Molecular Formula | C5H10N2O3 |
Molar Mass | 146.15 |
Density | 1.3394 (rough estimate) |
Melting Point | >25 °C |
Boling Point | 265.74°C (rough estimate) |
Solubility | Chloroform (Soluble), Dichloromethane (Slightly), Ethyl Acetate (Slightly), Meth |
Appearance | Morphological Solid |
Color | Off-White to Yellow Oil to |
pKa | 4.57±0.10(Predicted) |
Storage Condition | Hygroscopic, -20°C Freezer, Under Inert Atmosphere |
Stability | Hygroscopic |
Refractive Index | 1.4954 (estimate) |
Introduction
Losartan genotoxic impurity (NMBA) is a known carcinogenic chemical substance in animals and potential humans. It is followed by N-nitrosodimethylamine (NDMA) and N-nitrosodiethylamine (NDEA) The third genotoxic impurity detected in ARBs drugs. In the FDA's published list of nitrosamines for ARBs, the maximum daily allowable intake of NMBA is 0.96ppm.
Preparation
5.0g(0.05mol)N-methylpyrrolidone is added into a 250mL four-mouth flask, 50g toluene is added, stirring is dissolved, 0.5g tetrabutyl ammonium bromide is added, and sodium hydroxide aqueous solution (sodium hydroxide: 4g(0.1mol) is added; Water: 40g), heating to 50 ℃, stirring for 28h, stirring for reaction, separating, organic discarding, adjusting pH = 1.0 with hydrochloric acid, filtering, filtrate collection, the filter cake is discarded.