ベクラブビル

ベクラブビル 価格

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

ベクラブビル 化学特性,用途語,生産方法

効能

抗ウイルス薬, NS5Bポリメラーゼ阻害薬

説明

Beclabuvir is a non-nucleoside, nonstructural protein 5B (NS5B) polymerase inhibitor approved in Japan as part of a fixed-dose combination product for the treatment of hepatitis C virus (HCV). Upon administration and after intracellular uptake, the drug binds to the allosteric, noncatalytic “Thumb 1” site of NS5B resulting in a decreased rate of viral RNA synthesis and replication.4 Beclabuvir is combined with asunaprevir and declatasvir (both approved in 2014) and was discovered and developed by Bristol-Myers Squibb.

合成

The syntheses of asunaprevir and declatasvir were described in an earlier review article.Condensation of indole-6-carboxylic acid (1) with cyclohexanone under basic conditions gave acid 2 in quantitative yield. Hydrogenation of the double bond in 2 using Pearlman?ˉs catalyst was followed by esterification to give ester 3 in high yield. Bromination of the indole at the 2-position was accomplished with pyridinium tribromide, and this was followed by saponification to provide acid 4. Treatment of 4 with carbonyldiimidazole (CDI) followed by N,N- dimethylsulfamide and 1, 8 - diazabicyclo[5.4.0]undec-7-ene (DBU) gave compound 5 in 74% yield. Suzuki coupling of 5 with commercial boronic acid 6 provided intermediate 7, which converted to hemiaminal 8 upon continued heating in 61% yield. Compound 8 was then treated with methyl 2-(dimethoxyphosphoryl)acrylate (9) to affect a tandem conjugate addition and Horner?Wadsworth? Emmons (HWE) olefination to give ester 10. Alternatively, the Suzuki coupling reaction of 5 with 6 could be stopped at intermediate 7, which could be treated with 9 to promote the tandem conjugate addition/HWE to give 10. Corey?-Chaykovsky cyclopropanation of 10 using sodium hydride and trimethylsulfoxonium iodide followed by chiral separation provided cyclopropane 11 in good yield and >99% enantiomeric excess (ee). Saponification of the methyl ester of 11 followed by coupling with 3-methyl-3,8-diazabicyclo[3.2.1]- octane dihydrochloride (12) gave beclabuvir (I) in high yield.

ベクラブビル 上流と下流の製品情報

原材料

準備製品

ベクラブビル 生産企業

名前	電話番号	電子メール	国籍	製品カタログ	優位度
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Wuhan Topule Biopharmaceutical Co., Ltd	+8618327326525	masar@topule.com	China	8474	58
Aladdin Scientific	+1-+1(833)-552-7181	sales@aladdinsci.com	United States	52927	58
Amadis Chemical Company Limited	571-89925085	sales@amadischem.com	China	131980	58
Shanghai Biopharmaleader Co., Ltd.	+86 18721201413	sales@biopharmaleader.com	China	1720	58
Musechem	+1-800-259-7612	info@musechem.com	United States	4662	60
Fan De(Beijing) Biotechnology Co., Ltd.	15911056312	liming@bio-fount.com	China	9730	58
Hangzhou Synstar pharmaceutical Technology CO.,Ltd	0571-85361029	synstar518@163.com	China	1991	58
Shanghai zhigan biotechnology co., LTD		zhiqianbio@126.com	China	19785	58

---

• 958002-33-0
• Beclabuvir
• Beclabuvir(BMS-791325)
• (1aR,12bS)-8-cyclohexyl-N-[(dimethylamino)sulfonyl]-1,1a,2,12b-tetrahydro-11-methoxy-1a-[(3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl]-cycloprop[d]indolo[2,1-a][2]benzazepine-5-carboxamide
• Cycloprop[d]indolo[2,1-a][2]benzazepine-9-carboxamide, 12-cyclohexyl-N-[(dimethylamino)sulfonyl]-4b,5,5a,6-tetrahydro-3-methoxy-5a-[(3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl]-, (4bS,5aR)-
• ベクラブビル
• (2S,4R)-N-(ジメチルスルファモイル)-18-メトキシ-4-[[(1R,5S)-3-メチル-3,8-ジアザビシクロ[3.2.1]オクタン-8-イル]カルボニル]-6-アザペンタシクロ[13.4.0.02,4.06,14.07,12]ノナデカン-1(19),7,9,11,13,15,17-ヘプタエン-9-カルボアミド
• (8S,10R)-N-(ジメチルスルファモイル)-5-メトキシ-10-[(1R,5S)-3-メチル-3,8-ジアザビシクロ[3.2.1]オクタン-8-カルボニル]-12-アザペンタシクロ[10.7.0.02,7.08,10.013,18]ノナデカ-1(19),2,4,6,13,15,17-ヘプタエン-15-カルボキサミド