- An efficient and practical synthesis of remogliflozin etabonate, a potent inhibitor of low-affinity Na+-dependent glucose co-transporter (SGLT2)
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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.
- Kobayashi, Masahiro,Ainai, Takayuki
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- AN IMPROVED PROCESS FOR THE PREPARATION REMOGLIFLOZIN ETABONATE OR PHARMACEUTICALLY ACCEPTABLE SALT, SOLVATE, HYDRATE THEREOF
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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
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- Method of manufacturing benzylsuccinic Pyrazolecarboxylic deriv. and its intermediate
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A production intermediate of a glucopyranosyloxypyrazole derivative which is represented by general formula (E) (wherein R3 and R4 are as defined below) and is useful as a therapeutic agent for diabetes or the like, and a method for producing a benzylpyrazole derivative, said method being indistrially more advantageous than conventional methods for producing a benzylpyrazole derivative, can be provided by causing a reaction of a compound represented by general formula (D) (wherein each of R1 and R2 represents a C1-6 alkyl group or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkoxy group or the like).
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- CHEMICAL PROCESS
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Disclosed herein are processes for preparing glucopyranosyloxypyrazole derivatives and pyrazole intermediates of the same. In particular, the present invention relates to glucopyranosyloxypyrazole derivatives having SGLT2 inhibitory activity and processes
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(2010/07/10)
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