1210344-57-2Relevant articles and documents
AN EFFICIENT PROCESS FOR THE PREPARATION OF ERTUGLIFLOZIN L-PYROGLUTAMIC ACID AND INTERMEDIATES THEREOF
-
Page/Page column 5; 16; 19; 20, (2021/07/10)
The present invention relates to an efficient process for the preparation of Ertugliflozin L-pyroglutamic acid of formula (I) and intermediate thereof, in environment friendly conditions. The present invention further relates to a process for the preparation of substantially pure intermediate of formula (IV).
A NOVEL PROCESS FOR THE PREPARATION OF SGLT-2 INHIBITORS
-
, (2020/01/24)
The present invention relates to a novel process for the preparation of SGLT-2 inhibitors via addition of a hydroxymethylene group in an open chain intermediate, readily accessible from D-glucose.
Studies towards the synthesis of ertugliflozin from L-Arabinose
Triantakonstanti, Virginia V.,Mountanea, Olga G.,Papoulidou, Kyriaki-Eleni C.,Andreou, Thanos,Koftis, Theocharis V.,Gallos, John K.
, p. 5700 - 5708 (2018/08/20)
A new method for the diastereoselective synthesis of enantiomerically pure ertugliflozin was developed. The crucial step involves an aldol condensation between 1-(4-chloro-3-(4-ethoxybenzyl)phenyl)ethanone and (4R,5R)-5-(((tert-butyldimethylsilyl)oxy)methyl)-2,2-dimethyl-5-((trityloxy)methyl)-1,3-dioxolane-4-carbaldehyde, which was prepared from known 2-C-trityloxymethyl-2,3-O-isopropylidene-L-erythrose (easily accessible in three steps from L-arabinose) by standard reduction/oxidation and protection/deprotection manipulations. Dihydroxylation of the aldol condensation product and further global deprotection led to the formation of the target molecule.