extracting with the solvent, and concentrating to obtain the key intermediate iodide. According to the preparation method of the ticagrelor key intermediate iodide, in the synthesis process of the intermediate 1, thionyl chloride is adopted to replace hydrochloric acid to serve as a catalyst, the reactionconversion rate is greatly increased, then trimethylchlorosilane/sodium iodide serves as an iodinating agent, the reaction condition is mild, aftertreatment is simple, and the conversion rate is high.
Industrial large-scale production method of capecitabine intermediate
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Paragraph 0041; 0042, (2020/09/20)
The invention provides an industrial large-scale production method of a capecitabine intermediate. The industrial large-scale production method adopts a one-pot production method of simultaneously adding methanol and acetone, and is a preparation method which is energy-saving, short in production period and high in yield; a method of adding low-boiling-point solvents such as ethyl acetate into dimethyl sulfoxide or pyrrolidone for reflux cooling to take away heat is adopted; and a production method of hydrolyzing while distilling is designed, the methanol and the acetone which are generated byhydrolysis are distilled out, the methanol and the acetone in water are continuously reduced, the reaction is carried out towards K3, and the reaction is complete and thorough.