Allisartan Isoproxil
- CAS No.
- 947331-05-7
- Chemical Name:
- Allisartan Isoproxil
- Synonyms
- Allisartan;Allisartan Isoproxil;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
- Molecular Weight:
- 553.01
- MDL Number:
- MFCD28502030
- MOL File:
- 947331-05-7.mol
| Boiling point | 745.0±70.0 °C(Predicted) |
|---|---|
| Density | 1.35±0.1 g/cm3(Predicted) |
| pka | 4.16±0.10(Predicted) |
| FDA UNII | DI4662MK4N |
Allisartan Isoproxil Chemical Properties,Uses,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
Allisartan Isoproxil Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| Hebei Miaoyin Technology Co.,Ltd | +86-17367732028 +86-17367732028 | kathy@hbyinsheng.com | China | 3582 | 58 |
| Yichang Chanod Biomedical Technology Co,LTD | 0717-6855399 15377615856 | sales@sndswyy.cn | China | 83 | 58 |
| Cdreamlab (Hubei) Technology Co., LTD | 0717-6300888 18062399888 | service@cdreamlab.com | China | 315 | 58 |
| Allikang Pharmaceutical Co., LTD | 0573-87390950 13806705416 | wzj@alicornpharma.com | China | 71 | 58 |
| ChemStrong Scientific Co.,Ltd | 0755-66853366 13670046396 | sales@chem-strong.com | China | 17982 | 56 |
| Nanjing Chalf-Pharm Technology Co., Ltd. | 025-57018978 18251899859 | sales@chalf-pharm.com | China | 5950 | 50 |
| Chengdu DingDang Pharmaceutical Co., Ltd. | 028-86040038 13980902949; | market@dingdangchem.com | China | 1746 | 55 |
| ATK CHEMICAL COMPANY LIMITED | 3429815786 13301662590 | sales@atkchemical.com | China | 10007 | 55 |