1401335-14-5Relevant articles and documents
AN IMPROVED PROCESS FOR THE PREPARATION REMOGLIFLOZIN ETABONATE OR PHARMACEUTICALLY ACCEPTABLE SALT, SOLVATE, HYDRATE THEREOF
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, (2019/10/29)
The present invention relates to an improved process for the preparation of Remogliflozin, Remogliflozin etabonate or pharmaceutically acceptable salt, solvate, hydrate thereof. The present invention relates to an improved process for preparation of Remog
An efficient and practical synthesis of remogliflozin etabonate, a potent inhibitor of low-affinity Na+-dependent glucose co-transporter (SGLT2)
Kobayashi, Masahiro,Ainai, Takayuki
, p. 733 - 747 (2018/04/26)
A practical process for the preparation of remogliflozin etabonate, a prodrug of the selective low-affinity Na+-dependent glucose co-transporter (SGLT2) inhibitor, remogliflozin, is described. We established a chemoselective synthetic route to 1,2-dihydro-4-[(4-isopropoxyphenyl)methyl]-1-isopropyl-5-methyl-3H-pyrazol-3-one and an efficient O-glycosylation of this compound with 2,3,4,6-tetra-O-pivaloyl-α-D-glucopyranosyl bromide. This synthetic process provided remogliflozin etabonate in a 39% overall yield from commercially available 4-isopropoxybenzaldehyde.
O-glycosylation of 4-(substituted benzyl)-1,2-dihydro-3H-pyrazol-3-one derivatives with 2,3,4,6-tetra-O-acyl-α-D-glucopyranosyl bromide via N1-acetylation of the pyrazole ring
Kobayashi, Masahiro,Isawa, Hidetoshi,Sonehara, Junichi,Kubota, Minoru,Ozawa, Tetsuji
, p. 1009 - 1018 (2016/07/19)
A practical preparation of 4-(substituted benzyl)-3-(2,3,4,6-tetra-O-acyl-β-D-glucopyranosyloxy)-1H-pyrazole derivative 2 is described. O-Glycosylation of 4-(substituted benzyl)-1,2-dihydro-3H-pyrazol-3-one derivative 3 was facilitated by introduction of