CAS: 402957-28-2; (1S,3Ar,6As)-2-((S)-2-((S)-2-Cyclohexyl-2-(Pyrazine-2-Carboxamido)Acetamido)-3,3-Dimethylbutanoyl)-N-((S)-1-(Cyclopropylamino)-1,2-Dioxohexan-3-yl)Octahydrocyclopenta[c]Pyrrole-1-Carboxamide

该化合物是一种抗病毒药物,主要用于治疗慢性丙型肝炎病毒(HCV)感染,属于一种被称为蛋白酶抑制剂的药物,它抑制了对病毒复制至关重要的NS3/4A蛋白酶,对病毒复制至关重要,Telaprevir具有化学配方的特点,其中包括碳,氢,氮和氧等元素,反映了其复杂的有机结构.该物质通常与其他抗病毒剂结合使用,以提高功效和降低抗药风险.Telaprevir以其相对较高的口服生物利用率而闻名,主要在肝脏中代谢,半衰期允许每日两次服用.常见副作用包括疲劳,恶心和狂躁等.由于它的具体行动机制和新疗法的出现,使用Traprevir已经演化,但在HCV治疗的历史背景下,它仍然是一个重要的选择.

结构式图片

欧盟法规

C&L通报REACH预注册

上下游产品

CAS号1257874-86-4 (3S)-3-((1S,3aR... | CAS号402958-96-7 (2S)-2-环己基-N-(2... | CAS号402958-25-2 特拉匹伟/VX950中间体1 | CAS号98-97-5 2-吡嗪羧酸 | CAS号22724-81-8 L-正缬氨醇 | CAS号145618-11-7 methyl (2S)-2-a... | CAS号848777-30-0 (S)-2-环丙基-2-(吡咯... | CAS号848777-29-7 Cyclohexaneacet... | CAS号402958-95-6 (2S)-2-环己基-N-(2...

合成工艺路线路线简述

  • 合成目标产物 Telaprevir 主要起始原料 1257874-86-4
  • (文献来源)合成步骤主要原料 1257874-86-4
[2H]-Telaprevir 反应生成 特拉匹韦
参考文献:Deuterated Hepatitis C Protease Inhibitors
标题:Deuterated Hepatitis C Protease Inhibitors
摘要:一种氘代的α-酮氨基立体特异化合物,其化学式为其中d表示立体特异碳原子上的一个氘原子.

专利信息


专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-8686145-B2
优先权日:2010-02-25
标 题 :Process for the preparation of α-acyloxy β-formamido amides
发明人:RUIJTER EELCO; ORRU ROMANO; ZNABET ANASS; POLAK MARLOES; TURNER NICHOLAS
权利人:RUIJTER EELCO; ORRU ROMANO; ZNABET ANASS; POLAK MARLOES; TURNER NICHOLAS; VERENIGING VOOR CHRISTELIJK HOGER ONDERWIJS WETENSCHAPPELIJK ONDERZOEK EN PATIENTENZORG C O TECHNOLO
摘要:The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R 2 COOH and a compound of the general Formula IV R 3 NC under such conditions that compound I is formed, wherein R 1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R 2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R 3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.

专利号:US-9573939-B2
优先权日:2011-09-08
标题:Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
发明人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; DANG QUN
权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; DANG QUN; MERCK SHARP & DOHME; MSD ITALIA SRL
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-12312361-B2
优先权日:2020-02-06
标题 :Methods for practical synthesis of deuterated amino acids
发明人:WANG WEI
权利人:UNIV ARIZONA
摘要:Disclosed are a deuterated compound of formula (I), or a salt thereof, and methods for preparation thereof. The present disclosure may provide a mild, versatile organophotoredox method for the preparation of diverse, enantioenriched α-deuterated α-amino acids. In particular, the present disclosure may address the long-standing challenge of installing sterically demanding side chains into α-amino acids, including late-stage modifications on medicinal agents and natural products.

专利号:US-2014148574-A1
优先权日:2012-11-29
标题 :Synthesis of an intermediate of an antiviral compound
发明人:ALLEGRINI PIETRO; BRUNOLDI ENRICO; ATTOLINO EMANUELE; BOVE ALESSIO
权利人:ALLEGRINI PIETRO; BRUNOLDI ENRICO; ATTOLINO EMANUELE; BOVE ALESSIO; DIPHARMA FRANCIS SRL
摘要:Process for the preparation of a cyclopropylamide compound which is useful as a structural unit in a process for the preparation of a viral protease inhibitor.

专利号:US-2015038677-A1
优先权日:2012-03-16
标 题:Process for the synthesis of telaprevir, or pharmaceutically acceptable salts or solvates as well as intermediate products thereof
发明人:FELZMANN WOLFGANG; BRUNNER STEFANIE; WILHELM THORSTEN
权利人:SANDOZ AG
摘要:The invention relates to a process for the preparation of telaprevir, or a pharmaceutically acceptable salt or solvate thereof, wherein the process requires a smaller number of process steps and/or does not require the use of toxic and instable compounds compared to the known processes. Another embodiment refers to telaprevir, or a pharmaceutically acceptable salt or solvate thereof as well as to intermediate products for preparation of the same, wherein the afore-mentioned products are obtained by the process described herein.
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主要参考文献


1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Telaprevir. 2025 Aug 15. 2012–. Telaprevir. 2022 Jan 26. 15(3):555-71. doi: 10.1016/j.cld.2011.05.013. 10(3):179-202. doi: 10.2165/11586020-000000000-00000.
5: Roujeau JC, Mockenhaupt M, Tahan SR, Henshaw J, Martin EC, Harding M, van Baelen B, Bengtsson L, Singhal P, Kauffman RS, Stern RS. Telaprevir-related dermatitis. JAMA Dermatol. 2013 Feb;149(2):152-8. doi: 10.1001/jamadermatol.2013.938. 13(2):199-200. 31 Suppl
3:26-32. Spanish. doi: 10.1016/S0213-005X(13)70121-6. 32 Suppl

合成参考文献


参考文献:10.1038/nbt0711-553
摘要:Sheridan C. New Merck and Vertex drugs raise standard of care in hepatitis C. Nat Biotechnol. 2011 Jul 11;29(7):553–4. doi: 10.1038/nbt0711-553.
参考文献:10.1056/nejmc1105515
摘要:Limaye AR, Draganov PV, Cabrera R. Boceprevir for chronic HCV genotype 1 infection. N Engl J Med. 2011 Jul 14;365(2):176; author reply 177–8. doi: 10.1056/nejmc1105515.
参考文献:10.1016/j.medmal.2011.04.003
摘要:Corouge M, Pol S. New treatments for chronic hepatitis C virus infection. Médecine et Maladies Infectieuses. 2011 Nov;41(11):579–87. doi: 10.1016/j.medmal.2011.04.003.
摘要:Telaprevir (Incivek) and boceprevir (Victrelis) for chronic hepatitis C. Med Lett Drugs Ther. 2011 Jul 25;53(1369):57–9.
参考文献:10.1186/1743-422x-10-53
摘要:Zhang EZ, Bartels DJ, Frantz J, Seepersaud S, Lippke JA, Shames B, Zhou Y, Lin C, Kwong A, Kieffer TL. Development of a sensitive RT-PCR method for amplifying and sequencing near full-length HCV genotype 1 RNA from patient samples. Virology Journal. 2013 Feb 12;10(1):53. doi: 10.1186/1743-422x-10-53.
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