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シロドシン

シロドシン 化学構造式
160970-54-7
CAS番号.
160970-54-7
化学名:
シロドシン
别名:
シロドシン;シロドシン (JP17)
英語化学名:
Silodosin
英語别名:
Urief;CS-288;Rapaflo;KMD 3213;KAD 3213;Silodosin;Silodoxin;Silodosin-d4;Silodosin API;Silodosin(Rapaflo)
CBNumber:
CB42129460
化学式:
C25H32F3N3O4
分子量:
495.53
MOL File:
160970-54-7.mol

シロドシン 物理性質

比旋光度 :
D25 -14.0° (c = 1.01 in methanol)
沸点 :
601.4±55.0 °C(Predicted)
比重(密度) :
1.249±0.06 g/cm3(Predicted)
貯蔵温度 :
Keep in dark place,Inert atmosphere,2-8°C
酸解離定数(Pka):
14.85±0.10(Predicted)
CAS データベース:
160970-54-7(CAS DataBase Reference)

安全性情報

HSコード  29339900

シロドシン 価格 もっと(11)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01COBQJ-1641 シロドシン
Silodosin
160970-54-7 100mg ¥19800 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01COBQJ-1641 シロドシン
Silodosin
160970-54-7 250mg ¥27000 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01TRCS465000 シロドシン
Silodosin
160970-54-7 100mg ¥27500 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01LKTS3346 シロドシン
Silodosin
160970-54-7 100mg ¥30300 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01W0119-1759 シロドシン 98.0+% (HPLC)
Silodosin 98.0+% (HPLC)
160970-54-7 200mg ¥37000 2021-03-23 購入

シロドシン 化学特性,用途語,生産方法

外観

白色~ほとんど白色, 結晶性粉末~粉末

溶解性

ジメチルスルホキシド及びメタノールに溶ける。

用途

α1A 受容体を選択的に阻害し ます。尿道をゆるめ、排尿障害改善作用を示 します。

効能

排尿障害改善薬, α1アドレナリン受容体拮抗薬

商品名

シロドシン (Meファルマ); シロドシン (エルメッド); シロドシン (キョーリンリメディオ); シロドシン (ニプロ); シロドシン (ニプロ); シロドシン (共創未来ファーマ); シロドシン (共創未来ファーマ); シロドシン (大原薬品工業); シロドシン (小林化工); シロドシン (日医工); シロドシン (日新製薬-山形); シロドシン (日本ケミファ); シロドシン (日本ケミファ); シロドシン (日本ジェネリック); シロドシン (沢井製薬); シロドシン (辰巳化学); シロドシン (陽進堂); シロドシン (陽進堂); シロドシン (陽進堂); シロドシン (鶴原製薬); ユリーフ (キッセイ薬品工業); ユリーフ (キッセイ薬品工業)

使用上の注意

不活性ガス封入

説明

Silodosin, an a1A adrenoceptor (a1A-AR) antagonist selective for prostatic receptors, was launched as an oral treatment for dysuria associated with benign prostatic hypertrophy (BPH). The regulation of smooth muscle tone in the bladder neck and prostate is thought to be primarily mediated by a1A-AR. Blockade of these receptors can cause smooth muscle relaxation in these areas, resulting in improved symptoms and urinary flow rates. Conversely, a1B-AR are largely located on vascular smooth muscle, and antagonism of these receptors can cause tissue relaxation and potentially decrease cardiac compensation mechanisms involved in regulating blood pressure.

化学的特性

White Solid

Originator

Kissei (Japan)

使用

An α1a-adrenoceptor antagonist. It is used in treatment of benign prostatic hypertophy.

使用

Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. It causes practically no orthostatic hypotension (in contrast to other α1 blockers). Since Silodosin is a highly selective inhibitor of the α1A adrenergic receptor, it causes pr

brand name

Urief

Chemical Synthesis

The synthesis of silodosin has been disclosed in several patents. The latest synthetic route disclosed in the 2006 patent is highlighted in the scheme. The synthesis started with Grignard generation from readily available bromoindoline 65 by treating it with Mg in the presence of a catalytic dibromoethane in THF. After initiation of the reaction with some heat and refluxing at a steady rate, CBZ protected oxazolidinone 66 [39b] was added over 1 h, refluxed for 4 h and then stirred at room temperature for 2 days. The reaction was quenched with 6 M aqueous HCl and stirred for 12 h after which time the reaction was worked up to provide product 67 in 53% yield. Ketone 67 was then treated with triethylsilane in TFA at 0oC and stirred at room temperature for 10 h to provide amine 68 in 61% yield. Bromination of the indoline 68 with bromine in warm acetic acid furnished bromide 69 in 53% yield which was reacted with copper cyanide in DMF at 130oC to give the cyano indoline 70 in 82% yield. Selective deprotection of the benzyloxycarbonyl over the benzyl group was accomplished by reacting indoline 70 with 1 atm hydrogen in the presence of 5% Pd/C in ethanol at room temperature. The resulting free amine 71 was then reacted with mesylate 72 in t-butanol with sodium carbonate as base at 80-90oC for 46 h to provide 73 in 67% yield. Removal of the benzyl ether was accomplished by reacting 73 with 1 atm hydrogen in the presence of 10%Pd/C to give alcohol 74, which upon hydrolysis provided the desired silodosin (X). No yield for the final reaction was given.

シロドシン 上流と下流の製品情報

原材料

準備製品


シロドシン 生産企業

Global( 299)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Chengdu Aslee Biopharmaceuticals, Inc.
+86 28 85305008
may.yang@asleechem.com CHINA 964 58
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Shenzhen Shengda Pharma Limited
+86-755-85269922
WeChat:shengdapharm sales@shengdapharm.com CHINA 313 58
Henan DaKen Chemical CO.,LTD.
+86-371-66670886
info@dakenchem.com China 20898 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Shanghai Time Chemicals CO., Ltd.
+8618017249410 +86-021-57951555
+86-021-57951555 jack.li@time-chemicals.com CHINA 1365 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8909 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26762 60
Shanxi Naipu Import and Export Co.,Ltd
+8613734021967
kaia@neputrading.com CHINA 1009 58

160970-54-7(シロドシン)キーワード:


  • 160970-54-7
  • Silodosin-d4
  • Silodoxin
  • 1H-Indole-7-carboxaMide,2,3-dihydro-1-(3-hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]aMino]propyl]-
  • 1-(3-hydroxypropyl)-5-[(2R)-({2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}aMino)propyl]indoline-7-carboxaMide
  • KAD 3213
  • KMD 3213
  • Urief
  • Silodosin API
  • (–)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide
  • Silodosin
  • Silodosin(Rapaflo)
  • (–)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-tr
  • (–)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]aMino]propyl]-2,3-di-h
  • (R)-1-(3-Hydroxypropyl)-5-[2-[[2-[2-(2,2,2- trifluoroethoxy)phenoxy]ethyl]aMino]propyl]indoline-7-carboxaMide
  • 2,3-Dihydro-1-(3-hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]aMino]propyl]-1H-indole-7-carboxaMide
  • Silodosin, 98%, an α1-adrenoceptor antagonist
  • Rapaflo
  • CS-288
  • Silodosin API, IH Grade
  • Silodosin (S)-Isomer
  • Silodosin fandachem
  • Silodosin USP/EP/BP
  • シロドシン
  • シロドシン (JP17)
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