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Allisartan Isoproxil

Product Name
Allisartan Isoproxil
CAS No.
947331-05-7
Chemical Name
Allisartan Isoproxil
Synonyms
Allisartan;Allisartan Isoproxil;Losartan Impurity N9;Losartan Impurity 19(Allisartan Isoproxil);1H-Imidazole-5-carboxylic acid, 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, [[(1-methylethoxy)carbonyl]oxy]methyl ester
CBNumber
CB03159860
Molecular Formula
C27H29ClN6O5
Formula Weight
553.01
MOL File
947331-05-7.mol
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Allisartan Isoproxil Property

Boiling point:
745.0±70.0 °C(Predicted)
Density 
1.35±0.1 g/cm3(Predicted)
pka
4.16±0.10(Predicted)
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Hazard and Precautionary Statements (GHS)

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Allisartan Isoproxil Chemical Properties,Usage,Production

Clinical Use

Allisartan isoproxil, a member of a new class of selective angiotensin II-1 receptor antagonists, was approved by the Chinese Food and Drug Administration (CFDA) for the treatment of hypertension in July 2012.19 At time of publication, there is no trade name associated with this drug. Allisartan was discovered and developed by the Chinese biomedical company Allist Pharmaceuticals. Allisartan isoproxil is a prodrug which is readily hydrolyzed to active metabolite EXP3174, which is also the active metabolite of losartan (des-triphenylmethyl-9).

Synthesis

Although several synthetic routes have been reported within two patents, the most likely scalable process route is described in the scheme. Commercial 2-butyl-4-chloro-5-(hydroxymethyl)-imidazole (7) was alkylated with Ntriphenylmethyl- 5-(4'-bromomethylbiphenyl-2-yl)tetrazole (8) under basic conditions in warm DMF, providing alcohol 9 in 90% yield. This alcohol was then oxidized to the corresponding carboxylic acid 10 with KMnO4 in 88% yield. Etherification of acid 10 with isopropyl chloromethyl carbonate (11) followed by de-tritylation of the tetrazole group under acidic contidions gave allisartan isoproxil (II) in 69% yield.

Allisartan Isoproxil Preparation Products And Raw materials

Raw materials

Preparation Products

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Allisartan Isoproxil Suppliers

Yichang Chanod Biomedical Technology Co,LTD
Tel
0717-6855399 15377615856
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sales@sndswyy.cn
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China
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84
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Cdreamlab (Hubei) Technology Co., LTD
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0717-6300888 18062399888
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service@cdreamlab.com
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China
ProdList
299
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Allikang Pharmaceutical Co., LTD
Tel
0573-87390950 13806705416
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wzj@alicornpharma.com
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China
ProdList
71
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ChemStrong Scientific Co.,Ltd
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0755-0755-66853366 13670046396
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0755-28363542
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sales@chem-strong.com
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China
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17993
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Nanjing Chalf-Pharm Technology Co., Ltd.
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025-57018978 18251899859
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025-57018008
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China
ProdList
5923
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Chengdu DingDang Pharmaceutical Co., Ltd.
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028-86040038 13980902949;
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market@dingdangchem.com
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China
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1758
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ATK CHEMICAL COMPANY LIMITED
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+86-21-51619052
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10004
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Shanghai Chaolan Chemical Technology Center
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QQ:65489617 15618227136
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21-5161 9052
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9838
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Shenzhen SUNGENING Bio-Medical Co., Ltd.
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0755-28967200 13631290199
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Chengdu Novel Biomedical Co., Ltd.
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028-85255396 18302801538
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028-85255396
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947331-05-7, Allisartan IsoproxilRelated Search:


  • Allisartan Isoproxil
  • Allisartan
  • 1H-Imidazole-5-carboxylic acid, 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, [[(1-methylethoxy)carbonyl]oxy]methyl ester
  • Losartan Impurity 19(Allisartan Isoproxil)
  • Losartan Impurity N9
  • 947331-05-7