Molecules | |
Mechanistic Study of the Spiroindolones: A New Class of Antimalarials | |
Bin Zou1  Peiling Yap1  Louis-Sebastian Sonntag1  Seh Yong Leong1  Bryan K. S. Yeung1  | |
[1] 1Novartis Institute for Tropical Diseases, 10 Biopolis Road, #05-01 Chromos, Singapore 2Experimental Therapeutics Centre, 31 Biopolis Drive, #03-01 Nanos, Singapore | |
关键词: malaria; spiroindolones; NITD609; Pictet-Spengler reaction; mechanism; | |
DOI : 10.3390/molecules170910131 | |
来源: mdpi | |
【 摘 要 】
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 4E and 4Z 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.
【 授权许可】
CC BY
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
【 预 览 】
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RO202003190042151ZK.pdf | 372KB | download |