HuagongsheHuagongshe Chemistry Print Report · For research reference only
Water → 4-[(4-isopropoxyphenyl)methyl]-1-isopropyl-5-methyl-3-(6-O-propionyl-beta-D-glucopyranosyloxy)pyrazole
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Water | HCID 962 | — |
| Reactant | 2-Hydroxy-1,2,3-propanetricarboxylic acid hydrate (1:1) | HCID 22230 | — |
| Reactant | Propionyl chloride | HCID 62324 | — |
| Reactant | Remogliflozin | HCID 9846588 | — |
| Solvent | 2,4,6-Trimethylpyridine | HCID 7953 | — |
| Product | 4-[(4-isopropoxyphenyl)methyl]-1-isopropyl-5-methyl-3-(6-O-propionyl-beta-D-glucopyranosyloxy)pyrazole | HCID 67335748 | 65.8% |
Reaction Steps
To a solution of 3-(β-D-glucopyranosyloxy)-4-[(4-iso-propoxyphenyl)methyl]-1-isopropyl-5-methylpyrazole (0.10 g) in 2,4,6-trimethylpyridine (1 mL) was added propionyl chloride (0.072 g) at 0° C., and the mixture was stirred for hours. To the reaction mixture were added citric acid monohydrate (3.3 g) and water, and the resulting mixture was purified by ODS solid phase extraction (washing solvent: distilled water, eluent: methanol). Further purification by column chromatography on silica gel (eluent: dichloromethane/methanol=10/1) afforded 4-[(4-isopropoxyphenyl)methyl]-1-isopropyl-5-methyl-3-(6-O-propionyl-β-D-glucopyranosyloxy)pyrazole (0.074 g)
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07989424B2 |
| Source dataset | uspto-grants-2011_08 |
| ORD ID | ord-88d369e858614b0e9c70fbe8de34d9ba |
| Source note | uspto-grants-2011_08 |