CAS: 159989-65-8; (3S,4As,8As)-N-(Tert-Butyl)-2-((2R,3R)-2-Hydroxy-3-(3-Hydroxy-2-Methylbenzamido)-4-(Phenylthio)Butyl)Decahydroisoquinoline-3-Carboxamide Methanesulfonate

该化合物是一种主要用于治疗艾滋病毒感染的抗逆转录病毒药物,属于蛋白抑制剂类别,通过抑制艾滋病毒蛋白酶,防止病毒发芽和复制;该物质是白色的脱白晶粉,可溶于有机溶剂,但水溶性有限;Nelfinavir mesylate通常口服,并经常与其他抗逆转录病毒剂结合使用,以提高治疗效力和降低抗药性风险;其药用植物特征显示,它有较短的半衰期,需要每天多剂量才能有效抑制病毒;常见副作用可能包括胃肠紊乱,如腹泻和腹泻,以及潜在的代谢效应;与其他抗逆转录病毒疗法一样,监测药物相互作用和坚持治疗疗法对于最佳患者结果至关重要.

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CAS号75-75-2 甲基磺酸 | CAS号159989-64-7 奈非那韦 | CAS号67000-01-5 ethyl-isopropyl...

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    📜(2R,3R)-4-((3S,4As,8As)-3-(Tertbutylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-Hydroxy-1-(Phenylthio)Butan-2-Aminium Benzoate 以 甲醇,二氯甲烷 用作溶剂,化学反应生成甲磺酸奈非那韦
    参考文献:Optimization Of An Electrolyte System For The Simultaneous Separation Of Nelfinavir Mesylate And Two Impurities By Micellar Electrokinetic Chromatography
    标题:Optimization Of An Electrolyte System For The Simultaneous Separation Of Nelfinavir Mesylate And Two Impurities By Micellar Electrokinetic Chromatography
    摘要:A Methodology For The Simultaneous Determination Of Nelfinavir Mesylate And The Impurities 3-Hydroxy-2-Methylbenzoic Acid And (2R,3R)-4-((3S,4As,8As)-3-(Tert-Butylcarbamoyl) octahydroisoquinolin-2(1H)-yl)-3-Hydroxy-1-(Phenylthio)Butan-2-Aminium Benzoate By Micellar Electrokinetic Chromatography,With An Analysis Time Of 25 Min,Was Proposed. An Electrolyte Composed Of Sodium Tetraborate Buffer (Ph 9.24; 25 Mmol L-1),Sodium Dodecyl Sulphate (9 Mmol L-1) And Methanol (10%,V/v) Was Optimized Using A Mixed-Level Factorial Design,With Direct Detection At 200 Nm. After Evaluating Some Figures Of Merit,Such As Selectivity,Linearity,Precision,Limit Of Detection,Limit Of Quantification,Accuracy And Robustness (Using Youden'S Test),The Method Was Successfully Applied To The Analysis Of Nelfinavir Mesylate And Its Impurities In A Pharmaceutical Formulation. The Optimized Methodology Is Demonstrated To Be Useful In The Determination Of These Analytes In A Synthesis Monitoring Process,In Raw Materials And In Pharmaceutical Formulations,While Offering Low Solvent Consumption,Requiring A Small Sample And Using Non-Specific Columns As Advantages.
    Doi:10.5935/0103-5053.20150049

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    专利信息


    专利号:US-7173059-B2
    优先权日:2003-05-08
    标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same
    发明人:ALBIZATI KIM FRANCIS; BABU SRINIVASAN
    权利人:AGOURON PHARMA
    摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.

    专利号:US-6472534-B2
    优先权日:1999-10-21
    标 题:Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors
    发明人:BORER BENNETT C; ZOOK SCOTT E; BUSSE JULIETTE K
    权利人:AGOURON PHARMA
    摘要:Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.

    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-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.

    专利号:US-11845970-B2
    优先权日:2016-01-15
    标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins
    发明人:WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN
    权利人:UNIV MARYLAND
    摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.

    专利号:US-8557979-B2
    优先权日:2004-06-10
    标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
    发明人:CHOI WOO-BAEG; KOWALIK EWA
    权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
    摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

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    主要参考文献


    1: Nagao Y, Hisanaga T, Utsumi T, Egami H, Kawato Y, Hamashima Y. Enantioselective Synthesis of Nelfinavir via Asymmetric Bromocyclization of Bisallylic Amide. J Org Chem. 2018 Mar 1. doi: 10.1021/acs.joc.8b00039. [Epub ahead of print] doi: 10.1002/art.40326. Epub 2017 Dec 8. doi: 10.1038/leu.2017.212. Epub 2017 Jul 5.
    5: Sato A, Asano T, Okubo K, Isono M, Asano T. Nelfinavir and Ritonavir Kill Bladder Cancer Cells Synergistically by Inducing Endoplasmic Reticulum Stress. Oncol Res. 2018 Mar 5;26(2):323-332. doi: 10.3727/096504017X14957929842972. Epub 2017 May 26. doi: 10.2147/OTT.S136484. eCollection 2017.
    7: Dunlop EA, Johnson CE, Wiltshire M, Errington RJ, Tee AR. Targeting protein homeostasis with nelfinavir/salinomycin dual therapy effectively induces death of mTORC1 hyperactive cells. Oncotarget. 2017 Jul 25;8(30):48711-48724. doi: 10.18632/oncotarget.16232.

    合成参考文献


    摘要:Gekkan Yakuji. Pharmaceuticals Monthly., 40(3395), 1998
    摘要:Full text:
    摘要:MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 1986
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