Smith Amos B, Chruma Jason J, Han Qiang, Barbosa Joseph
Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104-6323, USA.
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1697-702. doi: 10.1016/j.bmcl.2004.01.056.
The synthesis and structural analysis, involving X-ray crystallographic, nuclear magnetic resonance, and computational studies of four diastereomers of the common western BCD diarylether macrocycle of the complestatins, a family of HIV entry inhibitors, has been achieved exploiting a ruthenium-promoted intramolecular S(N)Ar reaction. The stereogenicity of the individual phenylglycines (residues C and D) results in remarkable effects on the backbone conformation.
利用钌促进的分子内S(N)Ar反应,已完成对复合他汀(一类HIV进入抑制剂)常见西方BCD二芳基醚大环的四种非对映异构体的合成及结构分析,其中包括X射线晶体学、核磁共振和计算研究。各个苯甘氨酸(残基C和D)的立体异构性对主链构象产生显著影响。