CAS: 259214-56-7; Ethyl (1R,2S)-1-Amino-2-Vinylcyclopropane-1-Carboxylate Hydrochloride

该化合物是一种具有立体化学界定结构的手性环丙烷衍生物,在非对称合成和制药应用中具有价值;该化合物具有氨基和酯功能组的特点,能够进行多功能反应以进一步衍生;其盐酸盐形式增强了稳定性和溶解性,便利了处理和储存;乙烯基次成分为交叉或聚合反应提供了额外的再活性.该化合物在生物活性分子的合成中特别有用,包括消毒器和受限制的类似物.其高对应性能确保了立体选择性变异的一贯性,使其成为医药化学和农用化学研究的首选中间体.

结构式图片

相似化合物

213316-49-5 681807-59-0 259217-95-3

上下游产品

N-B°C-(1R,2S)-1-amino-2-vinylcyclopropane carboxylic acid ethyl ester (1S,2R)-ethyl 2-vinyl-1-(tert-butoxycarbonylamino)cyclopropanecarboxylate (1R,2S)-ethyl 1-(tert-butoxycarbonylamino)-2-vinylcyclopropanecarboxylate rac-(1R,2S)-1-amino-2-vinylcyclopropanecarboxylic acid ethyl ester2-(1-ethoxycarbonyl-2-vinyl-cyclopropylcarbamoyl)-4-(6-methoxy-2-phenyl-pyrimidin-4-yloxy)-cyclopentanecarboxylic acid 2-(1-ethoxycarbonyl-2-vinyl-cyclopropylcarbamoyl)-4-(6-methoxy-2-phenyl-pyrimidin-4-yloxy)-cyclopentanecarboxylic acid tert-butyl ester 1-{[2-(hex-5-enyl-methyl-carbamoyl)-4-(6-methoxy-2-phenylpyrimidin-4-yloxy)cyclopentanecarbonyl]-amino}-2-vinyl-cyclopropanecarboxylic acid ethyl ester (1R,2R,4R)-2-((1R,2S)-1-ethoxycarbonyl-2-vinyl-cyclopropylcarbamoyl)-4-(7-methoxy-2-phenyl-quinazolin-4-yloxy)-cyclopentanecarboxylic acid

合成工艺路线路线简述

    1-叔丁氧羰基氨基-2-乙烯基环丙烷甲酸乙酯置于盐酸,Sodium Hydroxide,Alcalase体系中,用 1,4-二氧六环,二甲基亚砜 用作溶剂,化学反应 28.0H,反应生成(1R,2S)-1-氨基-2-乙烯基-环丙羧酸乙酯盐酸盐(1:1)
    参考文献:Inhibitors Of Hepatitis C Virus
    标题:Inhibitors Of Hepatitis C Virus
    摘要:揭示了具有一般公式的大环肽: 其中描述了r3,R'3,R4,R6,R',X,Q和w.还公开了包含这些化合物的组合物以及使用这些化合物抑制hcv的方法.

    海关参考信息

    专利信息


    专利号:US-8987195-B2
    优先权日:2012-08-08
    标 题:HCV NS3 protease inhibitors
    发明人:BARA THOMAS; BHAT SATHESH; BISWAS DIPSHIKHA; BROCKUNIER LINDA; BURNETT DUANE A; CHACKALAMANNIL SAMUEL; CHELLIAH MARIAPPAN V; CHEN AUSTIN; CLASBY MARTIN; COLANDREA VINCE J; GUO ZHUYAN; HAN YONGXIN; JAYNE CHARLES; JOSIEN HUBERT; MARCANTONIO KAREN; MIAO SHOUWU; NEELAMKAVIL SANTHOSH; PINTO PATRICK; RAJAGOPALAN MURALI; SHAH UNMESH; VELAZQUEZ FRANCISCO; VENKATRAMAN SRIKANTH; XIA YAN
    权利人:MERCK SHARP & DOHME; MERCK CANADA INC
    摘要:The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.

    专利号:US-8591878-B2
    优先权日:2008-02-25
    标 题:Therapeutic compounds
    发明人:MCCAULEY JOHN A; LIVERTON NIGEL J; HARPER STEVEN; MCINTYRE CHARLES J; RUDD MICHAEL T
    权利人:MCCAULEY JOHN A; LIVERTON NIGEL J; HARPER STEVEN; MCINTYRE CHARLES J; RUDD MICHAEL T; MERCK SHARP & DOHME; ANGELETTI P IST RICHERCHE BIO
    摘要:A class of macrocyclic compounds of formula (I), wherein R 1 , R 3 , R 4 , R a , R b , A, B, Z, M, W and n are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.

    专利号:US-8278322-B2
    优先权日:2005-08-01
    标题 :HCV NS3 protease inhibitors
    发明人:HOLLOWAY M KATHARINE; LIVERTON NIGEL J; MCCAULEY JOHN A; RUDD MICHAEL T; VACCA JOSEPH P; LUDMERER STEVEN W; OLSEN DAVID B
    权利人:HOLLOWAY M KATHARINE; LIVERTON NIGEL J; MCCAULEY JOHN A; RUDD MICHAEL T; VACCA JOSEPH P; LUDMERER STEVEN W; OLSEN DAVID B; MERCK SHARP & DOHME
    摘要:The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

    专利号:US-9738661-B2
    优先权日:2006-10-27
    标题:HCV NS3 protease inhibitors
    发明人:LIVERTON NIGEL J; SUMMA VINCENZO; HARPER STEVEN; MCCAULEY JOHN A; ROMANO JOSEPH J; RUDD MICHAEL T
    权利人:MERCK SHARP & DOHME; MSD ITALIA SRL
    摘要:The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

    专利号:US-2013178413-A1
    优先权日:2010-09-21
    标题 :Hcv ns3 protease inhibitors
    发明人:MCCAULEY JOHN A; LIVERTON NIGEL J; RUDD MICHAEL T; GILBERT KEVIN F; FERRARA MARCO; SUMMA VINCENZO; CRESCENZI BENEDETTA
    权利人:MCCAULEY JOHN A; LIVERTON NIGEL J; RUDD MICHAEL T; GILBERT KEVIN F; FERRARA MARCO; SUMMA VINCENZO; CRESCENZI BENEDETTA
    摘要:The present invention relates to macrocyclic compounds of formula I that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
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    主要参考文献

    参考标题: Hcv Ns3 Protease Inhibitors Inhibiteurs De La Protéase Ns3 Du Vhc
    摘要:The Present Invention Relates To Hepatitis C Virus (Hcv) Ns3 Protease Inhibitors Containing A Spirocyclic Moeity, Uses Of Such Compounds, And Synthesis Of Such Compounds.
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