CAS: 76272-36-1; Exo-8-Benzyl-8-Azabicyclo[3.2.1]Octan-3-Amine

该化合物是一种双环矿衍生物,具有硬性丙环[3.2.1-1octane scarffold,具有外向型苯基替代成分,在8号位置上具有.这个结构具有...

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合成工艺路线路线简述

  • 合成目标产物 3-Amino-8-Benzyl-8-Azabicyclo[3.2.1]Octane (3-Exo)- 主要起始原料 1,3-Acetonedicarboxylic Acid
  • (文献来源)合成步骤主要原料 1,3-Acetonedicarboxylic Acid
📜Tert-Butyl (3-Exo-8-Benzyl-8-Azabicyclo[3.2.1]oct-3-yl)Carbamate 在 盐酸体系中,用 1,4-二氧六环,甲醇作为反应溶剂,反应 2.0H,以100%的收率获得exo-8-Benzyl-8-Azabicyclo[3.2.1]octan-3-Amine
参考文献:Preparation And Activities Of Macromolecule Conjugates Of The Ccr5 Antagonist Maravir°C
标题:Preparation And Activities Of Macromolecule Conjugates Of The Ccr5 Antagonist Maravir°C
摘要:Ccr5 Antagonists Are Among The Most Advanced Approaches In Hiv Therapy And May Also Be Relevant To Treatment Of Graft-Versus-Host Disease And Staphyloocus Aureus Infection. To Expand The Potential Of The Only Approved Ccr5 Antagonist,Maravir°C,We Studied Derivatives That Would Enable Functional Linkage Of Maravir°C To Long-Lived Carriers. Through Targeted Synthesis,We Discovered An Effective Linkage Site On Maravir°C And Demonstrate The Potential Of These Derivatives To Prepare Potent Chemically Programmed Antibodies And Pegylated Derivatives. The Resulting Compounds Effectively Neutralized A Variety Of Hiv-1 Isolates. Both Chemically Programmed Antibody And Pegylation Approaches Extend The Neutralization Activity Of Serum Circulating Maravir°C. Derivation Of A Successful Conjugation Strategy For Maravir°C Should Further Enable Its Use In Chemically Programmed Vaccines,Novel Bispecific Antibodies,And Topical Microbicides.
Doi:10.1021/Ml400370W

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合成参考文献

参考DOI号:10.1021/ml400370w
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