[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.
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.