Name | Mizolastine |
Synonyms | Mizolastine MIZOLASTINE Mizolastine HCl iperidinyl)methylamino)- 4(1h)-pyrimidinone,2-((1-(1-((4-fluorophenyl)methyl)-1h-benzimidazol-2-yl)-4-p 2-[[1-[1-(4-fluorobenzyl)benzimidazol-2-yl]-4-piperidyl]-methyl-amino]-1H-pyrimidin-6-one 2-[{1-[1-(4-fluorobenzyl)-1H-benzimidazol-2-yl]piperidin-4-yl}(methyl)amino]pyrimidin-4(3H)-one 2-[[1-[1-[(4-fluorophenyl)methyl]benzoimidazol-2-yl]-4-piperidyl]-methyl-amino]-3h-pyrimidin-4-one 2-[[1-[1-[(4-fluorophenyl)methyl]benzimidazol-2-yl]piperidin-4-yl]-methyl-amino]-1H-pyrimidin-6-one 2-[[1-[1-[(4-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-4-piperidinyl]methylamino]-4(1H)-pyrimidinone |
CAS | 108612-45-9 |
EINECS | 1308068-626-2 |
InChI | InChI=1/C24H25FN6O/c1-29(23-26-13-10-22(32)28-23)19-11-14-30(15-12-19)24-27-20-4-2-3-5-21(20)31(24)16-17-6-8-18(25)9-7-17/h2-10,13,19H,11-12,14-16H2,1H3,(H,26,28,32) |
Molecular Formula | C24H25FN6O |
Molar Mass | 432.49 |
Density | 1.34±0.1 g/cm3(Predicted) |
Melting Point | 217° |
Solubility | Chloroform (Slightly, Heated), DMSO, Methanol (Slightly, Heated) |
Appearance | Solid |
Color | White |
Merck | 14,6221 |
pKa | 9.73±0.40(Predicted) |
Storage Condition | Refrigerator |
Refractive Index | 1.682 |
Physical and Chemical Properties | Treatment of chronic allergic rhinitis |
RTECS | UW7481284 |
White. Crystallization from ethanol, melting point 217 °c.
4-piperidinylcarbamate hydrochloride was dissolved in methanol, neutralized with sodium methoxide, filtered, and the filtrate was concentrated to dryness. The resulting material was reacted with 2 monochloro -1-[(4-fluorophenyl) methyl]-1H-benzimidazole cothermically at 140 °c. Add dichloromethane, alkalization with sodium hydroxide, organic layer after treatment to get [1-[1-[(4 fluorophenyl)) methyl]-1H-benzimidazol-2-yl]-4-piperidinyl] carbamic acid ethyl ester. The compound was dissolved in dimethylformamide and a solution of sodium hydride in dimethylformamide was added dropwise. Stir at room temperature, then add methyl iodide dimethylformamide solution, after the reaction is finished, processing to get [1-[1-[(4 fluorophenyl)) methyl -1H-benzimidazol-2-yl]-4-piperidinyl] -N-methyl ethyl carbamate. The compound is dissolved in acetic acid and hydrobromic acid, reflux, processing to obtain 1-[1] [4 fluorophenyl) methyl] -1H-benzimidazol-2-yl]-n-methyl-4-piperidinamide monohydrate. The compound was reacted with methyl thiourea to obtain mizolastine.
developed by the French company Sanofi-St. durburg France, was first launched in 1998 in Germany. It was listed in China in 2001. Anti-allergic. Second-generation non-sedating antihistamines, long-acting histamine Hi receptor antagonists. For acute and chronic, seasonal and perennial allergic rhinitis, urticaria and other skin allergies.