CAS No.144701-48-4,Telmisartan Suppliers

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Basic Information

Molecular Structure:
CAS No.:	144701-48-4
Name:	Telmisartan
Article Data:	56

Formula:	C₃₃H₃₀N₄O₂
Molecular Weight:	514.627
Synonyms:	(1,1-Biphenyl)-2-carboxylic acid, 4-((1,4-dimethyl-2-propyl(2,6-bi-1H-benzimidazol)-1-yl)methyl)-;Micardis;4-((4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic acid;Timetazidine;4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]- [1,1'-biphenyl]-2-carboxylic acid;
EINECS:	620-494-7
Density:	1.24 g/cm³
Melting Point:	261-263 °C
Boiling Point:	771.9 °C at 760 mmHg
Flash Point:	420.6 °C
Solubility:	insoluble in water
Appearance:	White or off white crystalline powder
Hazard Symbols:	Xi
Risk Codes:	36/37/38
Safety:	22-24/25-36-26
PSA:	72.94000
LogP:	7.26440

Synthetic route

: 144702-27-2
4'-[[2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)-1H-benzimidazol-1-yl]-methyl]-2-cyano-biphenyl

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
Stage #1: 4'-[[2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)-1H-benzimidazol-1-yl]-methyl]-2-cyano-biphenyl With sodium hydroxide; water In ethylene glycol for 8h; Heating / reflux; Stage #2: With acetic acid In water; ethylene glycol at 20℃; pH=4; Product distribution / selectivity;	98%
Stage #1: 4'-[[2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)-1H-benzimidazol-1-yl]-methyl]-2-cyano-biphenyl With potassium hydroxide; water In ethylene glycol at 140 - 150℃; for 21h; Stage #2: With hydrogenchloride In water; ethylene glycol at 20℃; pH=7; Product distribution / selectivity;	98%
Stage #1: 4'-[[2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)-1H-benzimidazol-1-yl]-methyl]-2-cyano-biphenyl With water; potassium hydroxide In ethylene glycol at 150 - 155℃; Stage #2: With water; acetic acid for 2h; pH=4 - 4.5; Product distribution / selectivity;	98.7%

: 528560-93-2
4'-[[4-methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-propyl-1H-benzimidazol-1-yl]methyl]biphenyl-2-carboxylic acid methyl ester

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
Stage #1: 4'-[[4-methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-propyl-1H-benzimidazol-1-yl]methyl]biphenyl-2-carboxylic acid methyl ester With methanol; sodium hydroxide; water for 2h; Heating / reflux; Stage #2: With acetic acid In water	98.6%
Stage #1: 4'-[[4-methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-propyl-1H-benzimidazol-1-yl]methyl]biphenyl-2-carboxylic acid methyl ester With methanol; potassium hydroxide for 24h; Reflux; Stage #2: With formic acid Product distribution / selectivity;	96%
Stage #1: 4'-[[4-methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-propyl-1H-benzimidazol-1-yl]methyl]biphenyl-2-carboxylic acid methyl ester With sodium hydroxide In methanol; water for 3h; Reflux; Stage #2: With acetic acid In methanol; water pH=5;	95%

: 152628-02-9
2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazole

: 150766-86-2
4'-bromomethylbiphenyl-2-carboxylic acid

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
Stage #1: 2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazole With sodium hydride In N,N-dimethyl-formamide at 0 - 5℃; for 1h; Stage #2: 4'-bromomethylbiphenyl-2-carboxylic acid In N,N-dimethyl-formamide at 10℃; Solvent; Reagent/catalyst; Temperature;	95%

: 515815-48-2
tert-butyl-4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylate hydrochloride

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
Stage #1: 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; Stage #2: With sodium hydroxide In water at 80 - 90℃;	93.3%
With sodium hydroxide; water In water; acetic acid at 80 - 90℃; Heating / reflux;	93.3%

: 144702-26-1
tert-butyl 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylate

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
With sodium hydroxide In tetrahydrofuran at 100℃; Reagent/catalyst; Solvent;	93%
With trifluoroacetic acid In N,N-dimethyl-formamide for 4h;	70%
With trifluoroacetic acid In N-methyl-acetamide	63.9%
With trifluoroacetic acid In dichloromethane for 24h; Ambient temperature; Yield given;

: 960356-44-9
4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylic acid ammonium salt

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
Stage #1: 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylic acid ammonium salt With pyrographite In methanol at 25℃; for 0.5h; Stage #2: With acetic acid In methanol at 5℃; for 1h;	93%
at 60℃; for 12h; Temperature; Time;	91%

: 4'-[(2-butyrylamino-3-methyl-5-(1N-methyl-1H-benzimidazol-2-yl)-phenylamino)-methyl]-biphenyl-2-carboxylic acid isopropyl ester

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
Stage #1: 4'-[(2-butyrylamino-3-methyl-5-(1N-methyl-1H-benzimidazol-2-yl)-phenylamino)-methyl]-biphenyl-2-carboxylic acid isopropyl ester With acetic acid for 3h; Reflux; Stage #2: With sodium hydroxide In ethanol for 12h; Reflux; Stage #3: With hydrogenchloride In ethanol; water for 1h; pH=5 - 6; Cooling;	92%

: 172525-90-5
4'-[(2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)-benzimidazol-1-yl)methyl]-biphenyl-2-carboxaldehyde

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
With hydrogenchloride; sodium chlorite; sodium dihydrogenphosphate; dihydrogen peroxide In water; acetonitrile at 10 - 20℃; for 1.5h;	90.6%
With oxone In N,N-dimethyl acetamide at 20 - 120℃; for 27.5h;
With sodium perborate In acetic acid at 100℃;

: C25H25BN2O4

: 49572-60-3
2-bromo-1-methyl-1H-benzo[d]imidazole

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
With palladium diacetate; sodium carbonate In 1,4-dioxane at 80℃; for 6h; Reagent/catalyst; Solvent; Suzuki Coupling; Inert atmosphere;	90.05%

: 915124-86-6
4’-((1,7′-dimethyl-2′-propyl-1H,3′H-[2,5′-bibenzo[d]imidazol]-3′-yl)methyl)-[1,1′-biphenyl]-2-carboxamide

: 144701-48-4
telmisatran

Conditions

Conditions	Yield
Stage #1: 4’-((1,7′-dimethyl-2′-propyl-1H,3′H-[2,5′-bibenzo[d]imidazol]-3′-yl)methyl)-[1,1′-biphenyl]-2-carboxamide With sulfuric acid In water at 125℃; for 28h; Stage #2: With sodium hydroxide In dichloromethane; water pH=5.4;	89%
Stage #1: 4’-((1,7′-dimethyl-2′-propyl-1H,3′H-[2,5′-bibenzo[d]imidazol]-3′-yl)methyl)-[1,1′-biphenyl]-2-carboxamide With potassium hydroxide In propylene glycol at 85 - 150℃; Stage #2: With water; acetic acid at 25 - 85℃; for 1.25h;	84%

Raw Materials

556-63-8

74-86-2

114772-38-2

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Consensus Reports

It is believed that telmisartan’s dual mode of action may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease (CVD).

Specification

1. Introduction of Telmisartan

Telmisartan, with the IUPAC Name of 2-[4-[[4-Methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid
Synonyms of Telmisartan (CAS NO.144701-48-4): 4'[(1,4'-Dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl][1,1'-biphenyl]-2-carboxylic acid, is one kind of white or off white crystalline powder. This chemical belongs to the Product Categories which include Pharmaceutical material and intermeidates; Active Pharmaceutical Ingredients; INTERMEDIATESOF; Antihypertensive; Imidazoles; (intermediates of telmisartan); Telmisartan;Hypertension; Intermediates & Fine Chemicals; Pharmaceuticals; API's. Telmisartan is also an angiotensin II receptor antagonist used in the management of hypertension.

2. Properties of Telmisartan

Telmisartan has the following properties: (1)Index of Refraction: 1.667; (2)Molar Refractivity: 154.51 cm³; (3)Molar Volume: 414.9 cm³; (4)Surface Tension: 48.7 dyne/cm; (5)Density: 1.24 g/cm³; (6)Flash Point: 420.6 °C; (7)Enthalpy of Vaporization: 117.87 kJ/mol; (8)Boiling Point: 771.9 °C at 760 mmHg; (9)Vapour Pressure: 4.58E-25 mmHg at 25°C; (10)Melting Point: 261-263°C; (11)Solubility: DMSO: >5 mg/mL at 60 °C; (12)Water Solubility: insoluble.

3. Safety Information of Telmisartan

Hazard Codes: Irritant Xi
Risk Statements: 36/37/38
R36/37/38: Irritating to eyes, respiratory system and skin.
Safety Statements: 22-24/25-36-26
S22: Do not breathe dust.
S24/25: Avoid contact with skin and eyes.
S26: In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
S36: Wear suitable protective clothing.
WGK Germany: 2