108440-70-6Relevant articles and documents
Synthesis and Optimization of Canagliflozin by Employing Quality by Design (QbD) Principles
Metil, Dattatray S.,Sonawane, Swapnil P.,Pachore, Sharad S.,Mohammad, Aaseef,Dahanukar, Vilas H.,McCormack, Peter J.,Reddy, Ch. Venkatramana,Bandichhor, Rakeshwar
, p. 27 - 39 (2018)
Efforts toward a synthesis and process optimization of canagliflozin 1 are described. Canagliflozin synthesis was accomplished via purified open ring intermediate 12. The process was optimized by employing quality by design (QbD) methodologies, and a telescopic strategy was executed for the first three and last two steps in a total six-step sequence. Optimization of the Friedel-Craft acylation reaction followed by Lewis acid mediated reductive elimination, n-BuLi mediated C-arylation, and reductive demethoxylation was performed to develop a robust process. These steps were found to be critical; therefore, critical process parameters (CPPs) were identified by employing design of experiment (DoE) methodology. In addition, control strategies for dealing with impurities are described.
Glucopyranosyl derivative and application thereof
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Paragraph 0260; 0287-0289, (2021/01/24)
The present invention relates to glucopyranosyl derivative and uses thereof. Specifically, the invention relates to a glucopyranosyl derivative used as a sodium-dependent glucose transporter 1(SGLT1)inhibitor and a pharmaceutically acceptable salt or stereoisomer thereof, and further relates to a pharmaceutical composition containing the derivative. The invention also relates to application of thecompound and the pharmaceutical composition thereof in preparation of drugs for treating diabetes and diabetes-related diseases.
GLUCOPYRANOSYL DERIVATIVE AND USE THEREOF
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Paragraph 0242; 0255-0256, (2020/12/16)
The present invention relates to a glucopyranosyl derivative and a use thereof. In particular, the present invention relates to a glucopyranosyl derivative that is used as an inhibitor of sodium-dependent glucose transporters (SGLTs), particularly being used as an inhibitor of sodium-dependent glucose transporter-1 (SGLT1), and a pharmaceutically acceptable salt or stereoisomer thereof, further relating to a pharmaceutical composition containing the derivative. The present invention further relates to a use of the compound and a pharmaceutical composition thereof in the preparation of a drug for treating diabetes and diabetes-related diseases.