CAS: 136465-81-1; (3S,4As,8As)-N-(Tert-Butyl)Decahydroisoquinoline-3-Carboxamide

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相似化合物

168899-60-3 1862323-56-5 1862340-28-0

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Tert-Butyl (3S,4As,8As)-3-(Tert-Butylcarbamoyl)-3,4,4A,5,6,7,8,8A-Octahydro-1H-Isoquinoline-2-Carboxylate 143978-60-3

合成工艺路线路线简述

    (S)-N-叔丁基-1,2,3,4-四氢异喹啉-3-甲酰胺置于rhodium Contaminated With Carbon,氢气体系中,用 异丙醇 用作溶剂,130.0 °C,3.04 Mpa 条件下,以82.6%的收率获得n-叔丁基-十氢异喹啉-3(S)-甲酰胺
    参考文献:十氢异喹啉类化合物及其制备方法和用途
    标题:十氢异喹啉类化合物及其制备方法和用途
    摘要:本发明提供了一种式i所述的十氢异喹啉类化合物及其制备方法和用途.本发明的十氢异喹啉类化合物为埃博拉侵入抑制剂,作用于ebov‑gp靶点,具有较强的生物活性和较好的选择性,可作为ebov‑gp抑制剂的应用和其在制备治疗埃博拉病等相关药物中的应用.#imgabs0#

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    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-5569762-A
    优先权日:1994-01-14
    标题:Asymmetric synthesis of intermediates for retroviral protease inhibitor compounds
    发明人:WISSNER ALLAN; TROVA MICHAEL P
    权利人:AMERICAN CYANAMID CO
    摘要:The disclosure describes an improved process for producing optically active compounds of Formula II or III, which compounds are useful as intermediates for preparing compounds active as inhibitors of retroviral protease enzymes: ##STR1## wherein R 1 , R 50 and Z are described in the specification. The improved process includes either synthesis of diastereomeric iodolactones which are separated prior to conversion to compounds of Formula II or III or synthesis of an epoxide which is converted directly to compounds of Formula II and III.

    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-6340760-B1
    优先权日:1998-06-26
    标题:Process for the preparation of (S)-N-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxyamide
    发明人:BELLANI PIETRO; FRIGERIO MARCO
    权利人:CLARIANT LSM ITALIA S P A
    摘要:A description is given here of a novel process for the synthesis of N-carboxyanhydride of formula VIby reacting (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid with triphosgene in dioxane; a description is also given of a process for the synthesis of (S)-N-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxyamide by treating the N-carboxyanhydride VI so obtained with tert-butylamine.

    专利号:US-6433177-B1
    优先权日:1999-11-25
    标 题 :Process for the preparation of (S)-N-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
    发明人:BELLANI PIETRO; BANFI ALDO
    权利人:CLARIANT LSM ITALIA S P A
    摘要:It is here described a new process for the synthesis of (S)-N-tertbutyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide wherein the N-carboxy anhydride of formulais treated with tert-butylamine in an organic inert solvent, preferably toluene, at a temperature of between -80 and -30° C.

    专利号:US-6586597-B1
    优先权日:1998-12-14
    标 题 :Continuous process for the preparation of optically pure decahydroisoquinolinecarboxamide
    发明人:PARK SANG-HOON; KWAK BYOUNG-SUNG; KIM TAE-YUN; LEE IN-WOO; OH SEUNG-HOON
    权利人:SK CORP
    摘要:The present invention relates to a continuous process for the preparation of [3S-(3α, 4 a β, 8 a β)]-N-tert-butyl-decahydro-3-isoquinolinecarboxamide, an intermediate useful in the synthesis of compounds for the treatment of viral diseases, from the reduction of N-tert-butyl-1,2,3,4-tetrahydro-3(S)-isoquinolinecarboxamide with a noble metal catalyst supported on inorganic oxide carrier in a fixed bed reaction system, with a high optical yield.
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    主要参考文献

    参考标题:Process For Synthesis Of Syn Azido Epoxide And Its Use As Intermediate For The Synthesis Of Amprenavir & Saquinavir
    摘要:Disclosed Herein Is A Novel Route Of Synthesis Of Syn Azide Epoxide Of Formula 5, Which Is Used As A Common Intermediate For Asymmetric Synthesis Of Hiv Protease Inhibitors Such As Amprenavir, Fosamprenavir, Saquinavir And Formal Synthesis Of Darunavir And Palinavir Obtained By Cobalt-Catalyzed Hydrolytic Kinetic Resolution Of Racemic Anti-(2Sr,3Sr)-3-Azido-4-Phenyl-1,2-Epoxybutane (Azido-Epoxide).

    合成参考文献


    摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).
    摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).
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