1030825-21-8Relevant articles and documents
Preparation method of canagliflozin
-
Paragraph 0018; 0035-0041, (2020/02/14)
The invention discloses a preparation method of canagliflozin. According to the method, the reaction of each step in a route is improved, so that the conversion rate of raw materials is increased, andintroduction of potential toxic compounds is avoided. In addition, reaction conditions are mild; operation is simple; purity of an obtained product is high; quality of drugs is improved; and the preparation method is suitable for industrial production.
Method for preparing Canagliflozin intermediate
-
Paragraph 0062-0079, (2019/04/26)
The invention relates to a method for preparing a Canagliflozin intermediate. The preparation method comprises the following steps: 1) in an inert environment, at a temperature of -30 DEG C to -15 DEGC, a thiophene compound and an alkaline reagent and 2, 3, 4, 6-tetra-O-(trimethylsilane)-D-Gluconolactone are fully reacted; and 2) a methanol solution containing strong acid is added dropwise to thereaction liquid obtained in the step 1), and after full reacting, quenching and purifying are carried out to obtain the Canagliflozin intermediate. The product of the preparation method has good yield and high purity; the method has low temperature requirement for equipment, safer operation and small equipment volume requirement, and the method is more suitable for industrial scale production.
Card geleg net intermediate and its amorphous preparation method
-
Paragraph 00035-0036; 0038-0039; 0041-0045; 0048-0052, (2018/02/04)
The invention provides an Invokana intermediate and a preparation method thereof in an amorphous form. The preparation method comprises the following steps: heating and clearly dissolving (1S)-1,5-dehydro-1-[3-[[5-(4-fluorophenyl)-2-thienyl] methyl]-4- methylphenyl-D-glucitol in a benign solvent, then dropwise adding into a rapidly-stirred poor solvent, filtering a precipitated solid and obtaining the amorphous Invokana intermediate. According to the preparation method provided by the invention, the solvent dosage can be reduced, and an obtained product is easily separated; moreover, the obtained product has good yield and high purity, and the operation is simple.