- Preparation method of Canagliflozin intermediate
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The invention provides a preparation method of a Canagliflozin intermediate. According to the method, a stable reagent is added to an organic solvent mixing system containing 2-(5-BroMo-2-Methylbenzyl)-5-(4-fluorophenyl)thiophene(compound III) and n-Butyllithium, so that the phenomenon that when the n-Butyllithium is used, reaction products are complex, and more by-products exist, can be improved.The method is stable and high in repetition rate, the purity of the obtained intermediate is as high as 94.7%, the continuous reaction yield can achieve 93.8%, and the preparation method has industrial application prospects.
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Paragraph 0115-0122; 0143-0144
(2019/11/13)
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- Method for continuously preparing canagliflozin by using microreactor one-pot method
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The invention discloses a method for continuously preparing canagliflozin by using a microreactor one-pot method. The method is used for continuously preparing the canagliflozin by using the microreactor one-pot method, and microreactors are divided into a unit A, a unit B, a unit C and a unit D. The method comprises the steps of mixing a solution of M1 with n-butyl lithium in the unit A for carrying out a reaction; after the reaction is finished, enabling the reaction product to enter the unit B together with a solution of M3, and carrying out a reaction at the temperature of -15 to -5 DEG C to obtain an intermediate A; enabling reaction liquid containing the intermediate A to enter the unit C together with a methanol solution of methane sulfonic acid, and carrying out a reaction to obtain an intermediate B; enabling reaction liquid containing the intermediate B to directly react with boron trifluoride and triethyl silicane in the unit D to obtain the canagliflozin. The method greatly simplifies the operation steps, shortens the reaction time, greatly reduces the use of various solvents, lowers the production cost, improves the production safety, can realize continuous and automatic production, and is high in product purity and yield, thus being suitable for industrial production.
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Paragraph 0025; 0052; 0053
(2017/07/19)
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- PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT
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The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
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Page/Page column 78-79
(2009/04/25)
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