CAS: 150378-17-9; (S)-1-((2S,4R)-4-Benzyl-2-Hydroxy-5-(((1S,2R)-2-Hydroxy-2,3-Dihydro-1H-Inden-1-yl)Amino)-5-Oxopentyl)-N-(Tert-Butyl)-4-(Pyridin-3-Ylmethyl)Piperazine-2-Carboxamide

该化合物是一个复杂的有机化合物,其特征是其特定的立体化学和功能组;其特征是:一个聚酰胺骨柱,表明存在一个附属于五碳链的氨化物功能组;该化合物包括多个手性中心,有助于其立体异构学,并包含各种替代成分,如氢氧化物组,一个管状子环和一个丙酰胺系;这些结构要素表明潜在的生物活动,可能是一个制药剂;成体的三丁基聚物组和苯甲基基亚基亚基元素的存在可能影响其溶性以及与生物目标的相互作用;此外,该化合物的复杂结构意味着它可能表现出特定的结合性和药用化学作用.

结构式图片

上下游产品

CAS号6959-48-4 3-氯甲基吡啶盐酸盐 | CAS号150323-38-9 [1(1S,2R),5(S)]... | CAS号848482-93-9 (S)-1-B°C-3-甲酸哌嗪 | CAS号150407-69-5 (S)-N-4-B°C-N-1... | CAS号150323-35-6 4-叔丁氧羰基-2(S)-哌嗪叔丁酰胺 | CAS号150323-36-7 dihydro-5(S)-[[... | CAS号32780-06-6 (S)-(+)-γ-羟甲基-γ-丁内酯

合成工艺路线路线简述

    (S)-4-[(2S,4R)-4-Benzyl-5-((3As,8Ar)-2,2-Dimethyl-8,8A-Dihydro-3Ah-Indeno[1,2-D]Oxazol-3-yl)-2-Hydroxy-5-Oxo-Pentyl]-3-Tert-Butylcarbamoyl-Piperazine-1-Carboxylic Acid Tert-Butyl Ester置于盐酸体系中,化学反应生成茚地那韦
    参考文献:手性非外消旋酰胺烯酸酯与(S)-缩水甘油基甲苯磺酸酯的高度非对映选择性反应.口服活性hiv-1蛋白酶抑制剂l-735,524的合成
    标题:手性非外消旋酰胺烯酸酯与(S)-缩水甘油基甲苯磺酸酯的高度非对映选择性反应.口服活性hiv-1蛋白酶抑制剂l-735,524的合成
    摘要:手性酰胺烯酸酯li-1与(S)-缩水甘油基甲苯磺酸酯11的反应以高非对映体选择性得到环氧化物3,产率为72%.环氧化物3以71%的分离产率转化为口服活性的hiv-1蛋白酶抑制剂l-735,524.
    Doi:10.1016/s0040-4039(00)75787-X

    海关参考信息

    专利信息


    专利号:US-9233943-B2
    优先权日:2012-01-10
    标题:Process for synthesis of syn azido epdxide and its use as intermediate for the synthesis of amprenavir and saquinavir
    发明人:GADAKH SUNITA KHANDERAO; REKULA REDDY SANTHOSH; SUDALAI ARUMUGAM
    权利人:COUNCIL SCIENT IND RES
    摘要:A novel synthetic route to the syn-azido epoxide of formula 5 includes cobalt-catalyzed hydrolytic kinetic resolution of a racemic mixture of the azido-epoxide. Reaction steps include subjecting an allylic alcohol to epoxidation with mCPBA to obtain a racemic epoxy alcohol; ring opening the epoxy alcohol with azide anion to obtain an anti-azido alcohol, which can then be selectively tosylated at the primary alcohol; treating the tosylate with base to obtain the racemic azido-epoxide; and subjecting the racemic azido-epoxide to cobalt-catalyzed hydrolytic kinetic resolution to obtain the syn-azido epoxide of formula 5. The compound of formula 5 may be used as a common intermediate for the asymmetric synthesis of HIV protease inhibitors, such as Amprenavir, Fosamprenavir, Saquinavir, and formal synthesis of Darunavir and Palinavir.

    专利号:US-6818633-B2
    优先权日:2001-06-29
    标题:Antiviral compounds and methods for synthesis and therapy
    发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN
    权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING
    摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).

    专利号:US-7189849-B2
    优先权日:1997-02-10
    标 题:Synthesis of acyclic nucleoside derivatives
    发明人:LEANNA M ROBERT; RASMUSSEN MICHAEL; HANNICK STEVEN M; TIEN JIEN-HEH J; LUKIN KIRILL A; TIAN ZHENPING; CHANG SOU-JEN; CURTY CYNTHIA B; NARAYANAN BIKSHANDARKOIL A; BELLETTINI JOHN; SHELAT BHADRA; SPITZ TIFFANY
    权利人:MEDIVIR AB
    摘要:Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.

    专利号:US-8987493-B2
    优先权日:2010-05-20
    标题 :Process for synthesis of silane dipeptide analogs
    发明人:SIEBURTH SCOTT MCNEILL; BO YINGJIAN
    权利人:SIEBURTH SCOTT MCNEILL; BO YINGJIAN; Temple University—Of the Commonwealth System of Higher Education
    摘要:The invention provides a method of preparing silane dipeptide analogs, comprising the steps of treating a solution of a substituted 1,2-oxasilolane with lithium metal to form a solution of the dilithium salt of a substituted 3-hydroxypropylsilanol, and reacting the solution of the dilithium salt of the substituted 3-hydroxypropylsilanol with a substituted enamine.

    专利号:US-2010261876-A1
    优先权日:2007-09-25
    标 题:Novel methods of synthesis for therapeutic antiviral peptides
    发明人:BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E
    权利人:BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E
    摘要:Provided herein are methods for synthesis of peptides. In particular, provided herein are methods of synthesis for therapeutic antiviral peptides.

    专利号:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
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    主要参考文献


    1: Barrail-Tran A, Taburet AM, Poirier JM; Groupe Suivi Therapeutique Pharmacologique de la Societe Francaise de Pharmacologie et de Therapeutique. [Evidence-based therapeutic drug monitoring for indinavir]. Therapie. 2011 May-Jun;66(3):239-46. doi: 10.2515/therapie/2011035. Epub 2011 Aug 9. Review. French. Review. Review. Review. Spanish. Review. Review. Review. Review. Review. Review. Review. Review.
    13: Youle M. Optimizing indinavir regimens. HIV Med. 2000 Jul;1 Suppl
    2:7-11. Review. Review. Review. Review. Review. French. Review.

    合成参考文献


    参考文献:10.4103/0971-6866.80354
    摘要:Shankarkumar U, Shankarkumar A, Ghosh K. Human immunodeficiency virus therapeutics and pharmacogenomics. Indian J Hum Genet. 2011 May;17 Suppl 1():S22–6.
    参考文献:10.1016/j.jchromb.2011.06.032
    摘要:Huang J, Gautam N, Bathena SP, Roy U, McMillan J, Gendelman HE, Alnouti Y. UPLC-MS/MS quantification of nanoformulated ritonavir, indinavir, atazanavir, and efavirenz in mouse serum and tissues. J Chromatogr B Analyt Technol Biomed Life Sci. 2011 Aug 01;879(23):2332–8.
    参考文献:10.1371/journal.pone.0021824
    摘要:Menezes P, Miller WC, Wohl DA, Adimora AA, Leone PA, Miller WC, Eron JJ. Does HAART Efficacy Translate to Effectiveness Evidence for a Trial Effect. PLoS ONE. 2011 Jul 13;6(7):e21824. doi: 10.1371/journal.pone.0021824.
    参考文献:10.3797/scipharm.1012-17
    摘要:Bielenica A, Kossakowski J, Struga M, Dybała I, Loddo R, Ibba C, La Colla P. Synthesis and Biological Evaluation of New 3-Phenyl-1-[(4-arylpiperazin-1-yl)alkyl]-piperidine-2,6-diones. Sci Pharm. 2011 Apr;79(2):225–38.
    参考文献:10.1097/qai.0b013e318211b43b
    摘要:Bastard M, Fall MB, Lanièce I, Taverne B, Desclaux A, Ecochard R, Sow PS, Delaporte E, Etard JF. Revisiting long-term adherence to highly active antiretroviral therapy in Senegal using latent class analysis. J Acquir Immune Defic Syndr. 2011 May 01;57(1):55–61. doi: 10.1097/qai.0b013e318211b43b.
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