Zopolrestat
- CAS NO.:110703-94-1
- Empirical Formula: C19H12F3N3O3S
- Molecular Weight: 419.38
- MDL number: MFCD00865476
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-09 19:38:33
What is Zopolrestat?
Originator
Alond,Pfizer
The Uses of Zopolrestat
Antidiabetic; inhibitor (aldose reductase).
Manufacturing Process
A mixture of 2-methyl-5-trifluoromethylbenzothiazole (1 mole-equivalent), N- bromosuccinimide (1 mole-equivalent), carbon tetrachloride (700 ml) and a catalytic amount of benzoyl peroxide (0.2 g) was refluxed under irradiation by an UV lamp for 14 hours. The reaction mixture was cooled to room temperature, filtered to remove the precipitated succinimide and the filtrate was evaporated to dryness. The resulting solid was chromatographed over silica gel to obtain the 2-bromomethyl-5-trifluoromethyl-benzothiazole. To a mixture of ethyl 4-oxo-3H-phthalazin-1-ylacetate (1 mole-equivalent) and sodium hydride (50% w/w dispersion in mineral oil) in dimethylformamide (150 ml) was added 2-bromomethyl-5-trifluoromethylbenzothiazole (1 mole- equivalent) and the resulting mixture stirred at room temperature for 1 hour. This reaction mixture was poured over ice-water (500 ml); sufficient 10% HCl was added to adjust the pH to about 4.0 and the precipitated crude solid was collected. This was chromatographed over silica gel to obtain the ethyl[4-oxo- 3-(5-trifluoromethylbenzothiazol-2-yl)-3,4-dihydro-phthalazin-1-yl]acetate; MP: 134°-136°C. A solution of methyl or ethyl [4-oxo-3-(5-trifluoromethylbenzothiazol-2-yl)- 3,4-dihydrophthalazin-1-yl]acetate (1 mole-equivalent) in methanol (50 ml)
Therapeutic Function
Aldose reductase inhibitor
Properties of Zopolrestat
Melting point: | 197-198℃ |
Density | 1.58 |
storage temp. | 2-8°C |
solubility | DMSO: ≥20mg/mL |
form | powder |
pka | pKa (dioxane/water): 5.46 (1:1); 6.38 (2:1) |
color | off-white to light brown |
Safety information for Zopolrestat
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 |
GHS Hazard Statements |
H301:Acute toxicity,oral H413:Hazardous to the aquatic environment, long-term hazard |
Precautionary Statement Codes |
P273:Avoid release to the environment. |
Computed Descriptors for Zopolrestat
New Products
ALUMINIUM IODIDE 100 GM BUFFER CAPSULE PH 7.0 - 10 CAP BUFFER SOLUTION PH 9.5 (BORATE) EZEE BLUE GEL STAINER BORAX CARMINE (GRENACHERS ALCOHOLIC) POTASSIUM IODATE - IODIDE SOLN 0.1 N Dabigatran Acyl-O3-D-Glucuronide Trifluoroacetic Acid Salt Isofolic Acid Dabigatran 2-O-acylglucuronide metabolite Dabigatran Acyl-?-D- glucuronide Trifluroacetic Acid Erythromycin EP Impurity A Desloratidine Related Compound ARelated products of tetrahydrofuran
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