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Appearance:White or off white crystalline powder
Purity:99%
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144701-48-4 Name |
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Name |
Telmisartan |
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Synonym |
4'-[{1,4'-Dimethyl-2'-Propyl[2,6'-Bi-1H-Benzimiaszol]-1'yl}-Methyl}-1,1'-Biphenyl-2-Caroxylic Acid Dimethyl Ethyl Ester;4'-[{1,4'-Dimethyl-2'-Propyl[2,6'-Bi-1H-Benzimiaszol]-1'yl}-Methyl}-1,1'-Biphenyl-2-Caroxylic Acid;4''-(1,7''-DIMETHYL-2''-PROPYL-1H-[2,5'']BIBENZOIMIDAZOLYL-3''-YLMETHYL)-BIPHENYL-2-CARBOXYLIC ACID;4-chloromethyl-5-methyl-1,3-dioxol-2-tone;4'-(1,7'-Dimethyl-2'-propyl-1H-;BIBR 277, 4μ[(1,4μ-Dimethyl-2μ-propyl[2,6μ-bi-1H-benzimidazol]-1μ-yl)methyl][1,1μ-biphenyl]-2-carboxylic acid;4'-[[4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl]methyl]-2-biphenylcarboxylic acid;Telmisartan,4′[(1,4′-Dimethyl-2′-propyl[2,6′-bi-1H-benzimidazol]-1′-yl)methyl][1,1′-biphenyl]-2-carboxylic acid, BIBR 277 |
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144701-48-4 Biological Activity |
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Related Catalog |
Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor Signaling Pathways >> Autophagy >> Autophagy Research Areas >> Cardiovascular Disease |
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Target |
IC50: 9.2 nM (angiotensin II type 1 receptor)[1] |
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144701-48-4 Chemical & Physical Properties |
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Melting point |
261-263°C |
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Boiling point |
771.9±70.0 °C at 760 mmHg |
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Density |
1.2±0.1 g/cm3 |
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Molecular Formula |
C33H30N4O2 |
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Molecular Weight |
514.617 |
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Flash Point |
420.6±35.7 °C |
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PSA |
72.94000 |
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LogP |
7.73 |
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Exact Mass |
514.236877 |
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Vapour Pressure |
0.0±2.8 mmHg at 25°C |
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Index of Refraction |
1.667 |
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Storage condition |
Hygroscopic, -20°C Freezer, Under Inert Atmosphere |
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Water Solubility |
insoluble |
White or off-white crystalline powder, odorless and tasteless. Telmisartan , a highly selective angiotensin II (AII) type 1 (AT1) receptor antagonist, is approved for the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents. Also used in the treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes mellitus, as well as the treatment of congestive heart.
Definition
ChEBI: A member of the class of benzimidazoles used widely in the treatment of hypertension.
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
Telmisartan (TEL) and Nebivolol (NEB) are frequently co-formulated in a single dosage form that is frequently prescribed for the treatment of hypertension, moreover, telmisartan is currently proposed to be used to treat COVID19-induced lung inflammation. The high sensitivity and selectivity of the method expanded its applications for the simultaneous determination of NEB and TEL in spiked human plasma without interference from endogenous components. The validated method is rapid and highly sensitive, thus can be used as an effective tool to monitor the therapeutic levels of the two drugs for in-patients.
The solid dispersions comprising telmisartan and a manufacturing method thereof, according to the present invention, unlike conventional methods requiring a low yield, can manufacture telmisartan of a high yield through simple and short steps by using a relatively inexpensive raw material, can secure excellent quality through reduction of generation of decomposition products, and can manufacture the solid dispersions on a mass production basis to be commercially available.
![tert-butyl 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylate](/upload/2023/1/f6259ea0-3fe8-4014-b7b9-edcc34bb34c2.png)
tert-butyl 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylate
telmisatran
| Conditions | Yield |
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With sodium hydroxide; In tetrahydrofuran; at 100 ℃; Reagent/catalyst; Solvent;
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93% |
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With trifluoroacetic acid; In N,N-dimethyl-formamide; for 4h;
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70% |
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With trifluoroacetic acid; In N-methyl-acetamide;
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63.9% |
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With trifluoroacetic acid; In dichloromethane; for 24h; Yield given; Ambient temperature;
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![tert-butyl-4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylate hydrochloride](/upload/2023/1/a62e5516-8e8a-4729-bcf0-643bdd97e66f.png)
tert-butyl-4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylate hydrochloride
telmisatran
| Conditions | Yield |
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tert-butyl-4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylate hydrochloride; With acetic acid; In water; Heating / reflux;
With sodium hydroxide; In water; at 80 - 90 ℃;
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93.3% |
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With sodium hydroxide; water; In water; acetic acid; at 80 - 90 ℃; Heating / reflux;
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93.3% |
tert-butyl 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylate
4'-[[2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)-1H-benzimidazol-1-yl]-methyl]-2-cyano-biphenyl
methyl 4-amino-3-methylbenzoate
N-methylbenzene-1,2-diamine dihydrochloride
telmisartan tert-butylamine salt
telmisartan choline salt
4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylic acid ammonium salt
telmisartan meglumine salt
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