📜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