アジルサルタンカメドキソミル
アジルサルタンカメドキソミル 物理性質(zhì)
- 融點 :
- 193 - 195°C
- 貯蔵溫度 :
- Refrigerator, Under inert atmosphere
- 溶解性:
- DMSO（微量）、メタノール（微量）
- 外見 :
- 個體
- 色:
- ホワイトからオフホワイト
安全性情報
- リスクと安全性に関する聲明
- 危険有害性情報のコード(GHS)
| 絵表示（GHS） |
|
| 注意喚起語 |
警告 |
| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
區(qū)分 |
注意喚起語 |
シンボル |
P コード |
| H302 |
飲み込むと有害 |
急性毒性、経口 |
4 |
警告 |
|
P264, P270, P301+P312, P330, P501 |
| H315 |
皮膚刺激 |
皮膚腐食性/刺激性 |
2 |
警告 |
|
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
強い眼刺激 |
眼に対する重篤な損傷性/眼刺激 性 |
2A |
警告 |
|
P264, P280, P305+P351+P338,P337+P313P |
| H335 |
呼吸器への刺激のおそれ |
特定標的臓器毒性、単回暴露； 気道刺激性 |
3 |
警告 |
|
|
|
| 注意書き |
| P261 |
粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。 |
| P280 |
保護手袋/保護衣/保護眼鏡/保護面を著用するこ と。 |
| P301+P312 |
飲み込んだ場合：気分が悪い時は醫(yī)師に連絡(luò)する こと。 |
| P302+P352 |
皮膚に付著した場合：多量の水と石鹸で洗うこと。 |
| P305+P351+P338 |
眼に入った場合：水で數(shù)分間注意深く洗うこと。次にコ ンタクトレンズを著用していて容易に外せる場合は外す こと。その後も洗浄を続けること。 |
|
アジルサルタンカメドキソミル 価格
| メーカー |
製品番號 |
製品説明 |
CAS番號 |
包裝 |
価格 |
更新時間 |
購入 |
アジルサルタンカメドキソミル 化學(xué)特性,用途語,生産方法
効能
血圧降下薬, アンジオテンシンII受容體拮抗薬
定義
ChEBI: Azilsartan kamedoxomil is an organic potassium salt that is the monopotassium salt of azilsartan medoxomil. A prodrug for azilsartan, it is used for treatment of hypertension. It has a role as a prodrug, an antihypertensive agent and an angiotensin receptor antagonist. It contains an azilsartan medoxomil(1-).
臨床応用
Azilsartan kamedoxomil, developed by Takeda Pharmaceuticals,
was approved for the treatment of hypertension and launched in
the U.S. under the brand name Edarbi. Edarbi is a prodrug that
undergoes rapid hydrolysis to liberate azilsartan, the active ingredient
(TAK-536, 39). As the 8th angiotensin receptor
blocker (ARB) to enter the world market, azilsartan kamedoxomil can function as monotherapy or in combination with other antihypertensive
agents. In several clinical studies, monotherapeutic azilsartan
kamedoxomil showed superior antihypertensive activity and a favorable safety/tolerability profile in patients compared
with other established therapeutics, including valsartan, olmesartan
medoxomil, candesartan, and telmisartan.In late 2011,Takeda announced that FDA also approved the fixed-dose combination
tablet of azilsartan kamedoxomil with chlorthalidone under
the trade name of Edarbyclor.
合成
Based on the synthesis of azilsartan, the process-scale approach to azilsartan kamedoxomil is
described in the scheme. The synthesis started with commercially
available methyl 2-[(tert-butoxycarbonyl)amino]-3-nitrobenzoate
(30), which can also be prepared by several different routes.41,42
Alkylation of 30 with diaryl bromide 31 gave benzylamine 32 in
78% yield, which was followed by deprotection with 30% ethanolic
HCl and alkalinization to produce amine 33 in 77% yield. The nitro
group within 33 was reduced with hydrazine hydrate and a catalytic
amount of ferric chloride to afford 2,3-diaminobenzoate 34
in 64% yield. Ring formation was achieved by treatment of 34 with
tetraethoxymethane and acetic acid to produce benzimidazole 35
in 91% yield.37 The addition of hydroxylamine to the cyano group
of 35 provided amidoxime 36 in 55% yield, which underwent
immediate cyclization upon treatment with 2-ethylhexyl chloroformate
37 in refluxing xylenes to give oxadiazolone 38 in 52%
yield. Hydrolysis of 38 gave azilsartan (39, TAK-536) in 94%
yield. In the presence of perchlorobenzoyl chloride 40 and triethylamine,
carboxylic acid 39 was converted to the mixed acid
anhydride intermediate, which when condensed with alcohol 41
furnished benzoate 42 in 50% yield. Salt preparation of 42 was
accomplished with potassium 2-ethylhexyl carboxylate 43 affording
azilsartan kamedoxomil (V) in 63% yield.
アジルサルタンカメドキソミル 上流と下流の製品情報
原材料
準備製品
アジルサルタンカメドキソミル 生産企業(yè)
Global( 174)Suppliers
863031-24-7(アジルサルタンカメドキソミル)キーワード:
- 863031-24-7
- Azilsartan kaMedoxoMil
- 1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester potassium salt
- Azilsartan MedoxoMil PotassiuM salt
- Azilsartan MedoxoMil (MonopotassiuM salt)
- Azilsartan MedoxoMil (MonopotassiuM)
- Azilsartan MedoxiMil PotassiuM
- Azilsartan KaModoxoMil
- Azilsartan kaMedoxoMil (with 5 ints.)
- Azilsartan MedoxMil PotassuiM
- 1H-BenziMidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]Methyl] -2-ethoxy-, (5-Methyl-2-oxo-1,3-dioxol-4-yl)Methyl ester, potassiuM salt
- Azilsartan Medoxomil Potassium
- Azilsartan Mehtyl ester
- Azilsartan Impurity 50 Potassium Salt
- Azilsartan medoxomil monopotassium (TAK 491)
- Azilsartan KaMedoximil
- Azilsartan Medoxomil Potassium Crude
- Azilsartan Impurity 45 Potassium Salt
- (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate, potassium salt
- TAK 491 kamedoxomil
- TAK-491 monopotassium
- Azilsartan Impurity 60 Potassium Salt
- (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate, potassium salt
- Potassium 3-(4'-((2-ethoxy-7-(((5-methyl-2-oxo-1,3-dioxol-4-yl)methoxy)carbonyl)-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-yl)-5-oxo-5H-1,2,4-oxadiazol-2-ide
- AZILSARTAN KAMEDOXOMIL IH
- アジルサルタンカメドキソミル