| Identification | Back Directory | [Name]
Ethyl-2-Ethoxy-1-[[(2'-(1h-Tetrazol-5-Yl)Biphenyl-4-Yl)Methyl]Benzimidazole]-7-Carboxylate | [CAS]
139481-69-9 | [Synonyms]
Candesartan Methyl Ester
Candesartan Impurity 7
candesartan methyl ester imp
Candesartan Cilexetil impurity I
Candesartan methyl ester impurity
candesartan cilexetil impurity1361
Candesartan Cilexetil EP IMpurity I
CANDESARTAN INTERMEDIATES(METHYL ESTER C7)
Candesartan Cilexetil Impurity 9(EP Impurity I)
Candesartan Cilexetil EP Impurity I (Candesartan Methyl Ester)
Methyl-2-Ethoxy-1-[[(2'-(1h-Tetrazol-5-Yl)Biphenyl-4-Yl)Meth...
ETHYL2-ETHOXY-1-[[2'-(1H-TETRAZOL-5-YL)METHYL]BENZIMIDAZOLE-7-CARBOXYLATE
thyl-2-ethoxy-1-[[2'-(1Htetrazol-5-yl-)methyl]benzimidazole]-7-carboxylate
Ethyl-2-Ethoxy-1-[[(2'-(1h-Tetrazol-5-Yl)Biphenyl-4-Yl)Methyl]Benzimidazole]-7-Carboxylate
Methyl 1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)-methyl)-2-ethoxy-1H-benzo[d]imidazole-7
Methyl 1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)-methyl)-2-ethoxy-1H-benzo[d]imidazole-7-ca
Methyl 1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)Methyl)-2-ethoxy-1H-benzo[d]iMidazole-7-carboxylate
methyl 1-((2,-(1H-tetrazol-5-yl)-[1,1,-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
2-ethoxy-4-ethyl-1-{[4-phenyl-3-(1H-1,2,3,4-tetrazol-5-yl)phenyl]Methyl}-1H-1,3-benzodiazole-7-carboxylate
2-Ethoxy-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]Methyl]-1H-benziMidazole-7-carboxylic Acid Methyl Ester
1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, methyl ester
2-Ethoxy-1-[[2-[1-(triphenylmethyl)-1H-tetrazol-5-yl][1,1-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid methyl ester
Candesartan Cilexetil EP Impurity IQ: What is
Candesartan Cilexetil EP Impurity I Q: What is the CAS Number of
Candesartan Cilexetil EP Impurity I Q: What is the storage condition of
Candesartan Cilexetil EP Impurity I Q: What are the applications of
Candesartan Cilexetil EP Impurity I | [EINECS(EC#)]
604-139-3 | [Molecular Formula]
C25H22N6O3 | [MDL Number]
MFCD09263633 | [MOL File]
139481-69-9.mol | [Molecular Weight]
454.48 |
| Chemical Properties | Back Directory | [Melting point ]
169-173°C | [Boiling point ]
704.5±70.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,2-8°C | [solubility ]
Chloroform (Slightly), Methanol (Slightly) | [form ]
Solid:particulate/powder | [pka]
4.15±0.10(Predicted) |
| Hazard Information | Back Directory | [Chemical Properties]
Off-White Solid | [Uses]
An intermediate in the preparation of Candesartan (C175575). | [Uses]
Candesartan Methyl Ester (Candesartan Cilexetil EP Impurity I) is an intermediate in the preparation of Candesartan (C175575). | [Synthesis]
1. Methyl 2-ethoxy-1-[(2'-cyanobiphenyl-4-yl)methyl]-1H-benzimidazole-7-carboxylate (310 g) and toluene (2.48 L) were added to a reactor, followed by tributyltin chloride (737 g), sodium azide (146 g) and tetrabutylammonium bromide (31 g).
2. The reaction mixture was slowly heated to 110 °C and maintained at 110-115 °C for 24 h, during which the progress of the reaction was monitored by TLC.
3. After completion of the reaction, the reaction mixture was cooled to 15 °C and methanol (3.1 L), water (2.17 L) and acetic acid (930 g) were added sequentially.
4. The mixture was stirred at 15-20 °C for 1 h to promote product separation.
5. After addition of toluene (1.24 L), the reaction mixture was filtered at 15-20 °C.
6. the filter cake was washed thoroughly with water (0.93 L) until the pH of the wash solution reached 5.5-7.0 to completely remove the acid.
7. The filter cake was washed again with toluene (0.62 L) and dried by suction filtration.
8. The product was air dried at 50-55 °C to give methyl 2-ethoxy-1-[[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]benzimidazole]-7-carboxylate. Yield: 290 g (85%). | [IC 50]
AT2 Receptor: 0.11 μM (IC50) | [References]
[1] Journal of Medicinal Chemistry, 1993, vol. 36, # 15, p. 2182 - 2195
[2] Patent: WO2005/51929, 2005, A1. Location in patent: Page/Page column 18
[3] Patent: US2009/203920, 2009, A1. Location in patent: Page/Page column 4
[4] Patent: EP1420016, 2004, A1. Location in patent: Page 19
[5] Patent: WO2009/157001, 2009, A2. Location in patent: Page/Page column 3 |
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