Mechanistic Study of the Spiroindolones: A New Class of Antimalarials
oleh: Thomas H. Keller, Bryan K. S. Yeung, Louis-Sebastian Sonntag, Seh Yong Leong, Peiling Yap, Bin Zou
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2012-08-01 |
Deskripsi
During the synthesis of the new antimalarial drug candidate NITD609, a high degree of diastereoselectivity was observed in the Pictet-Spengler reaction. By isolating both the <strong>4<em>E</em></strong> and <strong>4<em>Z</em></strong> imine intermediates, a systematic mechanistic study of the reaction under both kinetic and thermodynamic conditions was conducted. This study provides insight into the source of the diastereoselectivity for this important class of compounds.