864070-19-9Relevant articles and documents
Synthetic method for empagliflozin related substance IMPD
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, (2019/07/10)
The invention discloses a synthetic method for empagliflozin related substance IMPD. In a current synthetic method of IMPD, a whole synthetic route is longer and the total yield is lower. The synthetic method provided by the invention comprises the following steps: performing hydroxylation by using (2-chloro-5-iodophenyl)(4-fluorophenyl)methanone as a raw material to obtain (2-chloro-5-iodophenyl)(4-hydroxyphenyl)methanone, performing a reaction by using a carbonyl reducing agent to obtain 4-(5-iodo-2-chlorobenzyl)phenol, protecting phenolic hydroxyl groups by using protecting groups such as TBDMS, performing metallization of aromatic iodide by adopting a relatively stable and safe Grignard reagent i-PrMgCl.LiCl, performing methyl glucoside reduction by using a Lewis acid catalyst, and finally performing quenching to obtain the empagliflozin related substance IMPD. The synthetic method provided by the invention has the advantages of an abundant raw material source, a simple, quick andhigh-efficiency reaction, milder reaction conditions, a higher total yield and low costs.
PROCESS FOR PREPARATION OF DAPAGLIFLOZIN AND INTERMEDIATES THEREOF
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Page/Page column 23-24, (2018/03/06)
Processes for the preparation of dapagliflozin reduce or eliminate impurities in dapagliflozin, preferably individual impurities are not more than 0.15% by HPLC.
NOVEL SGLT INHIBITORS
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Page/Page column 56-57, (2013/02/28)
The present invention relates to novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula (I) and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).