274693-55-9Relevant articles and documents
Preparation method of key intermediate A of ticagrelor
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, (2020/05/29)
The invention discloses a preparation method of a key intermediate A of ticagrelor. The method comprises the following steps: (1) synthesis of an intermediate 9, (2) synthesis of an intermediate 10, and (3) synthesis of a key intermediate A. The synthesis of the intermediate 9 comprises the following steps: dropwise adding glacial acetic acid into a mixture of the intermediate 4, tetrahydrofuran and zinc powder at room temperature, stirring the mixture, keeping the temperature for 24 hours, neutralizing the reaction product with liquid caustic soda to neutrality, evaporating the solvent, and extracting, drying, filtering and concentrating the reaction product to obtain the intermediate 9. The invention discloses a preparation method of a key intermediate A of ticagrelor. On the basis of the existing preparation technology, through further improvement and optimization, the synthesis process is greatly shortened, the production cost is reduced, the safe and convenient preparation methodof the ticagrelor key intermediate A suitable for industrial large-scale production is provided, and the preparation method has good economic benefits and wide application prospects.
Bio-synthesis method for ticagrelor intermediate and the intermediate therefrom
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Paragraph 0032; 0043; 0044; 0045; 0052; 0057; 0062, (2018/11/04)
The invention discloses a bio-synthesis method for a ticagrelor intermediate and the intermediate therefrom. The method includes steps of: oxidizing a compound (2) to prepare a compound (3); performing an ortho-diol protection reaction to obtain a compound (4); performing an addition reaction to the compound (4) with ethylene oxide to obtain a compound (5); and performing bioconversion to the compound (5) to prepare the ticagrelor intermediate compound (1). Reaction equations in the method are represented in the specification. The synthesis method has advantages of creative technical route, simple operation, high synthesis yield and product purity, low cost and extensive source of raw materials and is suitable for industrial production. The ticagrelor intermediate can serve as an intermediate raw material for preparation of ticagrelor.
Synthesis process of ticagrelor intermediate
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, (2017/08/28)
The invention discloses a synthesis process of a ticagrelor intermediate. The synthesis process of the ticagrelor intermediate is characterized by including the steps: 1) under acidic condition, contacting benzaldoxime with cyclopentadiene for reaction so as to obtain a compound shown in formula I; 2) under the catalysis of osmium tetroxide, using hydrogen peroxide to oxidize the compound shown in the formula I so as to obtain a compound shown in formula II; 3) under the catalysis of p-toluenesulfonic acid, reacting the compound shown in the formula II and acetone to obtain a compound shown in formula III; 4) in the presence of an alkali, reacting the compound shown in the formula III with 2-bromoethyl alcohol so as to obtain a compound shown in formula IV; 5) reducing the compound shown in the formula IV so as to obtain the ticagrelor intermediate. The raw materials used here in the method provided herein are low in cost and easy to obtain, so that production cost; the use of chiral materials is not required, a high stereoselectivity product can be acquired through cycloaddition reaction, the steps are short, the reaction yield is very high, and a new approach for the synthesis of ticagrelor is provided.