Name | Telmisartan |
Synonyms | Telmisartan 4'-(1,7'-Dimethyl-2'-propyl-1H- 4-chloromethyl-5-methyl-1,3-dioxol-2-tone 4'-[(1,7'-dimethyl-2'-propyl-1H,3'H-2,5'-bibenzimidazol-3'-yl)methyl]biphenyl-2-carboxylic acid 4'-[{1,4'-Dimethyl-2'-Propyl[2,6'-Bi-1H-Benzimiaszol]-1'yl}-Methyl}-1,1'-Biphenyl-2-Caroxylic Acid 4'[(1,4'-Dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl][1,1'-biphenyl]-2-carboxylic acid 4''-(1,7''-DIMETHYL-2''-PROPYL-1H-[2,5'']BIBENZOIMIDAZOLYL-3''-YLMETHYL)-BIPHENYL-2-CARBOXYLIC ACID [1,1'-Biphenyl]-2-carboxylicacid,4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl] 2-[4-[[4-methyl-6-(1-methylbenzoimidazol-2-yl)-2-propyl-benzoimidazol-1-yl]methyl]phenyl]benzoic acid tert-butyl 4'-[(1,7'-dimethyl-2'-propyl-1H,3'H-2,5'-bibenzimidazol-3'-yl)methyl]biphenyl-2-carboxylate 4'-[[4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl]methyl]-2-biphenylcarboxylic acid BIBR 277, 4μ[(1,4μ-Dimethyl-2μ-propyl[2,6μ-bi-1H-benzimidazol]-1μ-yl)methyl][1,1μ-biphenyl]-2-carboxylic acid 4'-[{1,4'-Dimethyl-2'-Propyl[2,6'-Bi-1H-Benzimiaszol]-1'yl}-Methyl}-1,1'-Biphenyl-2-Caroxylic Acid Dimethyl Ethyl Ester Telmisartan,4′[(1,4′-Dimethyl-2′-propyl[2,6′-bi-1H-benzimidazol]-1′-yl)methyl][1,1′-biphenyl]-2-carboxylic acid, BIBR 277 |
CAS | 144701-48-4 |
EINECS | 620-494-7 |
InChI | InChI=1/C33H30N4O2/c1-7-12-33-39-34-24(2)21-27(35-38-30-15-10-11-16-31(30)40(35)6)22-32(34)41(33)23-25-17-19-26(20-18-25)28-13-8-9-14-29(28)36(42)43-37(3,4)5/h8-11,13-22H,7,12,23H2,1-6H3 |
InChIKey | RMMXLENWKUUMAY-UHFFFAOYSA-N |
Molecular Formula | C33H30N4O2 |
Molar Mass | 514.62 |
Density | 1.16 |
Melting Point | 261-263°C |
Boling Point | 771.9±70.0 °C(Predicted) |
Flash Point | 425.798°C |
Water Solubility | insoluble |
Solubility | Soluble in DMSO (13 mg/ml at 25 °C), chloroform, DMF (~1.6 mg/ml), and ethanol (<1 mg |
Vapor Presure | 0mmHg at 25°C |
Appearance | White or off-white crystalline powder |
Color | white |
Merck | 14,9129 |
pKa | 3.86±0.36(Predicted) |
Storage Condition | 2-8°C |
Stability | Hygroscopic |
Refractive Index | 1.624 |
MDL | MFCD00918125 |
Physical and Chemical Properties | White crystalline powder. |
Use | Antihypertensive agents, vasodilator antagonists |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 2 |
RTECS | DV2037500 |
HS Code | 2933995300 |
Reference Show more | 1. [IF=3.365] Cailian Fei et al."LC-MS/MS method for quantifying aescinate A and B and assessing their relationship with phlebitis."Anal Biochem. 2022 Mar;:114636 |
white or off-white crystalline powder, tasteless. Melting point 2 61-263 °c. It is almost insoluble at pH = 3 to 9. Insoluble in strong acid (but soluble in hydrochloric acid). Soluble in strong alkali solution.
2-n-propyl-4-methylbenzoxazole-6-carboxylic acid and N-methylo-phenylenediamine are reacted in paraformaldehyde at 150 °c, the cyclization forms 2-n-propyl -4-methyl -6-(1-methylbenzimidazol-2-yl) benzimidazole. This is followed by alkylation with tert-butyl 2-(4-bromomethylphenyl) benzoate in dimethyl sulfoxide in the presence of potassium tert-butoxide. The resulting product was hydrolyzed in dimethylformamide with trifluoroacetic acid to give telmisartan.
The original research of German Boehringer Ingelheim pharmaceutical company was granted a German patent in 1991. It was first approved to be listed in the United States in November 1998, and then listed in Germany, the Philippines, Australia, Belgium, the United Kingdom and other countries. Non-peptide angiotensin II receptor antagonists selectively block AT1 receptors, which are difficult to reverse, but have no effect on other receptor systems. For mild to moderate hypertension.