274693-55-9Relevant articles and documents
Preparation method of key intermediate A of ticagrelor
-
Paragraph 0049-0054, (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
-
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.
Preparation method for ticagrelor intermediate
-
, (2017/08/28)
The invention discloses a preparation method for a ticagrelor intermediate. The preparation method comprises the following steps: 1) subjecting o-substituted benzaldoxime and cyclopentadiene to a contact reaction so as to obtain a compound as shown in a formula I; 2) oxidizing the compound as shown in the formula I with hydrogen peroxide under the catalysis of osmium tetroxide so as to obtain a compound as shown in a formula II; 3) reacting the compound as shown in the formula II with acetone under the catalysis of p-toluenesulfonic acid so as to obtain a compound as shown in a formula III; 4) reacting the compound as shown in the formula III with 2-bromoethanol in the presence of alkali so as to obtain a compound as shown in a formula IV; and 5) reducing the compound as shown in the formula IV so as to obtain the ticagrelor intermediate. The method provided by the invention uses cheap and easily available raw material, reduces production cost, and does not need any chiral raw material; a cycloaddition reaction enables a highly stereoselective product to be obtained; and the method is short in steps and high in reaction yield and provides a novel approach for synthesis of ticagrelor.