CAS: 185122-75-2; 6,7-Dihydro-5H-Cyclopenta[b]Pyridin-7-Amine

该化合物是一个环环有机化合物,其特点是双环结构,由环球组成,与环相连;该化合物在环的7位置上具有一个探雷功能组,有助于其潜在的反应和生物活动;二氢结构的存在表明,该化合物有另外两个氢原子,可影响其稳定性和相互作用;通常,这种化合物可能具有与药用化学有关的特性,包括药物中可能的应用,因为它们与生物目标相互作用的能力;分子结构可导致各种异构体形式,影响其物理和化学特性,例如可溶性,熔点和再活动;此外,该化合物的CAS编号(18512-1972-2),作为管制和研究目的的独特识别码,便于在各种化学数据库和文献中进行研究.

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CAS号1071727-78-0 (Z)-5H-环戊二烯并[b]...

合成工艺路线路线简述

    📜N-(6,7-Dihydro-5H-Cyclopenta[b]Pyridin-7-yl)Acetamide置于水体系中,化学反应生成6,7-二氢-5H-环戊并[b]吡啶-7-胺
    参考文献:Discovery Of Novel Small Molecule Orally Bioavailable C−x−c Chemokine Receptor 4 Antagonists That Are Potent Inhibitors Of T-Tropic (X4) Hiv-1 Replication
    标题:Discovery Of Novel Small Molecule Orally Bioavailable C−x−c Chemokine Receptor 4 Antagonists That Are Potent Inhibitors Of T-Tropic (X4) Hiv-1 Replication
    摘要:The Redesign Of Azamacrocyclic Cxcr4 Chemokine Receptor Antagonists Resulted In The Discovery Of Novel,Small Molecule,Orally Bioavailable Compounds That Retained T-Tropic (Cxcr4 Using,X4) Anti-Hiv-1 Activity. A Structure Activity Relationship (Sa R) Was Determined On The Basis Of The Inhibition Of Replication Of X4 Hiv-1 Nl4.3 In Mt-4 Cells. As A Result Of Lead Optimization,We Identified (S)-N'-((1H-Benzo[d]Imidazol-2-Amethyl)-N'-(5,6,7,8-Tetrahydroquinolin-8-yl)Butane-1,4-Diamine (Amd070) 2 As A Potent And Selective Antagonist Of Cxcr4 With An Ic(50) Value Of 13 Nm In A Cxcr4 (125)I-Sdf Inhibition Binding Assay. Compound 2 Inhibited The Replication Of T-Tropic Hiv-1 (Nl4.3 Strain) In Mt-4 Cells And Pbmcs With An Ic(50) Of 2 And 26 Nm,Respectively,While Remaining Noncytotoxic To Cells At Concentrations Exceeding 23 Mu M. The Pharmacokinetics Of 2 Was Evaluated In Rat And Dog,And Good Oral Bioavailability Was Observed In Both Species. This Compound Represents The First Small Molecule Orally Bioavailable Cxcr4 Antagonist That Was Developed For The Treatment Of Hiv-1 Infection.
    Doi:10.1021/jm100073M

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    专利信息


    专利号:US-7452994-B2
    优先权日:2001-09-12
    标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
    发明人：MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN
    权利人:ANORMED INC
    摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.

    专利号:US-2003114679-A1
    优先权日:2001-09-12
    标 题:Synthesis of enantiomerically pure amino-substituted fused bicyclic rings

    专利号:US-2005080267-A1
    优先权日:2001-09-12
    标 题:Synthesis of enantiomerically pure amino-substituted fused bicyclic rings

    专利号:US-2007060757-A1
    优先权日:2001-09-12
    标题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings

    专利号:EP-1487795-A2
    优先权日:2001-09-12
    标题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings

    专利号:EP-1487795-A4
    优先权日:2001-09-12
    标题 :SYNTHESIS OF ENANTIOMERICALLY PURE AMINO-SUBSTITUTED FUSIONNATED BICYCLIC CORES

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    合成参考文献


    摘要:Azov, V. A., Science of Synthesis, (2009) 40, 421.
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