CAS: 127779-20-8; (S)-N1-((2S,3R)-4-((3S,4As,8As)-3-(Tert-Butylcarbamoyl)Octahydroisoquinolin-2(1H)-yl)-3-Hydroxy-1-Phenylbutan-2-yl)-2-(Quinoline-2-Carboxamido)Succinamide

该化合物是主要用于治疗艾滋病毒/艾滋病的抗逆转录病毒药物,属于蛋白抑制剂类别,它抑制了对病毒复制过程至关重要的蛋白酶,其特点是口服时生物利用率相对较低,需要与其他抗逆转录病毒剂一起管理,以提高其功效;该化合物通常被描述为混血盐,这提高了其溶性性和稳定性;化学上,Satiminavir具有复杂的结构,包括多个手性中心,有助于其药理活动;众所周知,其副作用包括胃肠扰动,以及由于通过cytochrome P450系统的新陈代谢而与其他药物可能发生互动;Satinavir的发展标志着艾滋病毒治疗的重大进步,而且经常被用于混合疗法,以达到更好的病毒抑制,改善患者结果.

结构式图片

上下游产品

CAS号136465-98-0 N-(2-喹啉基羰基)-L-天冬氨酰胺 | CAS号136522-17-3 (3S,4a,8aS)-2-[... | CAS号128019-40-9 N-(TERT-BUTYL)D... | CAS号32150-91-7 (S)-2-(1,3-diox... | CAS号136465-80-0 2(S)-[2-phenyl-... | CAS号136465-78-6 N-tert-Butyldec... | CAS号136522-18-4 benzyl N-[(2S)-... | CAS号63-91-2 L-苯丙氨酸 | CAS号74163-81-8 (S)-1,2,3,4-四氢异... | CAS号149845-06-7 甲磺酸沙奎那韦

合成工艺路线路线简述

    1-Hydroxy-4-Phenyl-3(S)-Phthalimido-2-Butanone置于palladium On Activated Charcoal 盐酸,Sodium Tetrahydroborate,乙醇,Potassium Tert-Butylate,氢气,对甲苯磺酸,甲胺体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应生成沙喹那韦
    参考文献:Goehring,Wolfgang; Gokhale,Surendra; Hilpert,Hans,Chimia,1996,Vol. 50,# 11,P. 532-537
    标题:Goehring,Wolfgang; Gokhale,Surendra; Hilpert,Hans,Chimia,1996,Vol. 50,# 11,P. 532-537

    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: Muret P, Solas C; Groupe Suivi Therapeutique Pharmacologique de la Societe Francaise de Pharmacologie et de Therapeutique. [Evidence-based therapeutic drug monitoring for saquinavir]. Therapie. 2011 May-Jun;66(3):207-12. doi: 10.2515/therapie/2011029. Epub 2011 Aug 9. Review. French. doi: 10.1517/17425250903273160. Review. Review. Review. Review.

    合成参考文献


    参考文献:10.1186/1752-0509-5-110
    摘要:Bordbar A, Jamshidi N, Palsson BO. iAB-RBC-283: A proteomically derived knowledge-base of erythrocyte metabolism that can be used to simulate its physiological and patho-physiological states. BMC Systems Biology. 2011 Jul 12;5(1):110. doi: 10.1186/1752-0509-5-110.
    参考文献:10.2147/ijn.s20903
    摘要:Shen Q, Wang Y, Zhang Y. Improvement of colchicine oral bioavailability by incorporating eugenol in the nanoemulsion as an oil excipient and enhancer. Int J Nanomedicine. 2011;6():1237–43.
    参考文献:10.1016/j.antiviral.2011.07.001
    摘要:Canducci F, Ceresola ER, Saita D, Al-Abed Y, Garotta G, Clementi M, Nicoletti F. The new and less toxic protease inhibitor saquinavir-NO maintains anti-HIV-1 properties in vitro indistinguishable from those of the parental compound saquinavir. Antiviral Res. 2011 Sep;91(3):292–5. doi: 10.1016/j.antiviral.2011.07.001.
    参考文献:10.1016/j.colsurfb.2011.06.026
    摘要:Kuo YC, Yu HW. Polyethyleneimine/poly-(γ-glutamic acid)/poly(lactide-co-glycolide) nanoparticles for loading and releasing antiretroviral drug. Colloids Surf B Biointerfaces. 2011 Nov 01;88(1):158–64. doi: 10.1016/j.colsurfb.2011.06.026.
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